[go: up one dir, main page]

AR063680A1 - Derivados de pirazolo[1, 5-a]pirimidina, metodos e intermediario para su preparacion, composiciones farmaceuticas que los comprenden y su uso en la fabricacion de medicamentos para el tratamiento de enfermedades mediadas por la modulacion de mglur5. - Google Patents

Derivados de pirazolo[1, 5-a]pirimidina, metodos e intermediario para su preparacion, composiciones farmaceuticas que los comprenden y su uso en la fabricacion de medicamentos para el tratamiento de enfermedades mediadas por la modulacion de mglur5.

Info

Publication number
AR063680A1
AR063680A1 ARP070103437A ARP070103437A AR063680A1 AR 063680 A1 AR063680 A1 AR 063680A1 AR P070103437 A ARP070103437 A AR P070103437A AR P070103437 A ARP070103437 A AR P070103437A AR 063680 A1 AR063680 A1 AR 063680A1
Authority
AR
Argentina
Prior art keywords
alkylaminocarbonyl
alkylamino
alkyl
aryl
heterocyclyl
Prior art date
Application number
ARP070103437A
Other languages
English (en)
Original Assignee
Merz Pharma Gmbh & Co Kgaa
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 Merz Pharma Gmbh & Co Kgaa filed Critical Merz Pharma Gmbh & Co Kgaa
Publication of AR063680A1 publication Critical patent/AR063680A1/es

Links

Classifications

    • 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
    • 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
    • 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
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/08—Drugs for disorders of the alimentary tract or the digestive system for nausea, cinetosis or vertigo; Antiemetics
    • 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
    • A61P1/14—Prodigestives, e.g. acids, enzymes, appetite stimulants, antidyspeptics, tonics, antiflatulents
    • 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
    • A61P11/04—Drugs for disorders of the respiratory system for throat disorders
    • 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
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/02—Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
    • 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
    • A61P17/04—Antipruritics
    • 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
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A61P21/02—Muscle relaxants, e.g. for tetanus or cramps
    • 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
    • A61P25/02—Drugs for disorders of the nervous system for peripheral neuropathies
    • 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
    • A61P25/06—Antimigraine agents
    • 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
    • A61P25/08—Antiepileptics; Anticonvulsants
    • 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
    • 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
    • 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
    • A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • 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
    • A61P25/20—Hypnotics; Sedatives
    • 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
    • A61P25/22—Anxiolytics
    • 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
    • A61P25/24—Antidepressants
    • 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
    • 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
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/32—Alcohol-abuse
    • 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
    • A61P25/34—Tobacco-abuse
    • 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
    • A61P25/36—Opioid-abuse
    • 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
    • A61P27/02—Ophthalmic agents
    • 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
    • A61P27/02—Ophthalmic agents
    • A61P27/06—Antiglaucoma agents or miotics
    • 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
    • A61P27/16—Otologicals
    • 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
    • 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
    • A61P3/04—Anorexiants; Antiobesity agents
    • 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
    • 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
    • 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
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • 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
    • 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
    • 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
    • C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Psychiatry (AREA)
  • Addiction (AREA)
  • Pain & Pain Management (AREA)
  • Pulmonology (AREA)
  • Hematology (AREA)
  • Diabetes (AREA)
  • Immunology (AREA)
  • Obesity (AREA)
  • Ophthalmology & Optometry (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Rheumatology (AREA)
  • Oncology (AREA)
  • Otolaryngology (AREA)
  • Psychology (AREA)
  • Urology & Nephrology (AREA)
  • Cardiology (AREA)
  • Hospice & Palliative Care (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Vascular Medicine (AREA)
  • Communicable Diseases (AREA)
  • Child & Adolescent Psychology (AREA)

Abstract

Estos compuestos son potentes moduladores de mGluR5 y son útiles, por ejemplo, para el tratamiento de diversos trastornos neurológicos. Reivindicación 1: Un compuesto de pirazolo-pirimidina de fórmula (1) donde Y1, Y2 e Y3 independientemente son CR10, CR11, CR10R11, NR12, S o O, donde al menos uno de Y1, Y2 e Y3 denota CR10; o Y1 e Y2 juntos denotan un grupo R10C=N; R10C=CR11; R10R11C-C(=O) o R12N-(C=O); o Y2 e Y3 juntos denotan un grupo R10C=N; R10C=CR11; R10R11C-C(=O) o R12N-(C=O); R1 representa cloro o bromo; R2 representa hidrógeno, alquilo C1-6, cicloalquiIo C3-7 o trifluorometilo; R3 representa hidrógeno, alquilo C1-6, cicloaIquilo C3-7 o trifluorometilo; o R2 y R3, junto con el átomo de carbono del anillo, representan un grupo carbonilo; R4 representa hidrógeno, alquilo C1-6, cicloalquilo C3-7 o trifluorometilo; R5 representa hidrógeno, alquilo C1-6, cicloalquilo C3-7 o trifluorometilo; o R4 y R5, junto con el átomo de carbono del anillo, representan un grupo carbonilo; R6 representa hidrógeno, alquilo C1-6, cicloalquilo C3-7 o trifluorometilo; R7 representa hidrógeno, alquilo C1-6, cicloalquilo C3-7 o trifluorometilo; R6 y R7, junto con el átomo de carbono del anillo, representan un grupo carbonilo; R2 o R3, junto con R6 o R7, pueden formar un radical bivalente del tipo CH2-CH2 o CH2-O; R10 y R11 independientemente representan hidrógeno, halógeno, amino, hidroxi, nitro, ciano, trifluorometilo, trifluorometoxi, arilo, alquilo C1-6, cicloalquilo C3- 7, alquenilo C2-6, alquinilo C2-6, alcoxi C1-6, cicloalquiloxi C3-7, alqueniloxi C2-6, alquiniloxi C2-6, heteroarilo, heterociclilo, ariloxi, heteroariloxi, heterocicliloxi, alquilamino C1-6, di-alquilamino C1-6, cicloalquilamino C3-7, di- cicloalquilamino C3-7, alquil C1-6-cicloalquilamino C3-7, alquenilamino C2-6, alquinilamino C2-6, di-alquenilamino C2-6, di-alquinilamino C2-6, alquil C1-6-alquenilamino C2-6, alquil C1-6-alquinilamino C2-6, alquenil C2-6-cicloalquilamino C3-7, alquinil C2-6-cicloalquilamino C3-7, alquenil C2-6-alquinilamino C2-6, arilamino, diarilamino, aril-alquilamino C1-6, aril-alquenilamino C2-6, aril-alquinilamino C2-6, aril-cicloalquilamino C3-7, heteroarilamino, diheteroarilamino, heteroaril- alquilamino C1-6, heteroaril-alquenilamino C2-6, heteroaril-alquinilamino C2-6, heteroaril-cicloalquilamino C3-7, heteroarilarilamino, heterociclilamino, diheterociclilamino, heterociclilalquilamino C1-6, heterociclil-alquenilamino C2-6, heterociclil-alquinilamino C2-6, heterociclil-cicloalquilamino C3-7, heterociclilarilamino, heterociclilheteroarilamino, acil, aciloxi, acilamino, alcoxicarbonilo C1-6, cicloalcoxicarbonilo C3-7, alqueniloxicarbonilo C2-6, alquiniloxicarbonilo C2-6, ariloxicarbonilo, heteroariloxicarbonilo, heterocicliloxicarbonilo, aminocarbonilo, alquilamino-carbonilo C1-6, di-alquilaminocarbonilo C1-6, cicloalquilaminocarbonilo C3-7, di-cicloalquilaminocarbonilo C3-7, aIquil C1-6-cicloalquilaminocarbonilo C3- 7, alquenil-aminocarbonilo C2-6, alquinil-aminocarbonilo C2-6, di-alquenilaminocarbonilo C2-6, di-alquinilaminocarbonilo C2-6, alquil C1-6-alquenilaminocarbonilo C2-6, aIquil C1-6-alquinil-aminocarbonilo C2-6, alquenil C2-6- cicloalquilaminocarbonilo C3-7, alquinil C2-6-cicloalquilaminocarbonilo C3-7, alqueniI C2-6-alquinilaminocarbonilo C2-6, arilaminocarbonilo, diarilaminocarbonilo, aril-alquilaminocarbonilo C1-6, aril-alquenilaminocarbonilo C2-6, aril- alquinilaminocarbonilo C2-6, aril- cicloalquilaminocarbonilo C3-7, heteroarilaminocarbonilo, diheteroarilaminocarbonilo, heteroaril-alquilaminocarbonilo C1-6, heteroaril-alquenilaminocarbonilo C2-6, heteroaril-alquinilaminocarbonilo C2-6, heteroaril- cicloalquilaminocarbonilo C3-7, heteroarilarilaminocarbonilo, heterociclilaminocarbonilo, diheterociclilamino-carbonilo, heterociclil-alquilaminocarbonilo C1-6, heterociclil-alquenilamino-carbonilo C2-6, heterociclil-alquinilaminocarbonilo C2-6, heterociclil- cicloalquilaminocarbonilo C3-7, heterociclilarilaminocarbonilo, heterociclilheteroarilamino-carbonilo, alquilsulfinilo C1-6, cicloalquilsulfinilo C3-7, alquenilsulfinilo C2-6, alquinilsulfinilo C2-6, arilsulfinilo, heteroarilsulfinilo, heterociclilsulfinilo, alquilsulfonilo C1-6, cicloalquilsulfonilo C3-7, alquenilsulfonilo C2-6, alquinilsulfonilo C2-6, arilsulfonilo, heteroarilsulfonilo, heterociclilsulfonilo, alquilsulfonilamino C1-6 o arilsulfonilamino; y R12 representa hidrógeno, alquilo C1-6, cicloalquilo C3-7, alquenilo C2-6, alquinilo C2-6, acilo, arilo, heteroarilo, heterociclilo, alquilamino-carbonilo C1-6, di-alquilamino-carbonilo C1-6, alquilsulfonilo C1-6, arilsulfonilo o heteroarilsulfonilo; e isómeros ópticos, sales, hidratos, solvatos y polimorfos farmacéuticamente aceptables de dicho compuesto. Reivindicación 29: Un proceso para la síntesis de un compuesto seleccionado entre aquellos de fórmula (1) donde: Y1, Y2 e Y3 independientemente son CR10, CR11, CR10R11, NR12, S o O, donde al menos uno de Y1, Y2 e Y3 denota CR10; o Y1 e Y2 juntos denotan un grupo R10C=N; R10C=CR11; R10R11C-C(=O) o R12N-(C=O); o Y2 e Y3 juntos denotan un grupo R10C=N; R10C=CR11; R10R11C-C(=O) o R12N-(C=O); R1 representa cloro o bromo; R2 representa hidrógeno, alquilo C1-6, cicloalquiIo C3-7 o trifluorometilo; R3 representa hidrógeno, alquilo C1-6, cicloaIquilo C3-7 o trifluorometilo; o R2 y R3, junto con el átomo de carbono del anillo, representan un grupo carbonilo; R4 representa hidrógeno, alquilo C1-6, cicloalquilo C3-7 o trifluorometilo; R5 representa hidrógeno, alquilo C1-6, cicloalquilo C3-7 o trifluorometilo; o R4 y R5, junto con el átomo de carbono del anillo, representan un grupo carbonilo; R6 representa hidrógeno, alquilo C1-6, cicloalquilo C3-7 o trifluorometilo; R7 representa hidrógeno, alquilo C1-6, cicloalquilo C3-7 o trifluorometilo; R6 y R7, junto con el átomo de carbono del anillo, representan un grupo carbonilo; R2 o R3, junto con R6 o R7, pueden formar un radical bivalente del tipo CH2-CH2 o CH2-O; R10 y R11 independientemente representan hidrógeno, halógeno, amino, hidroxi, nitro, ciano, trifluorometilo, trifluorometoxi, arilo, alquilo C1-6, cicloalquilo C3- 7, alquenilo C2-6, alquinilo C2-6, alcoxi C1-6, cicloalquiloxi C3-7, alqueniloxi C2-6, alquiniloxi C2-6, heteroarilo, heterociclilo, ariloxi, heteroariloxi, heterocicliloxi, alquilamino C1-6, di-alquilamino C1-6, cicloalquilamino C3-7, di- cicloalquilamino C3-7, alquil C1-6-cicloalquilamino C3-7, alquenilamino C2-6, alquinilamino C2-6, di-alquenilamino C2-6, di-alquinilamino C2-6, alquil C1-6-alquenilamino C2-6, alquil C1-6-alquinilamino C2-6, alquenil C2-6-cicloalquilamino C3-7, alquinil C2-6-cicloalquilamino C3-7, alquenil C2-6-alquinilamino C2-6, arilamino, diarilamino, aril-alquilamino C1-6, aril-alquenilamino C2-6, aril-alquinilamino C2-6, aril-cicloalquilamino C3-7, heteroarilamino, diheteroarilamino, heteroaril- alquilamino C1-6, heteroaril-alquenilamino C2-6, heteroaril-alquinilamino C2-6, heteroaril-cicloalquilamino C3-7, heteroarilarilamino, heterociclilamino, diheterociclilamino, heterociclilalquilamino C1-6, heterociclil-alquenilamino C2-6, heterociclil-alquinilamino C2-6, heterociclil-cicloalquilamino C3-7, heterociclilarilamino, heterociclilheteroarilamino, acil, aciloxi, acilamino, alcoxicarbonilo C1-6, cicloalcoxicarbonilo C3-7, alqueniloxicarbonilo C2-6, alquiniloxicarbonilo C2-6, ariloxicarbonilo, heteroariloxicarbonilo, heterocicliloxicarbonilo, aminocarbonilo, alquilamino-carbonilo C1-6, di-alquilaminocarbonilo C1-6, cicloalquilaminocarbonilo C3-7, di-cicloalquilaminocarbonilo C3-7, aIquil C1-6-cicloalquilaminocarbonilo C3- 7, alquenil-aminocarbonilo C2-6, alquinil-aminocarbonilo C2-6, di-alquenilaminocarbonilo C2-6, di-alquinilaminocarbonilo C2-6, alquil C1-6-alquenilaminocarbonilo C2-6, aIquil C1-6-alquinil-aminocarbonilo C2-6, alquenil C2-6- cicloalquilaminocarbonilo C3-7, alquinil C2-6-cicloalquilaminocarbonilo C3-7, alqueniI C2-6-alquinilaminocarbonilo C2-6, arilaminocarbonilo, diarilaminocarbonilo, aril-alquilaminocarbonilo C1-6, aril-alquenilaminocarbonilo C2-6, aril- alquinilaminocarbonilo C2-6, aril- cicloalquilaminocarbonilo C3-7, heteroarilaminocarbonilo, diheteroarilaminocarbonilo, heteroaril-alquilaminocarbonilo C1-6, heteroaril-alquenilaminocarbonilo C2-6, heteroaril-alquinilaminocarbonilo C2-6, heteroaril- cicloalquilaminocarbonilo C3-7, heteroarilarilaminocarbonilo, heterociclilaminocarbonilo, diheterociclilamino-carbonilo, heterociclil-alquilaminocarbonilo C1-6, heterociclil-alquenilamino-carbonilo C2-6, heterociclil-alquinilaminocarbonilo C2-6, heterociclil- cicloalquilaminocarbonilo C3-7, heterociclilarilaminocarbonilo, heterociclilheteroarilamino-carbonilo, alquilsulfinilo C1-6, cicloalquilsulfinilo C3-7, alquenilsulfinilo C2-6, alquinilsulfinilo C2-6, arilsulfinilo, heteroarilsulfinilo, heterociclilsulfinilo, alquilsulfonilo C1-6, cicloalquilsulfonilo C3-7, alquenilsulfonilo C2-6, alquinilsulfonilo C2-6, arilsulfonilo, heteroarilsulfonilo, heterociclilsulfonilo, alquilsulfonilamino C1-6 o arilsulfonilamino; y R12 representa hidrógeno, alquilo C1-6, cicloalquilo C3-7, alquenilo C2-6, alquinilo C2-6, acilo, arilo, heteroarilo, heterociclilo, alquilamino-carbonilo C1-6, di-alquilamino-carbonilo C1-6, alquilsulfonilo C1-6, arilsulfonilo o heteroarilsulfonilo; e isómeros ópticos, sales, hidratos, solvatos y polimorfos farmacéuticamente aceptables de dicho compuesto, donde un compuesto de fórmula (2) se suspende en una mezcla de etanol y agua y se trata con ácido clorhídrico, seguido por la reacción con H2NNHCOOCH3, para proporcionar un compuesto de fórmula (3), el cual se hace reaccionar con un compuesto de fórmula (4) para proporcionar un compuesto de fórmula (5) el cual se hidroliza en condiciones ácidas para proporcionar un compuesto de fórmula (6) el cual se trata con una amina de fórmula (7) en presencia de un agente de condensación, para proporcionar un compuesto de fórmula (1), el cual se convierte, si así se desea, en una sal, hidrato, solvato o polimorfo farmacé
ARP070103437A 2006-08-04 2007-08-03 Derivados de pirazolo[1, 5-a]pirimidina, metodos e intermediario para su preparacion, composiciones farmaceuticas que los comprenden y su uso en la fabricacion de medicamentos para el tratamiento de enfermedades mediadas por la modulacion de mglur5. AR063680A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US83582006P 2006-08-04 2006-08-04
US87754406P 2006-12-28 2006-12-28

Publications (1)

Publication Number Publication Date
AR063680A1 true AR063680A1 (es) 2009-02-11

Family

ID=38710494

Family Applications (3)

Application Number Title Priority Date Filing Date
ARP070103437A AR063680A1 (es) 2006-08-04 2007-08-03 Derivados de pirazolo[1, 5-a]pirimidina, metodos e intermediario para su preparacion, composiciones farmaceuticas que los comprenden y su uso en la fabricacion de medicamentos para el tratamiento de enfermedades mediadas por la modulacion de mglur5.
ARP070103439A AR062210A1 (es) 2006-08-04 2007-08-03 Pirazolopirimidinas sustituidas, un proceso para su preparacion y su uso como medicamento
ARP070103438A AR062209A1 (es) 2006-08-04 2007-08-03 Pirazolopirimidinas moduladoras de receptores de glutamato metabotropicos mglur5, proceso para su preparacion, medicamentos que las contienen y usos en la prevencion y/o tratamiento de trastornos neurologicos agudos y cronicos.

Family Applications After (2)

Application Number Title Priority Date Filing Date
ARP070103439A AR062210A1 (es) 2006-08-04 2007-08-03 Pirazolopirimidinas sustituidas, un proceso para su preparacion y su uso como medicamento
ARP070103438A AR062209A1 (es) 2006-08-04 2007-08-03 Pirazolopirimidinas moduladoras de receptores de glutamato metabotropicos mglur5, proceso para su preparacion, medicamentos que las contienen y usos en la prevencion y/o tratamiento de trastornos neurologicos agudos y cronicos.

Country Status (21)

Country Link
US (4) US7985753B2 (es)
EP (3) EP2054416B8 (es)
JP (2) JP2009545569A (es)
KR (1) KR20090047450A (es)
AR (3) AR063680A1 (es)
AT (2) ATE494289T1 (es)
AU (2) AU2007280429A1 (es)
BR (2) BRPI0714622A2 (es)
CA (2) CA2659876A1 (es)
CY (1) CY1112003T1 (es)
DE (2) DE602007011773D1 (es)
DK (1) DK2054416T3 (es)
HR (1) HRP20110128T1 (es)
IL (2) IL196008A0 (es)
MX (2) MX2009001036A (es)
PL (1) PL2054416T3 (es)
PT (1) PT2054416E (es)
RU (2) RU2450004C2 (es)
TW (3) TW200823215A (es)
WO (3) WO2008015270A1 (es)
ZA (1) ZA200810605B (es)

Families Citing this family (28)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2008056176A1 (en) * 2006-11-10 2008-05-15 Scottish Biomedical Limited Pyrazolopyrimidines as phosphodiesterase inhibitors
JP5856990B2 (ja) * 2007-03-31 2016-02-10 インターベット インターナショナル ベー． フェー． ジルパテロールおよびこの塩の製造方法
EP2090576A1 (en) * 2008-02-01 2009-08-19 Merz Pharma GmbH & Co.KGaA 6-halo-pyrazolo[1,5-a]pyridines, a process for their preparation and their use as metabotropic glutamate receptor (mGluR) modulators
US8703809B2 (en) * 2008-06-30 2014-04-22 Novartis Ag Combination products
WO2011064237A1 (en) 2009-11-25 2011-06-03 Merz Pharma Gmbh & Co. Kgaa Crystalline forms of substituted pyrazolopyrimidines
AU2011338339A1 (en) 2010-12-08 2013-06-27 Vanderbilt University Bicyclic pyrazole compounds as allosteric modulators of mGluR5 receptors
US8865725B2 (en) 2011-03-15 2014-10-21 Vanderbilt University Substituted imidazopyrimidin-5(6H)-ones as allosteric modulators of MGLUR5 receptors
CA2830220A1 (en) * 2011-03-15 2012-09-20 Vanderbilt University Substituted imidazopyrimidin-5(6h)-ones as allosteric modulators of mglur5 receptors
WO2012139876A1 (en) 2011-04-14 2012-10-18 Merz Pharma Gmbh & Co. Kgaa Enteric formulations of metabotropic glutamate receptor modulators
US8791108B2 (en) 2011-08-18 2014-07-29 Bristol-Myers Squibb Company Inhibitors of human immunodeficiency virus replication
WO2013087815A1 (en) 2011-12-15 2013-06-20 Merz Pharma Gmbh & Co. Kgaa Liquid pharmaceutical composition containing a pyrazolopyrimidine derivative and pharmaceutical uses thereof
WO2013087808A1 (en) 2011-12-15 2013-06-20 Merz Pharma Gmbh & Co. Kgaa Pharmaceutical composition comprising a pyrazolopyrimidme and cyclodextrin
US9006235B2 (en) 2012-03-06 2015-04-14 Bristol-Myers Squibb Company Inhibitors of human immunodeficiency virus replication
WO2013144172A1 (en) * 2012-03-29 2013-10-03 Boehringer Ingelheim International Gmbh Novel pyrazolopyrimidines
JO3407B1 (ar) 2012-05-31 2019-10-20 Eisai R&D Man Co Ltd مركبات رباعي هيدرو بيرازولو بيريميدين
WO2014035707A1 (en) * 2012-08-25 2014-03-06 The Johns Hopkins University Gapdh cascade inhibitor compounds and methods of use and treatment of stress induced disorders including mental illness
MD20150071A2 (ro) 2013-02-19 2016-02-29 Pfizer Inc. Compuşi azabenzimidazolici ca inhibitori ai PDE4 izoenzimelor pentru tratamentul tulburărilor SNC şi altor afecţiuni
WO2014164428A1 (en) 2013-03-13 2014-10-09 Bristol-Myers Squibb Company Inhibitors of human immunodeficiency virus replication
CN105189511B (zh) 2013-03-13 2017-05-24 百时美施贵宝公司 人免疫缺陷病毒复制的抑制剂
US9540393B2 (en) 2013-03-14 2017-01-10 VIIV Healthcare UK (No.5) Limited Inhibitors of human immunodeficiency virus replication
WO2014197536A2 (en) 2013-06-04 2014-12-11 Temple University Of The Commonwealth Novel beta lactams as modulators of glutamate uptake and methods for use thereof
CN106102730A (zh) 2013-11-05 2016-11-09 天普大学高等教育联合体 作为抗微生物剂的聚阳离子两亲物
US10398142B2 (en) 2013-11-05 2019-09-03 Temple University Of The Commonwealth System Of Higher Education Polycationic amphiphiles as antimicrobial agents
GB201320905D0 (en) 2013-11-27 2014-01-08 Takeda Pharmaceutical Therapeutic compounds
US9273067B2 (en) 2014-02-19 2016-03-01 Bristol-Myers Squibb Company Pyrazolopyrimidine macrocycles as inhibitors of human immunodeficiency virus replication
US10131669B2 (en) 2014-07-24 2018-11-20 Pfizer Inc. Pyrazolopyrimidine compounds
HUE044040T2 (hu) 2014-08-06 2019-09-30 Pfizer Imidazopiridazin vegyületek
EP3407886A1 (en) 2016-01-27 2018-12-05 Universität Zürich Use of gabaa receptor modulators for treatment of itch

Family Cites Families (34)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CH603545A5 (es) 1972-04-20 1978-08-31 Merz & Co
GB1383409A (en) * 1972-09-09 1974-02-12 Pfizer Ltd Derivatives of 2-amino- and 4-amino-quinazoline and pharmaceutical compositions containing them
US3988339A (en) 1974-02-08 1976-10-26 Smithkline Corporation Pharmaceutical compositions and methods of inhibiting phenylethanolamine N-methyltransferase
US3974283A (en) * 1974-03-18 1976-08-10 Sandoz, Inc. N-substituted-4-T-butyl-1-pyridinethiocarboxamides and their use for treatment of inflammation or pain
NZ190915A (en) * 1978-07-31 1984-07-31 Hoffmann La Roche Oxadiazolotriazine derivatives and pharmaceutical compositions
DE2856393C2 (de) 1978-12-27 1983-04-28 Merz + Co GmbH & Co, 6000 Frankfurt Arzneimittel zur Behandlung von Morbus Parkinson
US4340597A (en) * 1981-04-13 1982-07-20 Schering Corporation 1-Substituted-4-aryl-1,2,5,6-tetrahydro and hexahydropyridines
DE3308554A1 (de) * 1983-03-10 1984-09-13 Hoechst Ag, 6230 Frankfurt 1-/1,3-dioxolan-2-ylmethyl)-azole, ihre salze, verfahren zu ihrer herstellung und ihre verwendung
WO1989005643A1 (en) * 1987-12-18 1989-06-29 Pfizer Inc. Heterocyclic-substituted quinoline-carboxylic acids
ES2059602T3 (es) 1989-04-14 1994-11-16 Merz & Co Gmbh & Co Uso de derivados de adamantano para la prevencion y tratamiento de isquemia cerebral.
US6177443B1 (en) * 1997-03-07 2001-01-23 Novo Nordisk A/S 4,5,6,7-tetrahydro-thieno[3, 2-C]pyridine derivatives, their preparation and use
ES2200358T3 (es) 1997-06-30 2004-03-01 MERZ PHARMA GMBH & CO. KGAA 1-amino-alquilciclohexanos antagonistas del receptor de nmda.
US6071966A (en) 1997-06-30 2000-06-06 Merz + Co. Gmbh & Co. 1-amino-alkylcyclohexane NMDA receptor antagonists
DE19732589A1 (de) * 1997-07-29 1999-02-04 Huels Chemische Werke Ag Verfahren zur Herstellung von 1,2,3,6-tetrahydro-2,2,6,6-tetramethylpyridin
FR2769313B1 (fr) * 1997-10-06 2000-04-21 Sanofi Sa Derives d'esters hydroxyacetiques, leur procede de preparation et leur utilisation comme intermediaires de synthese
CN1158264C (zh) 1997-11-21 2004-07-21 Nps药物有限公司 用于治疗中枢神经系统疾病的代谢性谷氨酸受体拮抗剂
ATE290527T1 (de) * 1997-12-25 2005-03-15 Meiji Seika Kaisha Tetrahydrobenzindol-derivate
JP2002523448A (ja) 1998-08-28 2002-07-30 サイオス インコーポレイテッド ｐ３８−αキナーゼのインヒビター
US20020049223A1 (en) 1999-11-05 2002-04-25 Elmore Steven W. Quinoline and naphthyridine carboxylic acid antibacterials
AU776933B2 (en) * 1999-12-28 2004-09-23 Eisai R&D Management Co., Ltd. Heterocyclic compounds having sulfonamide groups
GB0110338D0 (en) 2001-04-27 2001-06-20 Sb Pharmco Inc Novel processes
GB0118752D0 (en) * 2001-08-01 2001-09-26 Pfizer Ltd Process for the production of quinazolines
US6833371B2 (en) * 2001-11-01 2004-12-21 Icagen, Inc. Pyrazolopyrimidines
MXPA04010441A (es) 2002-04-23 2005-02-14 Shionogi & Co Derivado de pirazolo[1,5-a]pirimidina e inhibidor de nad(p)h oxidasa que contiene el mismo.
AR040126A1 (es) * 2002-05-29 2005-03-16 Glaxo Group Ltd Compuesto de fenilsulfonilo, composicion farmaceutica que lo comprende y su uso para la elaboracion de un medicamento
CA2487211C (en) 2002-06-04 2010-09-14 Neogenesis Pharmaceuticals, Inc. Pyrazolo(1,5a) pyrimidine compounds as antiviral agents
MXPA05001590A (es) * 2002-08-09 2005-05-23 Astrazeneca Ab Compuestos que tienen actividad en los receptores metabotropicos de glutamato.
WO2004087153A2 (en) 2003-03-28 2004-10-14 Chiron Corporation Use of organic compounds for immunopotentiation
JP2006522744A (ja) 2003-04-11 2006-10-05 ノボ　ノルディスク　アクティーゼルスカブ グルココルチコイド受容体アゴニスト療法に伴う副作用を最小化するための、１１β−ヒドロキシステロイドデヒドロゲナーゼ１型阻害剤およびグルココルチコイド受容体アゴニストを使用する併用療法
JP2006522750A (ja) 2003-04-11 2006-10-05 ノボ　ノルディスク　アクティーゼルスカブ 代謝性症候群ならびに関連の疾患および障害を治療するために、１１β−ヒドロキシステロイドデヒドロゲナーゼ１型阻害剤および抗高血圧剤を使用する併用療法
EP1615697A2 (en) * 2003-04-11 2006-01-18 Novo Nordisk A/S New pyrazolo[1,5-a] pyrimidine derivatives and pharmaceutical use thereof
EP1773880A4 (en) 2004-06-08 2009-09-09 Novartis Vaccines & Diagnostic ENV POLYPEPTIDE COMPLEXES AND METHOD FOR THEIR USE
US20080051409A1 (en) 2004-08-02 2008-02-28 Peter Gmeiner Indolizine Carboxamides and Aza and Diaza Derivatives Thereof
EP1841766A1 (en) 2005-01-19 2007-10-10 Biolipox AB Pyrrolopyridines useful in the treatment of inflammation

Also Published As

Publication number Publication date
BRPI0714622A2 (pt) 2013-04-30
RU2009107686A (ru) 2010-09-10
EP2054421B1 (en) 2010-11-17
BRPI0714766A2 (pt) 2013-07-16
IL196007A0 (en) 2009-09-01
WO2008015269A1 (en) 2008-02-07
PL2054416T3 (pl) 2011-05-31
PT2054416E (pt) 2011-04-06
US7947689B2 (en) 2011-05-24
US7985753B2 (en) 2011-07-26
EP2295439A1 (en) 2011-03-16
ATE494289T1 (de) 2011-01-15
US20110212956A1 (en) 2011-09-01
EP2054416A1 (en) 2009-05-06
AR062209A1 (es) 2008-10-22
US20080039458A1 (en) 2008-02-14
AU2007280429A1 (en) 2008-02-07
DE602007011773D1 (de) 2011-02-17
AU2007280428B2 (en) 2012-04-12
DK2054416T3 (da) 2011-04-04
ZA200810605B (en) 2009-12-30
ATE488520T1 (de) 2010-12-15
KR20090047450A (ko) 2009-05-12
EP2054416B8 (en) 2014-07-16
JP2009545569A (ja) 2009-12-24
DE602007010640D1 (de) 2010-12-30
EP2054421A1 (en) 2009-05-06
WO2008015271A1 (en) 2008-02-07
CA2659876A1 (en) 2008-02-07
JP2010500288A (ja) 2010-01-07
WO2008015270A1 (en) 2008-02-07
HRP20110128T1 (hr) 2011-03-31
TWI399376B (zh) 2013-06-21
AR062210A1 (es) 2008-10-22
TW200823215A (en) 2008-06-01
EP2054416B1 (en) 2011-01-05
US20080039476A1 (en) 2008-02-14
IL196008A0 (en) 2009-09-01
CY1112003T1 (el) 2015-11-04
RU2009107688A (ru) 2010-09-10
MX2009001036A (es) 2009-04-23
US20080032998A1 (en) 2008-02-07
RU2450004C2 (ru) 2012-05-10
MX2009000919A (es) 2009-04-16
TW200817394A (en) 2008-04-16
AU2007280428A1 (en) 2008-02-07
CA2659871A1 (en) 2008-02-07
TW200815432A (en) 2008-04-01

Similar Documents

Publication Publication Date Title
AR063680A1 (es) Derivados de pirazolo[1, 5-a]pirimidina, metodos e intermediario para su preparacion, composiciones farmaceuticas que los comprenden y su uso en la fabricacion de medicamentos para el tratamiento de enfermedades mediadas por la modulacion de mglur5.
ES2905318T3 (es) Profármacos de riluzol y su uso
ES2545865T3 (es) Compuestos de pirazol como antagonistas de CRTH2
AR059064A1 (es) Compuestos de tiazol, composiciones farmaceuticas que los contienen y usos en el tratamiento de enfermedades mediadas por la proteina quinasa b(pkb), tales como cancer.
PE20040164A1 (es) Mimeticos de glucocorticoides, procedimientos para su preparacion y composiciones farmaceuticas
DE60335869D1 (de) 1h-benzo(f)indazol-5-yl-derivate als selektive glucocorticoid-rezeptor-modulatoren
NO20080865L (no) Spirokromanonderivater som acetyl-koenzym-A-karboksylase(ACC)inhibitorer
RU2018121834A (ru) Новое соединение бифенила или его соль
TW200734322A (en) Indole derivatives exhibiting PGD2 receptor antagonism
TW200745029A (en) Sulfonamide derivatives exhibiting PGD2 receptor antagonism
AR055057A1 (es) Inhibidores heterociclicos de mek, formas cristalinas de los mismos, procesos para su preparacion y metodos de uso de los mismos en composiciones farmaceuticas y medicamentos para el tratamiento de un trastorno hiperproliferativo o de una condicion inflamatoria.
MX2009003874A (es) Derivados de espiro-oxindol triciclicos y sus usos como agentes terapeuticos.
AR053415A1 (es) Inhibidores dipeptidil peptidasa iv, composiciones farmaceuticas que los contienen y procesos para la preparacion de los compuestos y de la composicion
DK1856045T3 (da) 1-eddikesyreindolderviater med PGD2-antagonisteffekt
AR036103A1 (es) Imidazotriazinas, procedimiento para su preparacion, uso de dichos compuestos para la manufactura de un medicamento para enfermedades neurodegenerativas y dicho medicamento
AR063101A1 (es) Derivados de pirazina-2-carboxiamida, un proceso para su obtencion, composiciones farmaceuticas que los contienen y su uso en la preparacion de medicamentos para el tratamiento o profilaxis de enfermedades asociadas con la modulacion de receptores del cb2.
AR076460A1 (es) Antagonistas del receptor cxcr3
ECSP077402A (es) Derivados de 2-amido-4-feniltiazol, su preparación y su aplicación en terapéutica
TW200800938A (en) Indole carboxylic acid derivatives exhibiting PGD2 receptor antagonism
ECSP088457A (es) Compuestos de benzamida útiles como inhibidores de la histona deacetilasa
MX2009010731A (es) Derivados de acido 1-(1-bencilpiperidin-4-il)benzimidazol-5-carbox ilico para el tratamiento de diabetes mellitus.
AR057072A1 (es) Compuestos quimicos derivados de 2-azetidinona, formulacion farmaceutica y un proceso de preparacion del compuesto
AR049438A1 (es) Derivados con estructura aroil-o-piperidina, procedimientos para su preparacion, composiciones farmaceuticas que los comprenden y sus aplicaciones terapeuticas
BR112022017382A2 (pt) Composto, composição farmacêutica, uso do composto, e, métodos para tratar ou prevenir uma doença relacionada a ep4 e para tratar uma doença selecionada a partir de uma doença inflamatória, uma dor, um câncer, uma doença metabólica e uma doença do sistema urinário
AR042155A1 (es) Aminoalcoxiindoles, composicion farmaceutica que los comprenden y usos

Legal Events

Date Code Title Description
FA Abandonment or withdrawal