ES2571335T3 - Derivados de benzazol como ligandos del receptor de la histamina H4 - Google Patents

Derivados de benzazol como ligandos del receptor de la histamina H4

Info

Publication number
ES2571335T3
ES2571335T3 ES11761383T ES11761383T ES2571335T3 ES 2571335 T3 ES2571335 T3 ES 2571335T3 ES 11761383 T ES11761383 T ES 11761383T ES 11761383 T ES11761383 T ES 11761383T ES 2571335 T3 ES2571335 T3 ES 2571335T3
Authority
ES
Spain
Prior art keywords
alkyl
substituted
halo
amino
optionally substituted
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.)
Active
Application number
ES11761383T
Other languages
English (en)
Inventor
Isabelle Berrebi-Bertrand
Xavier Billot
Thierry Calmels
Marc Capet
Denis Danvy
Stéphane Krief
Olivier Labeeuw
Jeanne-Marie Lecomte
Nicolas Levoin
Xavier Ligneau
Philippe Robert
Jean-Charles Schwartz
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.)
Bioprojet SC
Original Assignee
Bioprojet SC
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 Bioprojet SC filed Critical Bioprojet SC
Application granted granted Critical
Publication of ES2571335T3 publication Critical patent/ES2571335T3/es
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • 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
    • C07D417/14—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 three or more hetero rings
    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/425—Thiazoles
    • A61K31/428—Thiazoles condensed with carbocyclic rings
    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/454—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4545—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
    • 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
    • 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
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • 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
    • A61K31/535—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 oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • A61P11/02—Nasal agents, e.g. decongestants
    • 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
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/08—Bronchodilators
    • 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
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/08—Drugs for disorders of the urinary system of the prostate
    • 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
    • A61P13/10—Drugs for disorders of the urinary system of the bladder
    • 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
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/08—Drugs for genital or sexual disorders; Contraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/10—Drugs for genital or sexual disorders; Contraceptives for impotence
    • 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
    • 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
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • 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
    • 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
    • A61P25/28—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]
    • 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
    • A61P37/08—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
    • 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
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/12—Antidiuretics, e.g. drugs for diabetes insipidus
    • 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
    • A61P9/02—Non-specific cardiovascular stimulants, e.g. drugs for syncope, antihypotensives
    • 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
    • A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • 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
    • A61P9/06—Antiarrhythmics
    • 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
    • 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
    • A61P9/12—Antihypertensives
    • 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
    • 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
    • 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
    • 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
    • C07D405/14—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 three or more hetero rings
    • 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
    • C07D417/04—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 directly linked by a ring-member-to-ring-member bond
    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Epidemiology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pulmonology (AREA)
  • Urology & Nephrology (AREA)
  • Dermatology (AREA)
  • Reproductive Health (AREA)
  • Diabetes (AREA)
  • Immunology (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Rheumatology (AREA)
  • Pain & Pain Management (AREA)
  • Gynecology & Obstetrics (AREA)
  • Endocrinology (AREA)
  • Hematology (AREA)
  • Hospice & Palliative Care (AREA)
  • Otolaryngology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Vascular Medicine (AREA)
  • Pregnancy & Childbirth (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Psychiatry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

Compuesto de fórmula (I):**Fórmula** en la que: X representa NR', S u O; HetAr representa un fenilo o heteroarilo, opcionalmente sustituido con uno o más sustituyentes seleccionados de halógeno, OR'', alquilo, ciano, NR''R'", -COR'', -COOR'', -CONR''R'", arilo, alquilarilo; R representa un alquilo inferior o H R' representa H, alquilo inferior, alcoxialquilo o alcoxicarbonilo; R", R''' idénticos o diferentes representan independientemente H o alquilo; HET representa un heterociclo monocíclico no aromático que contiene al menos un átomo de nitrógeno, que está unido a R; B representa un enlace sencillo o un grupo -CH2-; A representa O, NH o S; Ar es un aromático monocíclico o policíclico o un heteroaromático monocíclico o policíclico que puede estar opcionalmente sustituido con uno o más de: · halo; azido; ciano; hidroxi; nitro; · alquilo; alcoxi; alquilsulfanilo; alquenilo; alquinilo; alqueniloxi; alqueniloxi; alquenilsulfanilo; alquinilsulfanilo; cicloalcoxi; cicloalquilalquilo; cuya parte alquilo, alquenilo, alquinilo o cicloalquilo puede estar sustituido con uno o más de halo, hidroxi, polihidroxi, alcoxi, hidroxialcoxi, ciano, amino, aminoalquilo, alquilamino, dialquilamino, aminoalquilamino, aminoalquilaminocarbonilo, alcoxicarbonilamino, diarilmetilimino (donde arilo está opcionalmente sustituido con uno o más de hidroxi o halo), cicloalquenilimino (donde cicloalquenilo está opcionalmente sustituido con uno o más de alquilo, OH), alquilsulfanilo, alquilsulfinilo, alquilsulfonilo, cicloalquilo, policicloalquilo, cicloalquenilo, policicloalquenilo, guanidino, alquilcarbonilguanidino, acilguanidino, cianoguanidino, alcoxicarbonilguanidino, alcoxicarbonilo, alcoxicarbonilalquilamino, alcoxicarbonilalquilcicloalquilo, alcoxicarbonilheterociclilo, aminocarbonilo, alquilaminocarbonilo, alquilcarbonilo, alquilcarbonilalcoxi, ariloxi, arilsulfanilo, arilsulfinilo, arilsulfonilo, heteroarilo, heterociclilo (siendo heterociclilo opcionalmente sustituido con uno o más de oxo, amino, imino), heteroariloxi, heterocicliloxi, heteroarilamino, heterociclilamino, hidrazinocarbonilo, hidroxialquilcicloalquilo, N-alquil(tioureido), ftalimido, ureido, oxocicloalquenilamino sustituido con amino, carbamimidoilheterociclilo; · amino; alquilamino; alquilcarbonilo; alcoxicarbonilo; alquilsulfanilo; alquilsulfinilo; alquilsulfonilo; alquilsulfoniloxi cuyo alquilo puede estar sustituido con uno o más de halo; · aminocarbonilo que puede estar N-sustituido con uno o dos de alquilo, arilo, arilalquilo; · arilo; arilalquilo; ariloxi; arilalcoxi; arilalquilamino; arilalquilsulfanilo; heteroarilo; heteroariloxi cuya parte arilo puede estar sustituida con uno o más de amino, halo, alquilo, (poli)haloalquilo, hidroxialquilo, alcoxi, (poli)haloalcoxi, alcoxicarbonilamino, alquilcarbonilo, alquilsulfanilo, alquilsulfinilo, alquilsulfonilo, nitro, cianoalquilo, o fusionado con un heterociclo no aromático; · heterociclilo; heterocicliloxi; heterociclilalcoxi cuyo heterociclo puede estar sustituido con uno o más de halogenoalquilo, acilamino, aciloxi, amino, alquilo, alquilamino, dialquilamino, aminoalquilo, oxo, carbamimidoilo, halo, hidroxi, hidroxialquilo, hidroximetilo, alcoxicarbonilo; o · fusionado con un heterociclo no aromático (opcionalmente sustituido con uno o más de halógenos) o carbociclo; en la que "alquilo inferior" tiene de 1 a 4 átomos de carbono; así como sus enantiómeros, diastereoisómeros, mezclas de los mismos y sales farmacéuticamente aceptables, tautómeros, hidratos y solvatos.
ES11761383T 2010-09-27 2011-09-27 Derivados de benzazol como ligandos del receptor de la histamina H4 Active ES2571335T3 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP20100306038 EP2447263A1 (en) 2010-09-27 2010-09-27 Benzazole derivatives as histamine H4 receptor ligands
PCT/EP2011/066782 WO2012041860A1 (en) 2010-09-27 2011-09-27 Benzazole derivatives as histamine h4 receptor ligands

Publications (1)

Publication Number Publication Date
ES2571335T3 true ES2571335T3 (es) 2016-05-24

Family

ID=43513798

Family Applications (1)

Application Number Title Priority Date Filing Date
ES11761383T Active ES2571335T3 (es) 2010-09-27 2011-09-27 Derivados de benzazol como ligandos del receptor de la histamina H4

Country Status (16)

Country Link
US (2) US8802664B2 (es)
EP (2) EP2447263A1 (es)
JP (1) JP5922128B2 (es)
CN (1) CN103228643B (es)
CA (1) CA2812686C (es)
CY (1) CY1117416T1 (es)
DK (1) DK2621916T3 (es)
ES (1) ES2571335T3 (es)
HR (1) HRP20160398T1 (es)
HU (1) HUE027252T2 (es)
MX (1) MX339460B (es)
PL (1) PL2621916T3 (es)
RS (1) RS54737B1 (es)
SI (1) SI2621916T1 (es)
SM (1) SMT201600262B (es)
WO (1) WO2012041860A1 (es)

Families Citing this family (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN103648639B (zh) 2011-04-19 2016-10-12 沙特基础工业公司 碳负载的钴和钼催化剂
EA027113B1 (ru) * 2012-05-04 2017-06-30 Новартис Аг Регуляторы пути комплемента и их применение
EP2671870A1 (en) * 2012-06-05 2013-12-11 Bioprojet Novel (aza)benzhydryl ether derivatives, their process of preparation and their use as H4-receptor ligands for therapeutical applications
HUE039713T2 (hu) 2012-06-08 2019-02-28 Sensorion H4 receptor inhibitorok tinnitus kezelésére
CN106800524A (zh) * 2015-02-13 2017-06-06 佛山市赛维斯医药科技有限公司 一类含双酰肼和萘基结构的化合物、制备方法及其用途
JP7447002B2 (ja) * 2017-09-11 2024-03-11 クルーゾン・ファーマシューティカルズ・インコーポレイテッド ＳＨＰ２のオクタヒドロシクロペンタ［ｃ］ピロールのアロステリック阻害剤
CA3024429A1 (en) * 2017-11-15 2019-05-15 Bioprojet New benzimidazole derivatives as dual histamine h1 and histamine h4 receptor ligands
CN113278409B (zh) * 2021-06-22 2022-04-29 西南石油大学 一种高温酸化缓蚀剂
CN119086786B (zh) * 2024-11-08 2025-02-14 南京恒远科技开发有限公司 叔丁基-(s)-[2-(2-氰基-4,4-二氟吡咯烷-1-基)-2-氧乙基]氨基甲酸酯光学异构体的检测方法

Family Cites Families (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FI803127A7 (fi) * 1979-10-03 1981-04-04 Glaxo Group Ltd Heterosyklisiä yhdisteitä.
IT1154888B (it) * 1980-11-12 1987-01-21 Menarini Sas Derivati del benzofurano 2-sostituiti e relativi metodi di preparazione
US4908372A (en) * 1988-10-13 1990-03-13 Merrell Dow Pharmaceuticals Inc. Antihistaminic piperidinyl benzimidazoles
JPH05339266A (ja) * 1992-06-05 1993-12-21 Kaken Pharmaceut Co Ltd 新規なピペリジン誘導体
US6476041B1 (en) 1999-10-29 2002-11-05 Merck & Co., Inc. 1,4 substituted piperidinyl NMDA/NR2B antagonists
PL369856A1 (en) 2001-12-21 2005-05-02 Anormed Inc. Chemokine receptor binding heterocyclic compounds with enhanced efficacy
RU2006110561A (ru) * 2003-09-30 2007-10-10 Янссен Фармацевтика Н.В. (Be) Соединения бензоимидазола
EP1687452A4 (en) * 2003-09-30 2008-08-06 Centocor Inc HUMAN HINGE-CORE MIMETICORPS, COMPOSITIONS, METHODS AND APPLICATIONS THEREOF
EP1642577A1 (en) * 2004-09-07 2006-04-05 Laboratorios del Dr. Esteve S.A. Derivatives of aryl (or heteroaryl) azolylcarbinols for the treatment of central neuropathic pain
US7557103B2 (en) 2005-04-05 2009-07-07 Eli Lilly And Company Imidazopyridazine compounds
US8163901B2 (en) 2008-01-09 2012-04-24 Evotec Ag Amide derivatives as ion-channel ligands and pharmaceutical compositions and methods of using the same

Also Published As

Publication number Publication date
CA2812686A1 (en) 2012-04-05
US8802664B2 (en) 2014-08-12
HRP20160398T1 (hr) 2016-05-20
CN103228643A (zh) 2013-07-31
EP2621916A1 (en) 2013-08-07
SMT201600262B (it) 2016-08-31
EP2621916B1 (en) 2016-02-10
SI2621916T1 (sl) 2016-06-30
MX2013003479A (es) 2013-06-24
JP5922128B2 (ja) 2016-05-24
CY1117416T1 (el) 2017-04-26
CN103228643B (zh) 2015-11-25
WO2012041860A1 (en) 2012-04-05
PL2621916T3 (pl) 2016-08-31
RS54737B1 (sr) 2016-10-31
JP2013537898A (ja) 2013-10-07
HUE027252T2 (en) 2016-10-28
US20130231329A1 (en) 2013-09-05
CA2812686C (en) 2019-04-02
MX339460B (es) 2016-05-27
EP2447263A1 (en) 2012-05-02
US9029357B2 (en) 2015-05-12
US20150004181A1 (en) 2015-01-01
DK2621916T3 (en) 2016-04-18
HK1183867A1 (en) 2014-01-10

Similar Documents

Publication Publication Date Title
ES2571335T3 (es) Derivados de benzazol como ligandos del receptor de la histamina H4
RU2470017C2 (ru) Производные пиперидина/пиперазина
MY160394A (en) Novel phenol derivative
ES2662444T3 (es) Derivado de piridina
AR083339A1 (es) Compuestos de quinazolina como bloqueadores de los canales de sodio
AR053405A1 (es) Derivados de urea sustituidas, composiciones farmaceuticas y metodos para el tratamiento de cardiopatias
MX2017010735A (es) Inhibidores de inhibidores del factor beta de crecimiento de transformacion (tgf-beta).
AR038703A1 (es) Derivados de 5-feniltiazol y uso como inhibidor de quinasa p i 3
MX2011011875A (es) Compuesto de carboxamida heterociclica diamino.
AR082888A1 (es) Compuestos de piridina para la inhibicion de nampt
MY140039A (en) Pyrido-(2,1-a)-isoquinoline derivatives as dpp-iv inhibitors
PE20131377A1 (es) Triazina-oxadiazoles
AR096620A1 (es) Derivado de aminotriazina y composición farmacéutica que lo comprende
AR099379A1 (es) Compuestos tricíclicos como agentes antineoplásicos
CO6260132A2 (es) Derivados de oxadiazol como inhibidores de dgat
AR085585A1 (es) Vinil- y alquinilciclohexanoles sustituidos como principios activos contra estres abiotico de plantas
AR063653A1 (es) Inhibidores del virus de la hepatitis c
JO3261B1 (ar) مشتق بيريدين أحادي الحلقة
AR092289A1 (es) Derivados de aminoquinazolina y sus sales y metodos de uso
AR083023A1 (es) Compuestos de piridina y una composicion farmaceutica que los comprende
AR066153A1 (es) Derivados de piperidina / piperazina
AR110992A1 (es) Derivados heterocíclicos con sustituyentes que contienen azufre activos como plaguicidas
WO2007122634A3 (en) Pyrimidinediones as tyrosine kinase inhibitors
RU2015121431A (ru) Замещенные производные индол-5-ола и их терапевтическое применение
AR058984A1 (es) Derivados de ciclohexil piperazinil metanona