PE20030868A1 - Derivados de nicotinamida utiles como inhibidores de pde4 - Google Patents

Derivados de nicotinamida utiles como inhibidores de pde4

Info

Publication number
PE20030868A1
PE20030868A1 PE2003000151A PE2003000151A PE20030868A1 PE 20030868 A1 PE20030868 A1 PE 20030868A1 PE 2003000151 A PE2003000151 A PE 2003000151A PE 2003000151 A PE2003000151 A PE 2003000151A PE 20030868 A1 PE20030868 A1 PE 20030868A1
Authority
PE
Peru
Prior art keywords
alkyl
phenyl
nicotinamide
fluoro
cyclohexyl
Prior art date
Application number
PE2003000151A
Other languages
English (en)
Inventor
Elisabeth Colette Louise Gautier
John Paul Mathias
Thomas Victor Magee
Alan John Henderson
Blanda Luzia Christa Stammen
Sandra Marina Monaghan
Dale Gordon Mcleod
Simon Bailey
Anthony Marfat
Original Assignee
Pfizer
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
Priority claimed from GB0203196A external-priority patent/GB0203196D0/en
Priority claimed from GB0220999A external-priority patent/GB0220999D0/en
Priority claimed from GB0224453A external-priority patent/GB0224453D0/en
Priority claimed from GB0227139A external-priority patent/GB0227139D0/en
Application filed by Pfizer filed Critical Pfizer
Publication of PE20030868A1 publication Critical patent/PE20030868A1/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen 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
    • C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/81—Amides; Imides
    • C07D213/82—Amides; Imides in position 3
    • 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
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4433—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with oxygen as a ring hetero atom
    • 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
    • A61K31/455—Nicotinic acids, e.g. niacin; Derivatives thereof, e.g. esters, amides
    • 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
    • A61K31/46—8-Azabicyclo [3.2.1] octane; Derivatives thereof, e.g. atropine, cocaine
    • 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
    • A61K31/537—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 spiro-condensed or forming part of bridged ring systems
    • 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
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • 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
    • A61P1/18—Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
    • 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
    • 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
    • A61P13/12—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
    • A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • 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
    • 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
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • 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
    • A61P25/14—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
    • A61P25/24—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
    • 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
    • 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
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A61P31/16—Antivirals for RNA viruses for influenza or rhinoviruses
    • 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
    • A61P31/12—Antivirals
    • A61P31/20—Antivirals for DNA viruses
    • A61P31/22—Antivirals for DNA viruses for herpes viruses
    • 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
    • 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
    • A61P7/06—Antianaemics
    • 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
    • C07D401/12—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
    • C07D451/00—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof
    • C07D451/02—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof
    • C07D451/04—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof with hetero atoms directly attached in position 3 of the 8-azabicyclo [3.2.1] octane or in position 7 of the 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring system
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D451/00—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof
    • C07D451/02—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof
    • C07D451/04—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof with hetero atoms directly attached in position 3 of the 8-azabicyclo [3.2.1] octane or in position 7 of the 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring system
    • C07D451/06—Oxygen atoms
    • C07D451/10—Oxygen atoms acylated by aliphatic or araliphatic carboxylic acids, e.g. atropine, scopolamine
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
    • Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
    • Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change

Landscapes

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

Abstract

SE REFIERE A DERIVADOS DE NICOTINAMIDA DE FORMULA I DONDE R1 Y R2 SON H, HALO, CIANO, ALQUILO, ALCOXI; X ES O, S, NH; R3 ES FENILO, NAFTILO GRUPO BICICLICO 1.1, 1.2, ENTRE OTROS; Y ES UN GRUPO 1.5, 1.6, ENTRE OTROS; R5 ES ALQUILO-FENILO, ALQUILO; Z ES CO, CONH, SO2, SO2NH, CONHSO2, ENTRE OTROS; Y-Z SON JUNTOS UN GRUPO 1.16; R4 ES FENILO, NAFTILO, HETEOARILO, ALQUILO CON LA CONDICION QUE SI R1 ES H, HALO, METILO; R2 ES H; X ES O; R3 ES FENILO; Y ES UN GRUPO 1.5, 1.8, R5 ES ALQUIL-FENILO, Z ES CO; R4 NO ES CICLOALQUILO, FENILO, ALQUILO; ENTRE OTRAS CONDICIONES. SON COMPUESTOS PREFERIDOS ANTI-2-(BENZO[1,3]DIOXOL-5-ILOXI)-N-[4-(2-HIDROXI-BENZOIL-AMINA)CICLOHEXIL]-NICOTINAMIDA; ANTI-N-[4-(2-FLUORO-6-HIDROXI-BENZOILAMINA)CICLOHEXIL]-2-(4-FLUORO-FENOXI)-NICOTINAMIDA; ANTI-5-FLUORO-2-(3,4-DIFLUORO-FENOXI)-N-[4-(2-FLUORO-6-HIDROXI-BENZOILAMINO)CICLOHEXIL]-NICOTINAMIDA; ENTRE OTROS. TAMBIEN SE REFIERE A UN PROCEDIMIENTO PARA LA PREPARACION; LOS COMPUESTOS PUEDEN SER UTILES PARA EL TRATAMIENTO DE ENFERMEDADES, ASMA, BRONCOCONSTRICCION, ENFERMEDADES OBSTRUCTIVAS DE LAS VIAS RESPIRATORIAS, HERIDAS, NEUMOCONIOSIS, BRONQUITIS, BRONQUIECTASIA, ARTRITIS REUMATOIDEA, GOTA, DERMATITIS, URTICARIA, CONJUNTIVITIS
PE2003000151A 2002-02-11 2003-02-11 Derivados de nicotinamida utiles como inhibidores de pde4 PE20030868A1 (es)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
GB0203196A GB0203196D0 (en) 2002-02-11 2002-02-11 Nicotinamide derivatives useful as pde4 inhibitors
GB0220999A GB0220999D0 (en) 2002-09-10 2002-09-10 Nicotinamide derivatives useful as pde4 inhibitors
GB0224453A GB0224453D0 (en) 2002-10-21 2002-10-21 Nicotinamide derivatives useful as PDE4 inhibitors
GB0227139A GB0227139D0 (en) 2002-11-20 2002-11-20 Nicotinamide derivatives useful as pde4 inhibitors

Publications (1)

Publication Number Publication Date
PE20030868A1 true PE20030868A1 (es) 2003-10-21

Family

ID=27739229

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2003000151A PE20030868A1 (es) 2002-02-11 2003-02-11 Derivados de nicotinamida utiles como inhibidores de pde4

Country Status (33)

Country Link
US (3) US6949573B2 (es)
EP (1) EP1476158B1 (es)
JP (1) JP4583761B2 (es)
KR (1) KR100698982B1 (es)
CN (1) CN1652782A (es)
AP (1) AP2004003100A0 (es)
AR (1) AR038834A1 (es)
AT (1) ATE378049T1 (es)
AU (1) AU2003245711A1 (es)
BR (1) BR0307564A (es)
CA (1) CA2475712C (es)
DE (1) DE60317466T2 (es)
EA (1) EA008939B1 (es)
EC (1) ECSP045228A (es)
ES (1) ES2292988T3 (es)
GE (1) GEP20074055B (es)
HN (1) HN2003000064A (es)
HR (1) HRP20040708A2 (es)
MA (1) MA27174A1 (es)
MX (1) MXPA04007737A (es)
MY (1) MY135856A (es)
NI (1) NI200300025A (es)
NO (1) NO20043793L (es)
NZ (1) NZ534197A (es)
OA (1) OA12768A (es)
PA (1) PA8566401A1 (es)
PE (1) PE20030868A1 (es)
PL (1) PL372756A1 (es)
RS (1) RS70104A (es)
TN (1) TNSN04151A1 (es)
TW (1) TW200305419A (es)
UY (1) UY27659A1 (es)
WO (1) WO2003068235A1 (es)

Families Citing this family (43)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7102009B2 (en) 2001-01-12 2006-09-05 Amgen Inc. Substituted amine derivatives and methods of use
US6995162B2 (en) 2001-01-12 2006-02-07 Amgen Inc. Substituted alkylamine derivatives and methods of use
US6878714B2 (en) 2001-01-12 2005-04-12 Amgen Inc. Substituted alkylamine derivatives and methods of use
US7105682B2 (en) 2001-01-12 2006-09-12 Amgen Inc. Substituted amine derivatives and methods of use
NZ534197A (en) * 2002-02-11 2007-01-26 Pfizer Nicotinamide derivatives useful as PDE4 inhibitors
US7307088B2 (en) 2002-07-09 2007-12-11 Amgen Inc. Substituted anthranilic amide derivatives and methods of use
US20050186276A1 (en) * 2003-07-17 2005-08-25 Pfizer Inc Pharmaceutical formulations
GB0317509D0 (en) * 2003-07-25 2003-08-27 Pfizer Ltd Nicotinamide derivatives useful as PDE4 inhibitors
GB0317471D0 (en) * 2003-07-25 2003-08-27 Pfizer Ltd Novel compounds
GB0317482D0 (en) * 2003-07-25 2003-08-27 Pfizer Ltd Nicotinamide derivatives useful as pde4 inhibitors
GB0317516D0 (en) * 2003-07-25 2003-08-27 Pfizer Ltd Nicotinamide derivatives useful as PDE4 inhibitors
US7153870B2 (en) 2003-07-25 2006-12-26 Pfizer Inc. Nicotinamide derivatives useful as PDE4 inhibitors
GB0317484D0 (en) * 2003-07-25 2003-08-27 Pfizer Ltd Nicotinamide derivatives useful as pde4 inhibitors
US7132435B2 (en) 2003-07-25 2006-11-07 Pfizer Inc. Compounds
GB0317472D0 (en) * 2003-07-25 2003-08-27 Pfizer Ltd Nicotinamide derivatives useful as PDE4 inhibitors
US7378409B2 (en) 2003-08-21 2008-05-27 Bristol-Myers Squibb Company Substituted cycloalkylamine derivatives as modulators of chemokine receptor activity
US20050142104A1 (en) * 2003-11-06 2005-06-30 Zeldis Jerome B. Methods of using and compositions comprising PDE4 modulators for the treatment and management of asbestos-related diseases and disorders
PE20060272A1 (es) * 2004-05-24 2006-05-22 Glaxo Group Ltd (2r,3r,4s,5r,2'r,3'r,4's,5's)-2,2'-{trans-1,4-ciclohexanodiilbis-[imino(2-{[2-(1-metil-1h-imidazol-4-il)etil]amino}-9h-purin-6,9-diil)]}bis[5-(2-etil-2h-tetrazol-5-il)tetrahidro-3,4-furanodiol] como agonista a2a
TWI339578B (en) 2004-10-29 2011-04-01 Mitsubishi Tanabe Pharma Corp Use of a pyridine compound for the preparation of a medicament for the treatment of skin lesions
JP4874958B2 (ja) * 2005-03-30 2012-02-15 エーザイ・アール・アンド・ディー・マネジメント株式会社 ピリジン誘導体を含有する抗真菌剤
GB0514809D0 (en) 2005-07-19 2005-08-24 Glaxo Group Ltd Compounds
US7678363B2 (en) 2005-08-26 2010-03-16 Braincells Inc Methods of treating psychiatric conditions comprising administration of muscarinic agents in combination with SSRIs
EP2258359A3 (en) 2005-08-26 2011-04-06 Braincells, Inc. Neurogenesis by muscarinic receptor modulation with sabcomelin
SI1928409T1 (sl) 2005-09-12 2012-12-31 Actelion Pharmaceuticals Ltd. Stabilni farmacevtski sestavek, ki obsega pirimidin-sulfamid
US8247556B2 (en) 2005-10-21 2012-08-21 Amgen Inc. Method for preparing 6-substituted-7-aza-indoles
EP1940389A2 (en) 2005-10-21 2008-07-09 Braincells, Inc. Modulation of neurogenesis by pde inhibition
US20070112017A1 (en) 2005-10-31 2007-05-17 Braincells, Inc. Gaba receptor mediated modulation of neurogenesis
TWI385169B (zh) 2005-10-31 2013-02-11 Eisai R&D Man Co Ltd 經雜環取代之吡啶衍生物及含有彼之抗真菌劑
CN101355876B (zh) 2005-11-09 2012-09-05 康宾纳特克斯公司 一种适用于眼部给药的组合物
US20100216734A1 (en) 2006-03-08 2010-08-26 Braincells, Inc. Modulation of neurogenesis by nootropic agents
EP2021000A2 (en) 2006-05-09 2009-02-11 Braincells, Inc. Neurogenesis by modulating angiotensin
MX2008014320A (es) 2006-05-09 2009-03-25 Braincells Inc Neurogenesis mediada por el receptor de 5-hidroxitriptamina.
EP2068872A1 (en) 2006-09-08 2009-06-17 Braincells, Inc. Combinations containing a 4-acylaminopyridine derivative
US20100184806A1 (en) 2006-09-19 2010-07-22 Braincells, Inc. Modulation of neurogenesis by ppar agents
US8513287B2 (en) 2007-12-27 2013-08-20 Eisai R&D Management Co., Ltd. Heterocyclic ring and phosphonoxymethyl group substituted pyridine derivatives and antifungal agent containing same
WO2009144494A1 (en) * 2008-05-27 2009-12-03 Astrazeneca Ab Phenoxypyridinylamide derivatives and their use in the treatment of pde4 mediated disease states
US20100216805A1 (en) 2009-02-25 2010-08-26 Braincells, Inc. Modulation of neurogenesis using d-cycloserine combinations
US8697691B2 (en) * 2009-12-21 2014-04-15 Vanderbilt University Alkyl 3-((2-amidoethyl)amino)-8-azabicyclo[3.2.1]octane-8-carboxylate analogs as selective M1 agonists and methods of making and using same
EP2804603A1 (en) 2012-01-10 2014-11-26 President and Fellows of Harvard College Beta-cell replication promoting compounds and methods of their use
WO2015020013A1 (ja) * 2013-08-08 2015-02-12 日本電気株式会社 二次電池用負極、その製造方法、およびそれを用いた二次電池
CA3105657A1 (en) * 2018-07-09 2020-01-16 Lieber Institute, Inc. Pyridine carboxamide compounds for inhibiting nav1.8
CN109674808A (zh) * 2019-01-30 2019-04-26 四川大学 β-烟酰胺单核苷酸或其前体在制备延缓肺衰老药物中的用途
CN114656372A (zh) * 2020-09-14 2022-06-24 广州药本君安医药科技股份有限公司 对苯二胺桥连化合物及其在制备治疗糖代谢紊乱疾病的药物中的应用

Family Cites Families (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5376645A (en) 1990-01-23 1994-12-27 University Of Kansas Derivatives of cyclodextrins exhibiting enhanced aqueous solubility and the use thereof
KR0166088B1 (ko) 1990-01-23 1999-01-15 . 수용해도가 증가된 시클로덱스트린 유도체 및 이의 용도
NZ337698A (en) * 1997-04-04 2001-07-27 Pfizer Prod Inc Nicotinamide derivatives for selective inhibition of phosphodiesterase type 4 (PDE4) and the production of tumour necrosis factor (TNF) useful for the treatment of respiratory, rheumatoid and allergic diseases
GB9711643D0 (en) 1997-06-05 1997-07-30 Janssen Pharmaceutica Nv Glass thermoplastic systems
GB9924092D0 (en) * 1999-10-13 1999-12-15 Zeneca Ltd Pyrimidine derivatives
AU2700201A (en) 2000-01-31 2001-08-14 Pfizer Products Inc. Nicotinamide benzofused-heterocyclyl derivatives useful as selective inhibitors of pde4 isozymes
WO2003068233A1 (en) 2002-02-11 2003-08-21 Pfizer Limited Nicotinamide derivatives and a tiotropium salt in combination for the treatment of e.g. inflammatory, allergic and respiratory diseases
NZ534197A (en) * 2002-02-11 2007-01-26 Pfizer Nicotinamide derivatives useful as PDE4 inhibitors
GB0203193D0 (en) 2002-02-11 2002-03-27 Pfizer Ltd Nicotinamide derivatives useful as pde4 inhibitors
GB0317516D0 (en) * 2003-07-25 2003-08-27 Pfizer Ltd Nicotinamide derivatives useful as PDE4 inhibitors

Also Published As

Publication number Publication date
TNSN04151A1 (fr) 2007-03-12
GEP20074055B (en) 2007-03-12
OA12768A (en) 2006-07-04
NZ534197A (en) 2007-01-26
NI200300025A (es) 2005-09-21
HRP20040708A2 (en) 2005-06-30
DE60317466D1 (de) 2007-12-27
RS70104A (en) 2007-02-05
KR100698982B1 (ko) 2007-03-26
MA27174A1 (fr) 2005-01-03
ECSP045228A (es) 2004-09-28
EA200400892A1 (ru) 2005-02-24
BR0307564A (pt) 2004-12-21
HN2003000064A (es) 2003-11-24
US6949573B2 (en) 2005-09-27
JP4583761B2 (ja) 2010-11-17
AU2003245711A1 (en) 2003-09-04
UY27659A1 (es) 2003-09-30
PL372756A1 (en) 2005-08-08
CA2475712A1 (en) 2003-08-21
ES2292988T3 (es) 2008-03-16
US7060717B2 (en) 2006-06-13
EA008939B1 (ru) 2007-10-26
CA2475712C (en) 2009-11-24
CN1652782A (zh) 2005-08-10
PA8566401A1 (es) 2003-11-12
WO2003068235A1 (en) 2003-08-21
TW200305419A (en) 2003-11-01
DE60317466T2 (de) 2008-03-06
ATE378049T1 (de) 2007-11-15
AR038834A1 (es) 2005-01-26
MXPA04007737A (es) 2004-10-15
EP1476158A1 (en) 2004-11-17
MY135856A (en) 2008-07-31
NO20043793L (no) 2004-10-21
US20060014780A1 (en) 2006-01-19
JP2005522450A (ja) 2005-07-28
KR20040079994A (ko) 2004-09-16
US20030220366A1 (en) 2003-11-27
EP1476158B1 (en) 2007-11-14
US20040224975A1 (en) 2004-11-11
AP2004003100A0 (en) 2004-09-30

Similar Documents

Publication Publication Date Title
PE20030868A1 (es) Derivados de nicotinamida utiles como inhibidores de pde4
PE20030860A1 (es) Derivados de nicotamida utiles como inhibidores de pde4
HRP990167B1 (en) Sulphinic acid derivatives, method for producing them, and their use
DE60127863D1 (de) Phenylderivate
CY1113648T1 (el) Παραγωγα πυριδινονης για θεραπεια αθηροσκληρωσης
GB9801690D0 (en) Therapeutic agents
CR7807A (es) Piperacinil y diacepanil benzamidas y benztioamidas
PE20031037A1 (es) Derivados de nicotinamida y una sal de tiotropio en combinacion para el tratamiento de enfermedades
ME01310B (me) Derivati oksazola koji su supstituisani karboksilnom kiselinom za primenu kao ppar-alfa-1-gama aktivatori u lečenju dijabetesa
RS20050311A (en) Selected cgrp antagonists,method for production and use thereof as medicament
DE60040676D1 (de) BENZAMIDE UND ÄHNLICHE INHIBITOREN VON FAKTOR Xa
EA200200739A1 (ru) Пиримидинкарбоксамиды, используемые в качестве ингибиторов изосимов pde4
DK1864975T3 (da) Nikotinamid-derivater anvendelige som P38-inhibitorer
RS20050329A (en) Selected cgrp antagonists,method for production and use thereof as medicament
PE20030061A1 (es) 1-biaril-1,8-naftiridin-4-ona como inhibidores de fosfodiesterasa-4
ES510015A0 (es) Procedimiento para preparar 3-amino-sidnoniminas sustituidas.
BRPI0412910A (pt) derivados de nicotinamida úteis como inibidores de pde4
AU2001285958A1 (en) Method for obtaining 4-(n-alkylamine)-5, 6-dihydro-4h-thieno-(2,3-b)-thiopyran-2-sulfamide-7, 7-dioxides and intermediate products
EA199901096A1 (ru) Цианогуанидины в качестве ингибиторов пролиферации клеток
BR0201569A (pt) 4-(2-piridil) piperizinas possuindo uma atividade agonista do receptor 5ht7
DE69119509D1 (de) Benzhydryloxyethylpiperidyl-Derivate aliphatischer Carbonsäuren und ihre Anwendung zur Behandlung von Allergien und Asthma
DK1441726T3 (da) Derivater af phenoxy-N&#39; -4-(isothiazolidin-1,1-dioxid-2-yl)phenyl]-valerianesyreamid og andre forbindelser som inhibitorer af koagulationsfaktoren Xa til behandling af thromboemboliske lidelser og tumorer
BR0116721A (pt) Processo para a preparação de (±)-trans-4-p-fluorofenil-3-hidroximetil-1-metilpiperi dina
PT1430034E (pt) Derivados de alquilaminopiridazinona substituida processo para sua preparacao e composicoes farmaceuticas que os contem
UY26568A1 (es) Nuevos derivados de amidas heterocíclicas

Legal Events

Date Code Title Description
FG Grant, registration
FD Application declared void or lapsed