AR042673A1 - Inhibidores benzamidicos del receptor p2 x 7 - Google Patents

Inhibidores benzamidicos del receptor p2 x 7

Info

Publication number
AR042673A1
AR042673A1 ARP030104854A ARP030104854A AR042673A1 AR 042673 A1 AR042673 A1 AR 042673A1 AR P030104854 A ARP030104854 A AR P030104854A AR P030104854 A ARP030104854 A AR P030104854A AR 042673 A1 AR042673 A1 AR 042673A1
Authority
AR
Argentina
Prior art keywords
alkyl
cycloalkyl
aryl
heterocyclyl
optionally substituted
Prior art date
Application number
ARP030104854A
Other languages
English (en)
Original Assignee
Pfizer Prod Inc
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Pfizer Prod Inc filed Critical Pfizer Prod Inc
Publication of AR042673A1 publication Critical patent/AR042673A1/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D253/00—Heterocyclic compounds containing six-membered rings having three nitrogen atoms as the only ring hetero atoms, not provided for by group C07D251/00
    • C07D253/02—Heterocyclic compounds containing six-membered rings having three nitrogen atoms as the only ring hetero atoms, not provided for by group C07D251/00 not condensed with other rings
    • C07D253/06—1,2,4-Triazines
    • C07D253/065—1,2,4-Triazines having three double bonds between ring members or between ring members and non-ring members
    • C07D253/07—1,2,4-Triazines having three double bonds between ring members or between ring members and non-ring members 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
    • C07D253/075—Two hetero atoms, in positions 3 and 5
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D253/00—Heterocyclic compounds containing six-membered rings having three nitrogen atoms as the only ring hetero atoms, not provided for by group C07D251/00
    • C07D253/02—Heterocyclic compounds containing six-membered rings having three nitrogen atoms as the only ring hetero atoms, not provided for by group C07D251/00 not condensed with other rings
    • C07D253/06—1,2,4-Triazines
    • C07D253/065—1,2,4-Triazines having three double bonds between ring members or between ring members and non-ring members
    • C07D253/07—1,2,4-Triazines having three double bonds between ring members or between ring members and non-ring members 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
    • 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
    • A61K31/53—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
    • 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
    • A61P1/02—Stomatological preparations, e.g. drugs for caries, aphtae, periodontitis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/16—Central respiratory analeptics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • 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
    • A61P17/06—Antipsoriatics
    • 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
    • A61P17/16—Emollients or protectives, e.g. against radiation
    • 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
    • A61P19/06—Antigout agents, e.g. antihyperuricemic or uricosuric agents
    • 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
    • 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
    • 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
    • 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
    • A61P25/14—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
    • 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
    • A61P31/04—Antibacterial agents
    • 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
    • A61P31/18—Antivirals for RNA viruses for HIV
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P33/00—Antiparasitic agents
    • A61P33/02—Antiprotozoals, e.g. for leishmaniasis, trichomoniasis, toxoplasmosis
    • A61P33/06—Antimalarials
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P33/00—Antiparasitic agents
    • A61P33/10—Anthelmintics
    • A61P33/12—Schistosomicides
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/08—Antiallergic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P41/00—Drugs used in surgical methods, e.g. surgery adjuvants for preventing adhesion or for vitreum substitution
    • 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
    • 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
    • A61P9/04—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
    • A61P9/10—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
    • A61P9/14—Vasoprotectives; Antihaemorrhoidals; Drugs for varicose therapy; Capillary stabilisers
    • 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
    • C07D401/06—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 carbon chain containing only aliphatic carbon atoms
    • 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
    • C07D405/06—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 carbon chain containing only aliphatic carbon atoms

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)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Immunology (AREA)
  • Rheumatology (AREA)
  • Pain & Pain Management (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Pulmonology (AREA)
  • Cardiology (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Dermatology (AREA)
  • Diabetes (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Hematology (AREA)
  • Psychiatry (AREA)
  • Vascular Medicine (AREA)
  • Virology (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Psychology (AREA)
  • Urology & Nephrology (AREA)
  • Hospice & Palliative Care (AREA)
  • Molecular Biology (AREA)
  • Transplantation (AREA)

Abstract

Los compuestos de la presente son útiles en el tratamiento de trastornos mediados por IL-1, incluidos, sin limitación, enfermedades inflamatorias tales como osteoartritis y artritis reumatoide; alergias, asma, COPD (enfermedad pulmonar obstructiva crónica), cáncer, reperfusión o isquemia en accidente cerebrovascular o ataque cardíaco, enfermedades autoinmunes y otros trastornos. Reivindicación 1: Un compuesto de fórmula (1), caracterizado porque R1 es alquilo (C1-6), opcionalmente sustituido con cicloalquilo (C3-10), arilo (C6-10), heterociclilo (C1-10) o heteroarilo (C1-10), en donde cada uno de dichos alquilo (C1-6), cicloalquilo (C3-10), arilo (C6-10), heterociclilo (C1-10) o heteroarilo (C1-10) está opcionalmente sustituido con uno a tres restos adecuados, seleccionados independientemente del grupo formado por hidroxi, halógeno, CN-, alquilo (C1-6), HO-alquilo (C1-6), alquil(C1-6)-NH(C=O)-, NH2(C=O)-, alcoxi (C1-6) o cicloalquilo (C3-10), en donde dicho cicloalquilo (C3-10) está opcionalmente sustituido con uno o más restos seleccionados entre halógeno o alquil (C1-6)-; R2 es hidrógeno, halógeno, -CN y alquilo (C1-6), en donde dicho alquilo (C1-6) está opcionalmente sustituido con uno a tres restos adecuados, seleccionados independientemente del grupo formado por halo, hidroxi, amino, -CN, alquilo (C1-6), alcoxi (C1-6), -CF3, CF3O-alquilo(C1-6)-NH-, [alquil (C1-6)]2-N-, alquil(C1-6)-S-, alquil(C1-6)-(S=O)-, alquil(C1-6)-(SO2)-, alquil(C1-6)-O-(C=O)-, formilo, alquil(C1-6)-(C=O)- y cicloalquilo (C3-6); R3 es un heterociclilo (C1-10) unido por nitrógeno, de fórmula (2), en donde R4 se selecciona del grupo de sustituyentes adecuados, tales como hidrógeno, halo, hidroxi, -CN, HO-alquilo (C1-6), alquilo (C1-6) opcionalmente sustituido con uno a tres flúor, alcoxi (C1-6) opcionalmente sustituido con uno a tres flúor, HO2C-, alquil(C1-6)-O-(C=O)-, R5R6N(O2S)-, alquil(C1-6)-(O2S)-NH-, alquil(C1-6)-O2-S-[(alquil (C1-6)-N]-, R5R6N(C=O)-, R5R6N(CH2)m-, arilo (C6-10), cicloalquilo (C3-8), heteroarilo (C1-10), heterociclilo (C1-10), aril(C6-10)-O-, cicloalquil(C3-8)-O-, heteroaril(C1-10)-O- y heterociclil(C1-10)-O-; y R7 se selecciona del grupo de sustituyentes adecuados tales como hidrógeno y alquilo (C1-6) opcionalmente sustituido con uno o a tres halógenos, hidroxi, -CN, alcoxi (C1-6)-, alquenoxi (C2-6), alquil(C1-6)-SO2-, NH2-, (alquil (C1-6))n-N-, (alquenil C2-6))n-N-, (alquinil (C2-6))n-N-, NH2(C=O)-, alquil(C1-6)-(C=O)-N-, (alquil (C1-6))n-N-(C=)-, alquenil(C2-6)-(C=O)N-, (alquenil (C2-6))n-N-(C=O)-, alquinil(C2-6)-(C=O)-N-, (alquinil (C2-6))n-N-(C=O)-, alquil(C1-6)-(C=O)-, alquenil(C2-6)-(C=O)-, alquinil(C2-6)-(C=O)-, cicloalquil(C3-10)-(C=O)-, heterociclil(C1-10)-(C=O)-, aril(C6-10)-(C=O)-, heteroaril(C1-10)-(C=O)-, alquil(C1-6)-(C=O)O-, alquenil(C2-6)-(C=O)O-, alquinil(C2-6)-(C=O)O-, alquil(C1-6)-O(C=O)-, alquenil(C2-6)-O-(C=O)-, alquinil(C2-6)-O-(C=O)-, cicloalquilo (C3-10), arilo (C6-10), arilo (C6-10), heterociclilo (C1-10) y heteroarilo (C1-10); en donde cada uno de R4 y R7 puede estar opcionalmente sustituido en cualquier átomo de carbono alifático o aromático con uno a tres restos adecuados, seleccionados independientemente del grupo formado por halo, hidroxi, amino, -CN, alquilo (C1-6), alcoxi (C1-6), -CF3, CF3O-alquilo(C1-6)-NH-, [alquil (C1-6)]2-N-, alquil(C1-6)-S-, alquil(C1-6)-(S=O)-, alquil(C1-6)-(SO2)-, alquil(C1-6)-O-(C=O)-, formilo, alquil(C1-6)-(C=O)- y cicloalquilo (C3-6); cada uno de R5 y R6 se selecciona independientemente del grupo formado por hidrógeno, alquilo (C1-6), HO-alquilo (C2-6) y cicloalquilo (C3-8), o R5 y R6 opcionalmente se pueden tomar junto con el átomo de nitrógeno al que están unidos para formar un heterocíclico de 3 a 8 miembros; n es un número entero de cero a dos; y m es un número entero de uno a dos; o sus sales o solvatos o profármacos farmacéuticamente aceptables.
ARP030104854A 2002-12-31 2003-12-29 Inhibidores benzamidicos del receptor p2 x 7 AR042673A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US43750502P 2002-12-31 2002-12-31

Publications (1)

Publication Number Publication Date
AR042673A1 true AR042673A1 (es) 2005-06-29

Family

ID=32682427

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP030104854A AR042673A1 (es) 2002-12-31 2003-12-29 Inhibidores benzamidicos del receptor p2 x 7

Country Status (40)

Country Link
US (4) US6974812B2 (es)
EP (1) EP1581232B1 (es)
JP (1) JP4560411B2 (es)
KR (1) KR100689138B1 (es)
CN (1) CN1732006A (es)
AP (1) AP1997A (es)
AR (1) AR042673A1 (es)
AU (1) AU2003285716B2 (es)
BR (1) BR0317803A (es)
CA (1) CA2512193C (es)
CL (1) CL2003002765A1 (es)
CO (1) CO5580749A2 (es)
CR (1) CR7884A (es)
DO (1) DOP2003000790A (es)
EA (1) EA008591B1 (es)
EC (1) ECSP055884A (es)
ES (1) ES2464350T3 (es)
GE (1) GEP20084304B (es)
GT (1) GT200300297A (es)
HR (1) HRP20050609A2 (es)
IL (2) IL168513A (es)
IS (1) IS7840A (es)
MA (1) MA27575A1 (es)
MX (1) MXPA05006749A (es)
MY (1) MY141984A (es)
NI (1) NI200500118A (es)
NL (1) NL1025148C2 (es)
NO (1) NO20053587L (es)
NZ (1) NZ539913A (es)
OA (1) OA12978A (es)
PA (1) PA8591801A1 (es)
PE (1) PE20040802A1 (es)
PL (1) PL378251A1 (es)
RS (1) RS20050490A (es)
TN (1) TNSN05174A1 (es)
TW (1) TWI288133B (es)
UA (1) UA82346C2 (es)
UY (1) UY28153A1 (es)
WO (1) WO2004058270A1 (es)
ZA (1) ZA200503912B (es)

Families Citing this family (62)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PA8557501A1 (es) 2001-11-12 2003-06-30 Pfizer Prod Inc Benzamida, heteroarilamida y amidas inversas
US7071223B1 (en) * 2002-12-31 2006-07-04 Pfizer, Inc. Benzamide inhibitors of the P2X7 receptor
PA8591801A1 (es) * 2002-12-31 2004-07-26 Pfizer Prod Inc Inhibidores benzamidicos del receptor p2x7.
WO2004099146A1 (en) * 2003-05-12 2004-11-18 Pfizer Products Inc. Benzamide inhibitors of the p2x7 receptor
EP1837330B1 (en) * 2003-05-12 2012-10-24 Pfizer Products Inc. Benzamide inhibitors of the P2X7 receptor
WO2006003500A1 (en) 2004-06-29 2006-01-12 Pfizer Products Inc. Method for preparing 5-`4-(2-hydroxy-propyl)-3,5-dioxo-4,5-dihydro-3h`1,2,4!triazin-2-yl!-benzamide derivatives by deprotecting the hydroxyl-protected precursers
BRPI0512651A (pt) * 2004-06-29 2008-03-25 Pfizer Prod Inc método para a preparação de derivados de 5-4-(2-hidroxietil)-3,5-dioxo-4,5 dihidro-3h-1,2,4-trizin-2-ila com atividade inibidora de p2x7 por reaçaõ do derivado não substituìdo na posição 4 da trizina com um oxirano na presença de um ácido de lewis
EP1763353A1 (en) * 2004-06-29 2007-03-21 Warner-Lambert Company LLC COMBINATION THERAPIES UTILIZING BENZAMIDE INHIBITORS OF THE P2X<sb>7</sb> RECEPTOR
SA05260265A (ar) * 2004-08-30 2005-12-03 استرازينيكا ايه بي مركبات جديدة
WO2006083214A1 (en) * 2005-02-02 2006-08-10 Astrazeneca Ab Pharmaceutical composition comprising a p2x7 receptor antagonist and a hmg-coa reductase inhibitor
US20090124555A1 (en) * 2005-08-29 2009-05-14 Irma Bernatchez-Lemaire Use of histogranin and histogranin-like compounds as inhibitors of p2x7 receptor function and as anti-arthritic agents
WO2007109201A2 (en) * 2006-03-16 2007-09-27 Renovis, Inc. Bicycloheteroaryl compounds as p2x7 modulators and uses thereof
GB0622472D0 (en) * 2006-11-10 2006-12-20 Addex Pharmaceuticals Sa Novel heterocyclic derivatives
ES2576643T3 (es) * 2007-03-09 2016-07-08 Second Genome, Inc. Compuestos de bicicloheteroarilo como moduladores de P2X7 y usos de los mismos
GB0803729D0 (en) * 2008-02-29 2008-04-09 Ge Healthcare Ltd Imaging the central nervous system
CA2719745C (en) 2008-03-25 2016-07-05 Affectis Pharmaceuticals Ag Novel p2x7r antagonists and their use
ATE541832T1 (de) 2009-04-14 2012-02-15 Affectis Pharmaceuticals Ag Neuartige p2x7r-antagonisten und ihre verwendung
EA201290876A1 (ru) 2010-03-05 2013-03-29 Президент Энд Феллоуз Оф Гарвард Колледж Композиции индуцированных дендритных клеток и их использование
EP2386541A1 (en) 2010-05-14 2011-11-16 Affectis Pharmaceuticals AG Novel methods for the preparation of P2X7R antagonists
WO2012110190A1 (en) 2011-02-17 2012-08-23 Affectis Pharmaceuticals Ag Novel p2x7r antagonists and their use
CN103391923A (zh) * 2011-02-22 2013-11-13 埃科特莱茵药品有限公司 作为p2x7受体拮抗剂的苯甲酰胺衍生物
WO2012163792A1 (en) 2011-05-27 2012-12-06 Affectis Pharmaceuticals Ag Novel p2x7r antagonists and their use
WO2012163456A1 (en) 2011-05-27 2012-12-06 Affectis Pharmaceuticals Ag Novel p2x7r antagonists and their use
CA2838640C (en) 2011-07-22 2019-06-11 Actelion Pharmaceuticals Ltd Heterocyclic amide derivatives as p2x7 receptor antagonists
EA023752B1 (ru) * 2011-10-03 2016-07-29 Ооо "Эн.Си.Фарм" Фармацевтический состав для инъекций, обладающий нейропротекторной, антиамнестической, антиоксидантной, противогипоксической, противоишемической активностью (варианты)
EP2804865B1 (en) 2012-01-20 2015-12-23 Actelion Pharmaceuticals Ltd. Heterocyclic amide derivatives as p2x7 receptor antagonists
EA021231B1 (ru) * 2012-02-29 2015-05-29 Ооо "Фармацевтическая Компания "Славянская Аптека" Фармацевтический состав, обладающий сосудосуживающим, антиконгестивным, противовоспалительным действием (варианты)
EA020041B1 (ru) * 2012-03-11 2014-08-29 Ооо "Эн.Си.Фарм" Твердая лекарственная форма, обладающая нейропротекторной, антиамнестической, антиоксидантной, противогипоксической, противоишемической активностью (варианты)
EA021266B1 (ru) * 2012-03-14 2015-05-29 Ооо "Фармацевтическая Компания "Славянская Аптека" Фармацевтический состав, обладающий сосудосуживающим, антиконгестивным, противовоспалительным действием (варианты)
EA020538B1 (ru) * 2012-03-20 2014-11-28 Ооо "Эн.Си.Фарм" Фармацевтический состав, обладающий нейропротекторной, антиамнестической, антиоксидантной, противогипоксической, нейрометаболической, противоишемической активностью (варианты)
EA020539B1 (ru) * 2012-03-26 2014-11-28 Ооо "Эн.Си.Фарм" Фармацевтический состав, обладающий нейропротекторной, антиамнестической, антиоксидантной, противогипоксической, нейрометаболической, противоишемической активностью (варианты)
EA020521B1 (ru) * 2012-03-26 2014-11-28 Ооо "Эн.Си.Фарм" Фармацевтический состав, обладающий нейропротекторной, антиамнестической, антиоксидантной, противогипоксической, нейрометаболической, противоишемической активностью (варианты)
EA201200393A1 (ru) * 2012-03-30 2013-09-30 Анастасия Геннадьевна ЧЕЛЯЕВА Фармацевтический состав, обладающий противомикробным, бактериостатическим действием (варианты)
EA201200446A1 (ru) * 2012-04-06 2013-10-30 Анастасия Геннадьевна ЧЕЛЯЕВА Твердая лекарственная форма, обладающая отхаркивающим, местным обволакивающим и противовоспалительным действием (варианты)
EA020401B1 (ru) * 2012-07-09 2014-10-30 Ооо "Фармацевтическая Компания "Славянская Аптека" Фармацевтический состав, содержащий натрий, кальций, магний, железо, цинк и обладающий метаболическим, противокатарактным, ретинопротекторным действием (варианты)
EA020388B1 (ru) * 2012-10-01 2014-10-30 Ооо "Фармацевтическая Компания "Славянская Аптека" Фармацевтический состав, содержащий натрий, кальций, железо, цинк и обладающий метаболическим, противокатарактным, ретинопротекторным действием (варианты)
EA020361B1 (ru) * 2012-10-01 2014-10-30 Ооо "Фармацевтическая Компания "Славянская Аптека" Фармацевтический состав, содержащий магний, железо, цинк и обладающий метаболическим, противокатарактным, ретинопротекторным действием (варианты)
EA020109B1 (ru) * 2012-10-01 2014-08-29 Ооо "Эн.Си.Фарм" Твердая лекарственная форма, обладающая анорексигенным действием (варианты)
EA020129B1 (ru) * 2012-10-01 2014-08-29 Ооо "Эн.Си.Фарм" Твердая лекарственная форма, обладающая анорексигенным действием (варианты)
EA020402B1 (ru) * 2012-10-01 2014-10-30 Ооо "Фармацевтическая Компания "Славянская Аптека" Фармацевтический состав, содержащий натрий, кальций, цинк и обладающий метаболическим, противокатарактным, ретинопротекторным действием (варианты)
EA020404B1 (ru) * 2012-10-01 2014-10-30 Ооо "Фармацевтическая Компания "Славянская Аптека" Фармацевтический состав, содержащий кальций, железо, цинк и обладающий метаболическим, противокатарактным, ретинопротекторным действием (варианты)
EA020389B1 (ru) * 2012-10-01 2014-10-30 Ооо "Фармацевтическая Компания "Славянская Аптека" Фармацевтический состав, содержащий натрий, железо, цинк и обладающий метаболическим, противокатарактным, ретинопротекторным действием (варианты)
EA020043B1 (ru) * 2012-10-01 2014-08-29 Ооо "Эн.Си.Фарм" Твердая лекарственная форма, обладающая анорексигенным действием (варианты)
EA020403B1 (ru) * 2012-10-01 2014-10-30 Ооо "Фармацевтическая Компания "Славянская Аптека" Фармацевтический состав, содержащий натрий, кальций, магний, железо и обладающий метаболическим, противокатарактным, ретинопротекторным действием (варианты)
EA020060B1 (ru) * 2012-10-01 2014-08-29 Ооо "Эн.Си.Фарм" Твердая лекарственная форма, обладающая анорексигенным действием (варианты)
EA020143B1 (ru) * 2012-10-02 2014-08-29 Ооо "Эн.Си.Фарм" Твердая лекарственная форма, обладающая анорексигенным действием (варианты)
EA020061B1 (ru) * 2012-10-02 2014-08-29 Ооо "Эн.Си.Фарм" Твердая лекарственная форма, обладающая анорексигенным действием (варианты)
EA020063B1 (ru) * 2012-10-02 2014-08-29 Ооо "Эн.Си.Фарм" Твердая лекарственная форма, обладающая анорексигенным действием (варианты)
EA020021B1 (ru) * 2012-10-02 2014-08-29 Ооо "Эн.Си.Фарм" Твердая лекарственная форма, обладающая анорексигенным действием (варианты)
EA020062B1 (ru) * 2012-10-02 2014-08-29 Ооо "Эн.Си.Фарм" Твердая лекарственная форма, обладающая анорексигенным действием (варианты)
EA020162B1 (ru) * 2012-10-04 2014-09-30 Ооо "Эн.Си.Фарм" Твердая лекарственная форма, обладающая желчегонным действием (варианты)
TW201427947A (zh) 2012-10-12 2014-07-16 Lundbeck & Co As H 環狀胺
TWI598325B (zh) 2012-10-12 2017-09-11 Ｈ 朗德貝克公司 苯甲醯胺類
MX368044B (es) 2012-12-12 2019-09-17 Idorsia Pharmaceuticals Ltd Derivados de indol carboxamida como antagonistas del receptor p2x7.
EP2935211B1 (en) 2012-12-18 2016-11-09 Actelion Pharmaceuticals Ltd. Indole carboxamide derivatives as p2x7 receptor antagonists
EA024401B1 (ru) * 2012-12-28 2016-09-30 Ооо "Биотехсинтез" Фармацевтический состав, обладающий нейропротекторной, антиамнестической, антиоксидантной, противогипоксической, нейрометаболической, противоишемической активностью (варианты)
KR102220847B1 (ko) 2013-01-22 2021-02-26 이도르시아 파마슈티컬스 리미티드 Ｐ2ｘ7 수용체 길항제로서의 헤테로시클릭 아미드 유도체
KR102222220B1 (ko) 2013-01-22 2021-03-03 이도르시아 파마슈티컬스 리미티드 Ｐ2ｘ7 수용체 길항제로서의 헤테로시클릭 아미드 유도체
EA201300372A1 (ru) * 2013-04-17 2014-10-30 Ооо "Фармацевтическая Компания "Славянская Аптека" Антиоксидантный фармацевтический состав (варианты)
JP6422164B2 (ja) * 2013-12-26 2018-11-14 塩野義製薬株式会社 含窒素６員環誘導体およびそれらを含有する医薬組成物
DK3287443T3 (da) 2015-04-24 2022-02-07 Shionogi & Co 6-leddet heterocyklisk derivat og farmaceutisk sammensætning, som omfatter dette
WO2018074390A1 (ja) 2016-10-17 2018-04-26 塩野義製薬株式会社 二環性含窒素複素環誘導体およびそれらを含有する医薬組成物

Family Cites Families (66)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
BE640616A (es) 1962-12-19
US3492397A (en) 1967-04-07 1970-01-27 Warner Lambert Pharmaceutical Sustained release dosage in the pellet form and process thereof
US4060598A (en) 1967-06-28 1977-11-29 Boehringer Mannheim G.M.B.H. Tablets coated with aqueous resin dispersions
US3538214A (en) 1969-04-22 1970-11-03 Merck & Co Inc Controlled release medicinal tablets
US4173626A (en) 1978-12-11 1979-11-06 Merck & Co., Inc. Sustained release indomethacin
AU542544B2 (en) 1980-03-12 1985-02-28 Nippon Kayaku Kabushiki Kaisha Tetrahydrophthalimide derivatives
EP0077938A3 (en) 1981-10-23 1983-08-24 Mitsubishi Kasei Corporation N-(3-substituted aminophenyl) tetrahydrophthalimides and herbicidal composition
GR80558B (en) 1983-10-08 1985-02-06 Nippon Kayaku Kk Derivative of pyrazole and use thereof as a herbicide
US4766233A (en) 1984-06-12 1988-08-23 Fmc Corporation Herbicidal 2-aryl-1,2,4-triazine-3,5(2H,4H)-diones and sulfur analogs thereof
WO1986000072A1 (en) 1984-06-12 1986-01-03 Fmc Corporation Herbicidal 2-aryl-1,2,4-triazine-3,5(2h,4h)-diones and sulfur analogs thereof
GB8602342D0 (en) * 1986-01-30 1986-03-05 Janssen Pharmaceutica Nv 5 6-dihydro-2-(substituted phenyl)-1 2 4-triazine-3 5(2h 4h)-diones
EP0333791A1 (de) 1987-09-23 1989-09-27 Ciba-Geigy Ag Heterocyclische verbindungen
US5077409A (en) 1990-05-04 1991-12-31 American Cyanamid Company Method of preparing bis-aryl amide and urea antagonists of platelet activating factor
US5128351A (en) 1990-05-04 1992-07-07 American Cyanamid Company Bis-aryl amide and urea antagonists of platelet activating factor
BR9107169A (pt) 1990-12-17 1993-11-16 Shell Int Research Derivados de isoquinolina fungicidas
JP3089621B2 (ja) 1990-12-17 2000-09-18 日産化学工業株式会社 ウラシル誘導体
US5462938A (en) * 1990-12-21 1995-10-31 Annus; Gary D. Arthropodicidal oxadiazinyl, thiadiazinyl and triazinyl carboxanilides
GB9110679D0 (en) 1991-05-17 1991-07-10 Sandoz Ltd Improvements in or relating to organic compounds
GB9119467D0 (en) 1991-09-12 1991-10-23 Smithkline Beecham Corp Chemical compounds
TW403741B (en) * 1993-10-15 2000-09-01 Takeda Chemical Industries Ltd Triazine derivative, production and use thereof
US5691376A (en) 1994-02-17 1997-11-25 American Home Products Corporation Substituted biphenyl derivatives
DE4405614A1 (de) 1994-02-22 1995-08-24 Bayer Ag Substituierte Triazolinone
US5686061A (en) 1994-04-11 1997-11-11 The Board Of Regents Of The University Of Texas System Particulate contrast media derived from non-ionic water soluble contrast agents for CT enhancement of hepatic tumors
GB9412603D0 (en) 1994-06-23 1994-08-10 Sandoz Ltd Organic compounds
JP3144624B2 (ja) 1995-06-02 2001-03-12 杏林製薬株式会社 Ｎ−ベンジルジオキソチアゾリジルベンズアミド誘導体及びその製造法
JPH0959236A (ja) * 1995-08-23 1997-03-04 Dai Ichi Seiyaku Co Ltd ベンズアミド化合物
JP3906935B2 (ja) * 1995-12-18 2007-04-18 杏林製薬株式会社 Ｎ−置換ジオキソチアゾリジルベンズアミド誘導体及びその製造法
CA2240946C (en) 1995-12-21 2002-09-10 The Dupont Merck Pharmaceutical Company Isoxazoline, isothiazoline and pyrazoline factor xa inhibitors
EP0889877B1 (en) 1996-03-29 2001-08-29 G.D. Searle & Co. META-SUBSTITUTED PHENYLENE DERIVATIVES AND THEIR USE AS ALPHAvBETA3 INTEGRIN ANTAGONISTS OR INHIBITORS
RU2181360C2 (ru) * 1996-09-06 2002-04-20 Ниппон Каяку Кабусики Кайся Новые производные ацетамида, способ их получения, фармацевтический состав и ингибиторы протеаз на их основе
EP0946508B1 (en) 1996-12-23 2009-09-23 Bristol-Myers Squibb Pharma Company NITROGEN CONTAINING HETEROAROMATICS AS FACTOR Xa INHIBITORS
US6020357A (en) * 1996-12-23 2000-02-01 Dupont Pharmaceuticals Company Nitrogen containing heteroaromatics as factor Xa inhibitors
US6187797B1 (en) 1996-12-23 2001-02-13 Dupont Pharmaceuticals Company Phenyl-isoxazoles as factor XA Inhibitors
DE19701287A1 (de) * 1997-01-16 1998-07-23 Wernicke & Co Gmbh Verfahren zum Erhöhen der Gebrauchsdauer von Schleifscheiben
EP1019375A1 (en) 1997-03-25 2000-07-19 Astra Pharmaceuticals Limited Novel pyridine derivatives and pharmaceutical compositions containing them
AU7210398A (en) 1997-03-27 1998-10-22 Novartis Ag Intermediate products and method for the production of pyrimidine derivatives
DE19719621A1 (de) 1997-05-09 1998-11-12 Hoechst Ag Sulfonylaminocarbonsäuren
US5861950A (en) 1997-07-10 1999-01-19 Particle Measuring Systems, Inc. Particle detection system utilizing an inviscid flow-producing nozzle
US6297239B1 (en) 1997-10-08 2001-10-02 Merck & Co., Inc. Inhibitors of prenyl-protein transferase
SE9704272D0 (sv) 1997-11-21 1997-11-21 Astra Pharma Prod Novel Compounds
SE9704545D0 (sv) 1997-12-05 1997-12-05 Astra Pharma Prod Novel compounds
SE9704546D0 (sv) 1997-12-05 1997-12-05 Astra Pharma Prod Novel compounds
SE9704544D0 (sv) 1997-12-05 1997-12-05 Astra Pharma Prod Novel compounds
JPH11318492A (ja) 1998-03-09 1999-11-24 Aisin Seiki Co Ltd 蛍光発生性基質を含有する組成物
US6320078B1 (en) 1998-07-24 2001-11-20 Mitsui Chemicals, Inc. Method of producing benzamide derivatives
FR2783519B1 (fr) 1998-09-23 2003-01-24 Sod Conseils Rech Applic Nouveaux derives d'amidines, leur preparation, leur application a titre de medicaments et les compositions pharmaceutiques les contenant
DE19851184A1 (de) 1998-11-06 2000-05-11 Aventis Pharma Gmbh N-Arylsulfonyl-aminosäure-omega-amide
ES2249059T3 (es) 1998-12-16 2006-03-16 Bayer Healthcare Ag Nuevos compuestos de bifenilo y analogos de bifenilo como antagonista de integrina.
PL350907A1 (en) * 1999-04-09 2003-02-10 Astrazeneca Ab Adamantane derivatives
US6458952B1 (en) * 1999-05-19 2002-10-01 Pharmacia Corporation Substituted polycyclic aryl and heteroaryl uracils useful for selective inhibition of the coagulation cascade
EP1189879A1 (en) 1999-05-24 2002-03-27 Cor Therapeutics, Inc. INHIBITORS OF FACTOR Xa
SE9901875D0 (sv) 1999-05-25 1999-05-25 Astra Pharma Prod Novel compounds
EP1088821A1 (en) 1999-09-28 2001-04-04 Applied Research Systems ARS Holding N.V. Pharmaceutically active sulfonamide derivatives
EP1226112A4 (en) 1999-10-18 2004-10-13 Univ Connecticut RETRO-ANANDAMIDES, LIGANDS OF CANNABINOID RECEPTORS WITH HIGH AFFINITY AND STABILITY
SE9904505D0 (sv) 1999-12-09 1999-12-09 Astra Pharma Prod Novel compounds
TWI258462B (en) 1999-12-17 2006-07-21 Astrazeneca Ab Adamantane derivative compounds, process for preparing the same and pharmaceutical composition comprising the same
SE9904652D0 (sv) * 1999-12-17 1999-12-17 Astra Pharma Prod Novel Compounds
SE9904738D0 (sv) 1999-12-22 1999-12-22 Astra Pharma Prod Novel compounds
DE10005284A1 (de) 2000-02-07 2001-08-09 Bayer Ag Verfahren zur Herstellung von 1-Amino-3-aryl-uracilen
GB0006721D0 (en) 2000-03-20 2000-05-10 Mitchell Thomas A Assessment methods and systems
WO2003042190A1 (en) * 2001-11-12 2003-05-22 Pfizer Products Inc. N-alkyl-adamantyl derivatives as p2x7-receptor antagonists
PA8557501A1 (es) 2001-11-12 2003-06-30 Pfizer Prod Inc Benzamida, heteroarilamida y amidas inversas
PA8591801A1 (es) 2002-12-31 2004-07-26 Pfizer Prod Inc Inhibidores benzamidicos del receptor p2x7.
WO2004099146A1 (en) 2003-05-12 2004-11-18 Pfizer Products Inc. Benzamide inhibitors of the p2x7 receptor
BRPI0512651A (pt) 2004-06-29 2008-03-25 Pfizer Prod Inc método para a preparação de derivados de 5-4-(2-hidroxietil)-3,5-dioxo-4,5 dihidro-3h-1,2,4-trizin-2-ila com atividade inibidora de p2x7 por reaçaõ do derivado não substituìdo na posição 4 da trizina com um oxirano na presença de um ácido de lewis
WO2006003500A1 (en) 2004-06-29 2006-01-12 Pfizer Products Inc. Method for preparing 5-`4-(2-hydroxy-propyl)-3,5-dioxo-4,5-dihydro-3h`1,2,4!triazin-2-yl!-benzamide derivatives by deprotecting the hydroxyl-protected precursers

Also Published As

Publication number Publication date
IL168513A (en) 2011-06-30
DOP2003000790A (es) 2011-10-31
EP1581232A1 (en) 2005-10-05
US6974812B2 (en) 2005-12-13
KR20050098848A (ko) 2005-10-12
EP1581232B1 (en) 2014-04-09
JP4560411B2 (ja) 2010-10-13
MA27575A1 (fr) 2005-10-03
TWI288133B (en) 2007-10-11
US7176202B2 (en) 2007-02-13
HRP20050609A2 (en) 2006-02-28
MY141984A (en) 2010-08-16
NL1025148A1 (nl) 2004-07-01
BR0317803A (pt) 2005-11-29
AU2003285716B2 (en) 2010-03-18
CA2512193A1 (en) 2004-07-15
MXPA05006749A (es) 2005-09-08
OA12978A (en) 2006-10-13
US7671053B2 (en) 2010-03-02
KR100689138B1 (ko) 2007-03-08
US20090042886A1 (en) 2009-02-12
NL1025148C2 (nl) 2007-09-28
PL378251A1 (pl) 2006-03-20
CL2003002765A1 (es) 2005-01-07
AU2003285716A1 (en) 2004-07-22
IL212241A0 (en) 2011-06-30
CR7884A (es) 2005-08-05
CO5580749A2 (es) 2005-11-30
EA008591B1 (ru) 2007-06-29
US7407956B2 (en) 2008-08-05
UA82346C2 (en) 2008-04-10
ECSP055884A (es) 2005-09-20
WO2004058270A1 (en) 2004-07-15
AP1997A (en) 2009-04-22
EA200500777A1 (ru) 2005-12-29
US20060040939A1 (en) 2006-02-23
CA2512193C (en) 2010-09-07
JP2006513206A (ja) 2006-04-20
TNSN05174A1 (fr) 2007-05-14
NI200500118A (es) 2006-05-19
PA8591801A1 (es) 2004-07-26
NO20053587L (no) 2005-08-09
US20040180894A1 (en) 2004-09-16
ZA200503912B (en) 2006-07-26
US20070281939A1 (en) 2007-12-06
NZ539913A (en) 2007-11-30
GEP20084304B (en) 2008-02-11
ES2464350T3 (es) 2014-06-02
RS20050490A (en) 2007-11-15
IS7840A (is) 2005-05-09
UY28153A1 (es) 2004-07-30
GT200300297A (es) 2004-09-21
PE20040802A1 (es) 2004-11-25
TW200413336A (en) 2004-08-01
CN1732006A (zh) 2006-02-08
AP2005003350A0 (en) 2005-09-30

Similar Documents

Publication Publication Date Title
AR042673A1 (es) Inhibidores benzamidicos del receptor p2 x 7
CY1118102T1 (el) Αλατα διαμινιου φαινοθειαζινης και η χρηση αυτων
AR079648A1 (es) Inhibidores de la replicacion del virus de la hepatitis c
EA201591000A1 (ru) Пирролобензодиазепины
EA201700077A1 (ru) Соединения аминопиримидинила в качестве ингибиторов jak
EA201100113A1 (ru) Производные пурина для применения в лечении аллергических, воспалительных и инфекционных заболеваний
DE60115279D1 (de) Carbaminsäurederivate enthaltend eine amidgruppe als hdac-inhibitoren
RS54782B1 (sr) Novi heterociklični derivati i njihova upotreba u tretmanu neuroloških poremećaja
JP2014511892A5 (es)
MX2011009034A (es) Formas de profarmaco de inhibidores de cinasa y su uso en la terapia.
AR060432A1 (es) Tetrahidropteridinas utiles como inhibidores de las proteinas quinasas
EA201100115A1 (ru) Новые производные аденина
AR074608A1 (es) Derivados de 2-(piperidin-1-il)-4-heterociclil-tiazol-5-carboxilico para infecciones bacterianas
JP2014500265A5 (es)
AR086983A1 (es) Derivados de azetidinil fenil, piridil o pirazinil carboxamida como inhibidores de jak
CA2470476A1 (en) Pyrrolidine and piperidine derivates as nk1 antagonists
RU2013130256A (ru) Новые циклоспориновые производные для лечения и предупреждения вирусных инфекций
AR064212A1 (es) Uso de profarmacos de analogos de gaba para tratar enfermedades
JP2017504635A5 (es)
RU2015144653A (ru) Противовирусные соединения и их применения
JP2009533323A5 (es)
JP2007505931A5 (es)
ES2784475T3 (es) Compuestos de 6-hidroxi-2,5,7,8-tetrametilcromano para el tratamiento de enfermedades crónicas obstructivas de las vías respiratorias
AR083525A1 (es) Derivados de acido picolinico sustituidos con heterociclos, metodo para prepararlos, uso de los mismos como herbicidas y composiciones herbicidas que los contienen
RU2015137298A (ru) Ингибиторы тирозинкиназы брутона

Legal Events

Date Code Title Description
FB Suspension of granting procedure