[go: up one dir, main page]

AR086750A1 - Ligandos del receptor trpm8 y su uso en diversos tratamientos - Google Patents

Ligandos del receptor trpm8 y su uso en diversos tratamientos

Info

Publication number
AR086750A1
AR086750A1 ARP120102273A ARP120102273A AR086750A1 AR 086750 A1 AR086750 A1 AR 086750A1 AR P120102273 A ARP120102273 A AR P120102273A AR P120102273 A ARP120102273 A AR P120102273A AR 086750 A1 AR086750 A1 AR 086750A1
Authority
AR
Argentina
Prior art keywords
alkyl
nrara
nra
ora
substituted
Prior art date
Application number
ARP120102273A
Other languages
English (en)
Inventor
B Horne Daniel
R Kaller Matthew
Liu Qingyian
Van Ma Vu
Monenschein Holger
T Nguyen Thomas
J Jr St Jean David
Chenguang Yuan Chester
Biswas Kaustav
Brown James
J Chen Jian
Keshav Gore Vijay
Harried Scott
Zhong Wenge
Original Assignee
Amgen 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 Amgen Inc filed Critical Amgen Inc
Publication of AR086750A1 publication Critical patent/AR086750A1/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
    • 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
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/10—Laxatives
    • 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
    • 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
    • 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
    • A61P17/04—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
    • 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
    • A61P25/24—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
    • A61P25/26—Psychostimulants, e.g. nicotine, cocaine
    • 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
    • A61P31/20—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
    • 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
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • 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
    • C07D213/24—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 substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D213/36—Radicals substituted by singly-bound nitrogen atoms
    • C07D213/40—Acylated substituent nitrogen atom
    • 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
    • C07D213/61—Halogen atoms or nitro radicals
    • 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
    • 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
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • 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
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/04—Ortho-condensed systems

Landscapes

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

Abstract

Compuestos basados en amidas. Composiciones que los contienen. Su uso en el tratamiento del dolor agudo, del dolor en los dientes, de la cefalea en general, de la migraña, de la cefalea combinada, de los síndromes vasculares y no vasculares combinados, de la cefalea provocada por la tensión, de la inflamación en general, de la artritis, de las enfermedades reumáticas, de la osteoartritis, de los trastornos inflamatorios en el intestino, de los trastornos inflamatorios en los ojos, de los trastornos inflamatorios en la vejiga, de la inestabilidad a nivel de la vejiga, de la psoriasis, de las afecciones inflamatorias de la piel, de las afecciones inflamatorias crónicas, del dolor inflamatorio o de la hiperalgesia o la alodinia asociada a él, del dolor neuropático o de la hiperalgesia o la alodinia asociada a él, del dolor provocado por la neuropatía diabética, de la causalgia, del dolor que es mantenido por el sistema nervioso simpático, de los síndromes de diferenciación, del asma, de los daños o las disfunciones en el tejido epitelial, del herpes simple, de las alteraciones en la motilidad de las vísceras en los sistemas respiratorio, genitourinario, gastrointestinal o vascular, de las heridas, de las quemaduras, de las reacciones alérgicas en la piel, del prurito, del vitíligo, de los trastornos gastrointestinales en general, de la úlcera gástrica, de la úlcera duodenal, de la diarrea, de las lesiones gástricas inducidas por agentes necrosantes, de la pérdida de cabello, de la rinitis vasomotora o alérgica o de los trastornos en los bronquios. Reivindicación 1: Un compuesto caracterizado porque que tiene la estructura de formula (1) o cualquier sal farmacéuticamente aceptable del mismo, donde: m es 0, 1, 2 ó 3; n es 0 ó 1; X¹ es C(R⁴) o N; X² es C o N; R¹ se selecciona entre alquilo C₁₋₆ o un anillo saturado, parcialmente saturado o insaturado, monocíclico de 3, 4, 5, 6 ó 7 miembros o bicíclico de 7, 8, 9, 10 u 11 miembros, unido en forma directa, unido por alquilo C₁₋₂ o unido por alquil C₁₋₂-O que contiene 0, 1, 2, 3 ó 4 átomos seleccionados entre N, O y S, pero no contiene más que un átomo de O ó S, donde el alquilo C₁₋₆ y el anillo están sustituidos con 0, 1, 2 ó 3 sustituyentes seleccionados en forma independiente entre halo, oxo, alquilo C₁₋₆, haloalquilo C₁₋₄, ciano, nitro, -C(=O)Rᵃ, -C(=O)ORᵃ, -C(=O)NRᵃRᵃ, -C(=NRᵃ)NRᵃRᵃ, -ORᵃ, -OC(=O)Rᵃ, -OC(=O)NRᵃRᵃ, -OC(=O)N(Rᵃ)S(=O)₂Rᵃ, -O-alquil C₂₋₆-NRᵃRᵃ, O-alquil C₂₋₆-ORᵃ, -SRᵃ, -S(=O)Rᵃ, -S(=O)₂Rᵃ, -S(=O)₂NRᵃRᵃ, -S(=O)₂N(Rᵃ)C(=O)Rᵃ, -S(=O)₂N(Rᵃ)C(=O)ORᵃ, -S(=O)₂N(Rᵃ)C(=O)NRᵃRᵃ, -NRᵃRᵃ, -N(Rᵃ)C(=O)Rᵃ, -N(Rᵃ)C(=O)ORᵃ, -N(Rᵃ)C(=O)NRᵃRᵃ, -N(Rᵃ)C(=NRᵃ)NRᵃRᵃ, -N(Rᵃ)S(=O)₂Rᵃ, -N(Rᵃ)S(=O)₂NRᵃRᵃ, NRᵃ-alquil C₂₋₆-NRᵃRᵃ y NRᵃ-alquil C₂₋₆-ORᵃ, donde el anillo está adicionalmente sustituido con 0 ó 1 anillo saturado, parcialmente saturado o insaturado monocíclico de 3, 4, 5, 6 ó 7 miembros unido en forma directa, unido a través de SO₂, unido a través de C(=O) o unido a través de CH₂ sustituido con 0, 1, 2 ó 3 grupos seleccionados entre halo, alquilo C₁₋₆, haloalquilo C₁₋₄, ciano, nitro, -C(=O)Rᵃ, -C(=O)ORᵃ, -C(=O)NRᵃRᵃ, -C(=NRᵃ)NRᵃRᵃ, -ORᵃ, -OC(=O)Rᵃ, -SRᵃ, -S(=O)Rᵃ, -S(=O)₂Rᵃ, -S(=O)₂NRᵃRᵃ, -NRᵃRᵃ, y -N(Rᵃ)C(=O)Rᵃ; R² se selecciona entre H, halo, ciano, Rᶜ, -C(=O)Rᵇ, -C(=O)ORᵇ, -C(=O)NRᵃRᵃ, -C(=NRᵃ)NRᵃRᵃ, -ORᵃ, -OC(=O)Rᵇ, -OC(=O)NRᵃRᵃ, -O-alquil C₂₋₆-NRᵃRᵃ, O-alquil C₂₋₆-ORᵃ, -SRᵃ, -S(=O)Rᵇ, -S(=O)₂Rᵇ, -S(=O)₂NRᵃRᵃ, -NRᵃRᵃ, -N(Rᵃ)C(=O)Rᵇ, -N(Rᵃ)C(=O)ORᵇ, -N(Rᵃ)C(=O)NRᵃRᵃ, -N(Rᵃ)C(=NRᵃ)NRᵃRᵃ, -N(Rᵃ)S(=O)₂Rᵇ, -N(Rᵃ)S(=O)₂NRᵃRᵃ, NRᵃ-alquil C₂₋₆-NRᵃRᵃ y NRᵃ-alquil C₂₋₆-ORᵃ; o R² es alquilo C₁₋₆ sustituido con 0, 1, 2 ó 3 sustituyentes seleccionados entre haloalquilo C₁₋₄, halo, ciano, nitro, -C(=O)Rᵇ, -C(=O)ORᵇ, -C(=O)NRᵃRᵃ, -C(=NRᵃ)NRᵃRᵃ, -ORᵃ, -OC(=O)Rᵇ, -OC(=O)NRᵃRᵃ, O-alquil C₂₋₆-NRᵃRᵃ, -O-alquil C₂₋₆-ORᵃ, -SRᵃ, -S(=O)Rᵇ, S(=O)₂Rᵇ, S(=O)₂NRᵃRᵃ, -NRᵃRᵃ, -N(Rᵃ)C(=O)Rᵇ, -N(Rᵃ)C(=O)ORᵇ, -N(Rᵃ)C(=O)NRᵃRᵃ, -N(Rᵃ)C(=NRᵃ)NRᵃRᵃ, -N(Rᵃ)S(=O)₂Rᵇ, -N(Rᵃ)S(=O)₂NRᵃRᵃ, NRᵃ-alquil C₂₋₆-NRᵃRᵃ y NRᵃ-alquilo C₂₋₆-ORᵃ, o R² es alquilo C₁₋₆ sustituido con 0, 1, 2 ó 3 sustituyentes halo y adicionalmente sustituido con 0 ó 1 sustituyentes seleccionados entre Rᶜ; R³ es H, alquilo C₁₋₈, haloalquilo C₁₋₄, halo, ciano, -C(=O)Rᵇ, -C(=O)ORᵇ, -C(=O)NRᵃRᵃ, -C(=NRᵃ)NRᵃRᵃ, -ORᵃ, -OC(=O)Rᵇ, -OC(=O)NRᵃRᵃ, -O-alquil C₂₋₆-NRᵃRᵃ, -O-alquil C₂₋₆-ORᵃ, -SRᵃ, -S(=O)Rᵇ, -S(=O)₂Rᵇ, -S(=O)₂NRᵃRᵃ, -NRᵃRᵃ, -N(Rᵃ)C(=O)Rᵇ, -N(Rᵃ)C(=O)ORᵇ, -N(Rᵃ)C(=O)NRᵃRᵃ, -N(Rᵃ)C(=NRᵃ)NRᵃRᵃ, -N(Rᵃ)S(=O)₂Rᵇ, N(Rᵃ)S(=O)₂NRᵃRᵃ, NRᵃ-alquil C₂₋₆-NRᵃRᵃ o NRᵃ-alquil C₂₋₆-ORᵃ; R⁴ es en forma independiente, en cada instancia, H, alquilo C₁₋₆, -haloalquilo C₁₋₃, -O-alquilo C₁₋₆, -O-haloalquilo C₁₋₃, -N(alquil C₁₋₆)alquilo C₁₋₆, -NH-alquilo C₁₋₆, -NC(=O)alquilo C₁₋₆, -N(alquil C₁₋₆)alquilo C₁₋₆, F, Cl, Br, CN, OH o NH₂; o R³ y R⁴ juntos forman un puente insaturado de cuatro átomos que contiene 0 ó 1 átomos de N, donde el puente está sustituido con 0, 1 ó 2 sustituyentes R⁵; R⁵ es en forma independiente, en cada instancia, F, CH₃ o CF₃; R⁶ es F; Rᵃ es en forma independiente, en cada instancia, H o Rᵇ; Rᵇ es en forma independiente, en cada instancia, fenilo, bencilo o alquilo C₁₋₆, donde el fenilo, bencilo y alquilo C₁₋₆ está sustituido con 0, 1, 2 ó 3 sustituyentes seleccionados entre halo, oxo, alquilo C₁₋₄, haloalquilo C₁₋₃, -O-alquilo C₁₋₄, -OH, -NH₂, -O-alquilo C₁₋₄, -O-haloalquilo C₁₋₄, -NH-alquilo C₁₋₄, y -N(alquil C₁₋₄)alquilo C₁₋₄; y Rᶜ es en forma independiente, en cada instancia, un anillo saturado, parcialmente saturado o insaturado monocíclico de 4, 5 ó 6 miembros que contiene 0, 1, 2, 3 ó 4 átomos seleccionados entre N, O y S, donde el alquilo C₁₋₆ y el anillo están sustituidos con 0 ó 1 grupos oxo sustituidos con 0, 1, 2 ó 3 sustituyentes seleccionados entre alquilo C₁₋₈, haloalquilo C₁₋₄, halo y ciano.
ARP120102273A 2011-06-24 2012-06-25 Ligandos del receptor trpm8 y su uso en diversos tratamientos AR086750A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US201161500843P 2011-06-24 2011-06-24

Publications (1)

Publication Number Publication Date
AR086750A1 true AR086750A1 (es) 2014-01-22

Family

ID=46384521

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP120102273A AR086750A1 (es) 2011-06-24 2012-06-25 Ligandos del receptor trpm8 y su uso en diversos tratamientos

Country Status (23)

Country Link
US (3) US8710043B2 (es)
EP (1) EP2723717A2 (es)
JP (1) JP2014527511A (es)
KR (1) KR20140045507A (es)
CN (1) CN103906733A (es)
AP (1) AP2013007331A0 (es)
AR (1) AR086750A1 (es)
AU (1) AU2012272895B2 (es)
BR (1) BR112013033316A2 (es)
CA (1) CA2839699A1 (es)
CL (1) CL2013003715A1 (es)
CO (1) CO6852073A2 (es)
CR (1) CR20140037A (es)
EA (1) EA201490152A1 (es)
MA (1) MA35271B1 (es)
MX (1) MX2013015274A (es)
MY (1) MY157429A (es)
PE (1) PE20140868A1 (es)
PH (1) PH12013502611A1 (es)
TN (1) TN2013000529A1 (es)
TW (2) TW201429948A (es)
UY (1) UY34160A (es)
WO (1) WO2012177893A2 (es)

Families Citing this family (17)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8952009B2 (en) 2012-08-06 2015-02-10 Amgen Inc. Chroman derivatives as TRPM8 inhibitors
CA2962922C (en) * 2014-09-29 2021-10-26 The Scripps Research Institute Sphingosine-1-phosphate receptor modulators for treatment of cardiopulmonary disorders
US9765026B2 (en) * 2015-08-28 2017-09-19 Scinopharm Taiwan, Ltd. Forms of apremilast and the process of making the same
ES2957232T3 (es) * 2016-06-13 2024-01-15 Mitsubishi Tanabe Pharma Corp Composiciones para el tratamiento o la prevención de síntomas vasomotores
JP2020524717A (ja) * 2017-06-22 2020-08-20 キュラデブ・ファーマ・リミテッドＣｕｒａｄｅｖ Ｐｈａｒｍａ Ｌｉｍｉｔｅｄ ヒトｓｔｉｎｇの小分子調節因子
WO2018234808A1 (en) 2017-06-22 2018-12-27 Curadev Pharma Limited Small molecule modulators of human sting
WO2019124366A1 (en) 2017-12-19 2019-06-27 Mitsubishi Tanabe Pharma Corporation Compositions and methods for treating or preventing vasomotor symptoms
WO2019180627A1 (en) * 2018-03-21 2019-09-26 Piramal Enterprises Limited AN IMPROVED ASYMMETRIC SYNTHESIS OF alpha-(DIARYLMETHYL) ALKYL AMINES
WO2019202522A1 (en) * 2018-04-18 2019-10-24 Piramal Enterprises Limited An improved asymmetric synthesis of alpha-branched chiral amines
CN110981795B (zh) * 2019-12-18 2021-02-12 武汉世纪久海检测技术有限公司 一种利用2-氰基异烟酸甲酯制备2-氨酰基异烟酸的方法
KR20230026404A (ko) * 2020-06-17 2023-02-24 머크 샤프 앤드 돔 엘엘씨 Nav1.8 억제제로서의 2-옥소-옥사졸리딘-5-카르복스아미드
WO2021257490A1 (en) 2020-06-17 2021-12-23 Merck Sharp & Dohme Corp. 2-oxoimidazolidine-4-carboxamides as nav1.8 inhibitors
CN115697327A (zh) * 2020-06-17 2023-02-03 默沙东有限责任公司 作为nav1.8抑制剂的5-氧代-吡咯烷-3-甲酰胺
CA3221549A1 (en) * 2021-06-08 2022-12-15 Liqiang Fu Isoindolinone compounds, and uses thereof
CN115108980B (zh) * 2022-06-22 2023-06-16 济南大学 一种2-甲基喹啉类化合物的4号位酰基化衍生物的制备方法
WO2025113520A1 (zh) * 2023-11-28 2025-06-05 成都地奥制药集团有限公司 酰胺类化合物及其用途
CN119118901B (zh) * 2024-09-09 2025-09-30 中国人民解放军北部战区总医院 一种氧吲哚类衍生物及其制备方法与在trpa1抑制剂方向的应用

Family Cites Families (178)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US2483250A (en) 1949-09-27 Tt a it tt
DE2417763A1 (de) 1974-04-11 1975-10-30 Bayer Ag Carbonsaeureamide, verfahren zu ihrer herstellung sowie ihre verwendung als arzneimittel
DE2428673A1 (de) 1974-06-14 1976-01-02 Bayer Ag Carbonsaeureamide, verfahren zu ihrer herstellung sowie ihre verwendung als arzneimittel
PT72878B (en) 1980-04-24 1983-03-29 Merck & Co Inc Process for preparing mannich-base hydroxamic acid pro-drugs for the improved delivery of non-steroidal anti-inflammatory agents
US5081131A (en) 1986-01-13 1992-01-14 American Cyanamid Company Omega-((hetero)alkyl)benz(cd)-indol-2-amines
US5223499A (en) 1989-05-30 1993-06-29 Merck & Co., Inc. 6-amino substituted imidazo[4,5-bipyridines as angiotensin II antagonists
ZA913730B (en) 1990-05-30 1992-02-26 Ici Plc Anti-tumor compounds
US5380721A (en) 1990-09-10 1995-01-10 Sterling Winthrop Inc. Aryl-fused and hetaryl-fused-2,4-diazepine and 2,4-diazocine antiarrhythmic agents
WO1992012973A1 (en) 1991-01-23 1992-08-06 Nippon Kayaku Kabushiki Kaisha Chroman derivative
ES2036926B1 (es) 1991-08-08 1994-01-16 Uriach & Cia Sa J "procedimiento para la obtencion de derivados de la (2-alquil-3-piridil)metilpiperazina".
JP2600644B2 (ja) 1991-08-16 1997-04-16 藤沢薬品工業株式会社 チアゾリルベンゾフラン誘導体
DE4135474A1 (de) 1991-10-28 1993-04-29 Bayer Ag 2-aminomethyl-chromane
DE4138819A1 (de) 1991-11-26 1993-05-27 Basf Ag Hydroxypyridoncarbonsaeureamide, deren herstellung und verwendung
GB9127041D0 (en) 1991-12-20 1992-02-19 Fujisawa Pharmaceutical Co New use
FR2692895A1 (fr) 1992-06-26 1993-12-31 Adir Nouveaux 1-oxo 2,4,5,6-tétrahydro 2,3,7-triazaphénalènes leurs procédés de préparation et les compositions pharmaceutiques qui les contiennent.
DE4304455A1 (de) 1993-02-15 1994-08-18 Bayer Ag Heterocyclisch substituierte Phenyl-cyclohexan-carbonsäurederivate
EP0653434A1 (en) 1993-11-12 1995-05-17 Tanabe Seiyaku Co., Ltd. Glucosamine derivative, process for preparing the same and synthetic intermediate thereof
CA2207618A1 (en) 1994-12-23 1996-07-04 Helmut Pieper Piperazine derivatives, medicaments comprising these compounds, their use and processes for their preparation
US5916906A (en) 1995-03-14 1999-06-29 Shaskan; Edward G. Compositions comprising nicotinylalanine and an inhibitor of glycine conjugation or vitamin B6
US5891872A (en) 1995-04-07 1999-04-06 Schering Corporation Tricyclic compounds
IN186549B (es) 1995-04-19 2001-09-29 Kumiai Chemical Co Ltd
DE19518681A1 (de) 1995-05-22 1996-11-28 Bayer Ag Verfahren zur Herstellung von 5,6-Dihydro-1,3-oxazinen
DE19523087A1 (de) 1995-06-26 1997-01-02 Bayer Ag 1,3-Oxa(thia)zin-Derivate
IL118631A (en) 1995-06-27 2002-05-23 Tanabe Seiyaku Co History of pyridazinone and processes for their preparation
GB9518552D0 (en) 1995-09-11 1995-11-08 Fujisawa Pharmaceutical Co New heterocyclic compounds
EP0858457A1 (de) 1995-10-20 1998-08-19 Dr. Karl Thomae GmbH 5-gliedrige heterocyclen, diese verbindungen enthaltende arzneimittel und deren verwendung sowie verfahren zu ihrer herstellung
GB9525828D0 (en) 1995-12-18 1996-02-21 Bayer Ag Use of hetarylacetic acid derivatives
US5977090A (en) 1996-09-27 1999-11-02 Guilford Pharmaceuticals Inc. Pharmaceutical compositions and methods of treating compulsive disorders using NAALADase inhibitors
US6268384B1 (en) 1997-08-29 2001-07-31 Vertex Pharmaceuticals Incorporated Compounds possessing neuronal activity
US6075029A (en) 1998-01-02 2000-06-13 Cell Therapeutics, Inc. Xanthine modulators of metabolism of cellular P-450
JP4432261B2 (ja) 1998-01-21 2010-03-17 萬有製薬株式会社 複素芳香環縮合シクロペンテノピリジン誘導体
EP1082095A1 (en) 1998-06-03 2001-03-14 GPI NIL Holdings, Inc. N-oxide of heterocyclic ester, amide, thioester or ketone hair growth compositions and uses
US5910595A (en) 1998-06-26 1999-06-08 Salsbury Chemicals, Inc. Process for preparing oximidazoles
US6617351B1 (en) 1998-07-31 2003-09-09 Eli Lilly And Company Amide, carbamate, and urea derivatives
US6166028A (en) 1998-12-09 2000-12-26 American Home Products Corporation Diaminopuridine-containing thiourea inhibitors of herpes viruses
WO2000035889A1 (en) 1998-12-11 2000-06-22 Sankyo Company, Limited Substituted benzylamines
WO2000039102A1 (en) 1998-12-23 2000-07-06 Du Pont Pharmaceuticals Company THROMBIN OR FACTOR Xa INHIBITORS
US6200993B1 (en) 1999-05-05 2001-03-13 Merck Frosst Canada & Co. Heterosubstituted pyridine derivatives as PDE4 inhibitors
TR200002099A2 (tr) 1999-07-22 2001-06-21 Sankyo Company Limited Siklobüten türevleri, bunların hazırlanması ve terapötik kullanımları
GB9919588D0 (en) 1999-08-18 1999-10-20 Hoechst Schering Agrevo Gmbh Fungicidal compounds
BR0013593A (pt) 1999-09-01 2002-05-07 Unilever Nv Método para alvejar manchas de tecido
BR0013592A (pt) 1999-09-01 2002-05-07 Unilever Nv Embalagem comercial para alvejar manchas de tecido em um licor de lavagem aquoso, e, uso da mesma
EP1208188A1 (en) 1999-09-01 2002-05-29 Unilever Plc Composition and method for bleaching a substrate
US7291641B2 (en) 1999-10-11 2007-11-06 Societe De Conseils De Recherches Et D'applications Scientifiques (S.C.R.A.S.) Derivatives of heterocycles with 5 members, their preparation and their use as medicaments
CA2325358C (en) 1999-11-10 2005-08-02 Pfizer Products Inc. 7-¬(4'-trifluoromethyl-biphenyl-2-carbonyl)amino|-quinoline-3-carboxylic acid amides, and methods of inhibiting the secretion of apolipoprotein b
CN1260227C (zh) 1999-11-10 2006-06-21 武田药品工业株式会社 含氮的五元杂环化合物
IL139450A0 (en) 1999-11-10 2001-11-25 Pfizer Prod Inc Methods of administering apo b-secretion/mtp inhibitors
TW574193B (en) 1999-12-03 2004-02-01 Astrazeneca Ab Novel phenalkyloxy-phenyl derivatives, pharmaceutical composition containing the same and their uses
JP2003519697A (ja) 1999-12-28 2003-06-24 ファイザー・プロダクツ・インク 炎症性疾患、自己免疫疾患および呼吸器疾患の処置に有用な非ペプチド系のｖｌａ−４依存性細胞結合阻害薬
EP1254114A2 (en) 2000-01-28 2002-11-06 Melacure Therapeutics AB Melanocortin receptor agonists and antagonists
CA2399791A1 (en) 2000-02-11 2001-08-16 Bristol-Myers Squibb Company Cannabinoid receptor modulators, their processes of preparation, and use of cannabinoid receptor modulators in treating respiratory and non-respiratory diseases
US20020019527A1 (en) 2000-04-27 2002-02-14 Wei-Bo Wang Substituted phenyl farnesyltransferase inhibitors
JP2004509064A (ja) 2000-04-27 2004-03-25 アボット・ラボラトリーズ 置換フェニルファルネシルトランスフェラーゼ阻害剤
US6448281B1 (en) 2000-07-06 2002-09-10 Boehringer Ingelheim (Canada) Ltd. Viral polymerase inhibitors
US6417367B1 (en) 2000-08-11 2002-07-09 Pfizer Inc. Methods of making quinoline amides
US20030050211A1 (en) 2000-12-14 2003-03-13 Unilever Home & Personal Care Usa, Division Of Conopco, Inc. Enzymatic detergent compositions
WO2002051396A1 (en) 2000-12-26 2002-07-04 Sankyo Company, Limited Pharmaceutical compositions containing cyclobutene derivatives
US20040106635A1 (en) 2001-03-29 2004-06-03 Iwao Takamuro Spiroisoquinoline compound, a method for preparing the same and an intermediate thereof
DE10121003A1 (de) 2001-04-28 2002-12-19 Aventis Pharma Gmbh Anthranilsäureamide, Verfahren zur Herstellung, ihrer Verwendung als Medikament sowie sie enthaltende pharmazeutische Zubereitungen
MY130373A (en) 2001-10-29 2007-06-29 Malesci Sas Linear basic compounds having nk-2 antagonist activity and formulations thereof
RU2293083C2 (ru) 2001-11-27 2007-02-10 Ф.Хоффманн-Ля Рош Аг Производные бензотиазола и лекарственное средство на их основе
JP2005510564A (ja) 2001-11-28 2005-04-21 藤沢薬品工業株式会社 アポリポタンパク質ｂ阻害剤としての複素環式アミド化合物
AR037746A1 (es) 2001-12-06 2004-12-01 Novartis Ag Compuestos derivados de amidoacetonitrilo, un procedimiento para su preparacion, un procedimiento para la preparacion de compuestos intermediarios, una composicion para combatir parasitos, un procedimiento para combatir dichos parasitos, y el empleo de dichos derivados para la preparacion de una com
SE0104248D0 (sv) 2001-12-14 2001-12-14 Astrazeneca Ab Method of treatment
CN100383124C (zh) 2002-02-04 2008-04-23 霍夫曼-拉罗奇有限公司 作为npy拮抗剂的喹啉衍生物
IL164212A0 (en) 2002-03-28 2005-12-18 Applied Research Systems Thiazolidine carboxamide derivatives, their preparation and pharmaceutical compositions containing them
US7282591B2 (en) 2002-04-11 2007-10-16 Merck & Co., Inc. 1h-benzo{f}indazol-5-yl derivatives as selective glucocorticoid receptor modulators
FR2838739B1 (fr) 2002-04-19 2004-05-28 Sanofi Synthelabo Derives de n-[phenyl(piperidin-2-yl)methyl)benzamide, leur preparation et leur application en therapeutique
WO2003091217A1 (en) 2002-04-26 2003-11-06 Ishihara Sangyo Kaisha, Ltd. Pyridine compounds or salts thereof and herbicides containing the same
US7375093B2 (en) 2002-07-05 2008-05-20 Intrexon Corporation Ketone ligands for modulating the expression of exogenous genes via an ecdysone receptor complex
FR2842805A1 (fr) 2002-07-29 2004-01-30 Sanofi Synthelabo Derives de n-[phenyl(piperidin-2-yl)methyl]benzamide,leur preparation et leur application et therapeutique
GB0221697D0 (en) 2002-09-18 2002-10-30 Unilever Plc Novel compouds and their uses
WO2004029204A2 (en) 2002-09-27 2004-04-08 Merck & Co., Inc. Substituted pyrimidines
WO2004039795A2 (en) 2002-10-29 2004-05-13 Fujisawa Pharmaceutical Co., Ltd. Amide compounds for the treatment of hyperlipidemia
EP1560488B1 (en) 2002-11-05 2010-09-01 Glaxo Group Limited Antibacterial agents
AU2003290333A1 (en) 2002-12-24 2004-07-22 Biofocus Plc Compound libraries of imidazo(1,5-a)pyridin-3-yl derivatives and related heterobicycles for targetting compounds capable of binding to g-protein coupled receptors
US7601868B2 (en) 2003-02-12 2009-10-13 Takeda Pharmaceutical Company Limited Amine derivative
EP1625115A1 (en) 2003-05-09 2006-02-15 Pharmacia & Upjohn Company LLC Substituted pyrimidine derivatives
EP1660454A1 (en) * 2003-07-07 2006-05-31 Vernalis (R&D) Limited Azacyclic compounds as inhibitors of sensory neurone specific channels
EP1776362A1 (en) 2003-07-18 2007-04-25 Virochem Pharma Inc. Spiro compounds and methods for the modulation of chemokine receptor activity
US7094791B2 (en) 2003-07-31 2006-08-22 Avalon Pharmaceuticals, Inc. Derivatives of 3-hydroxy-pyrrole-2,4-dicarboxylic acid and uses thereof
WO2005021545A1 (en) 2003-09-03 2005-03-10 Galapagos Nv IMIDAZO[1,5-a]PYRIDINE OR IMIDAZO[1,5-a]PIPERIDINE DERIVATIVES AND THEIR USE FOR THE PREPARATION OF MEDICAMENT AGAINST 5-HT2A RECEPTOR-RELATED DISORDERS
GB0320983D0 (en) 2003-09-08 2003-10-08 Biofocus Plc Compound libraries
EP1786816A4 (en) 2003-09-10 2009-11-04 Virochem Pharma Inc SPIROHYDANTOIN COMPOUNDS AND METHODS FOR MODULATING CHEMOKINE RECEPTOR ACTIVITY
WO2005046683A1 (en) * 2003-10-07 2005-05-26 Renovis, Inc. Amide derivatives as ion-channel ligands and pharmaceutical compositions and methods of using the same
WO2005042524A1 (en) 2003-10-30 2005-05-12 Virochem Pharma Inc. Pyridine carboxamide and methods for inhibiting hiv integrase
CA2555133A1 (en) 2004-02-04 2005-09-01 Pfizer Products Inc. Substituted quinoline compounds
GB0403578D0 (en) 2004-02-18 2004-03-24 Biofocus Discovery Ltd Compounds which interact with the G-protein coupled receptor family
JP2007526324A (ja) 2004-03-02 2007-09-13 スミスクライン・ビーチャム・コーポレイション Ａｋｔ活性のある阻害剤
CA2561791A1 (en) 2004-03-31 2005-10-20 Janssen Pharmaceutica, N.V. Non-imidazole heterocyclic compounds
DE102004022897A1 (de) 2004-05-10 2005-12-08 Bayer Cropscience Ag Azinyl-imidazoazine
US7550499B2 (en) 2004-05-12 2009-06-23 Bristol-Myers Squibb Company Urea antagonists of P2Y1 receptor useful in the treatment of thrombotic conditions
WO2005115374A1 (en) 2004-05-29 2005-12-08 7Tm Pharma A/S Crth2 receptor ligands for therapeutic use
DE102004039876A1 (de) 2004-06-23 2006-01-26 Lanxess Deutschland Gmbh Herstellung von fluorierten 1,3-Benzodioxanen
DE102004031323A1 (de) 2004-06-29 2006-01-19 Bayer Cropscience Ag Substituierte Pyridazincarboxamide und Derivate hiervon
JP2008511552A (ja) * 2004-08-30 2008-04-17 ニューロメッド ファーマシューティカルズ リミテッド カルシウムチャネルブロッカーとしての尿素誘導体
AR050926A1 (es) 2004-09-03 2006-12-06 Astrazeneca Ab Derivados de benzamida como inhibidores de la histonadesacetilasa(hdac)
KR100677149B1 (ko) 2004-11-12 2007-02-02 삼성전자주식회사 잉크 조성물
EP1829863A4 (en) 2004-11-26 2009-04-22 Takeda Pharmaceutical ARYLALKANSÄUREDERIVAT
EP1831194A4 (en) 2004-12-21 2009-12-02 Astrazeneca Ab HETEROCYCLIC ANTAGONISTS OF MCHr1 AND THERAPEUTIC APPLICATIONS THEREOF
US20080207677A1 (en) 2004-12-31 2008-08-28 Gpc Biotech Ag Napthyridine Compounds As Rock Inhibitors
US20060173183A1 (en) 2004-12-31 2006-08-03 Alantos Pharmaceuticals, Inc., Multicyclic bis-amide MMP inhibitors
EP1844003A4 (en) 2005-01-27 2010-09-22 Astrazeneca Ab NEW BIAROMATIC COMPOUNDS AS INHIBITORS OF THE P2X7 RECEPTOR
WO2006094246A2 (en) 2005-03-03 2006-09-08 Sirtris Pharmaceuticals, Inc. N-arylmethyl benzamide sirtuin modulators
US20070155738A1 (en) 2005-05-20 2007-07-05 Alantos Pharmaceuticals, Inc. Heterobicyclic metalloprotease inhibitors
JP2008545744A (ja) 2005-06-02 2008-12-18 バイエル・クロツプサイエンス・アクチエンゲゼルシヤフト フェニルアルキル置換ヘテロアリール誘導体
ES2536351T3 (es) 2005-06-13 2015-05-22 Merck Sharp & Dohme Limited Agentes terapéuticos
ES2525217T3 (es) 2005-06-27 2014-12-19 Exelixis Patent Company Llc Moduladores de LXR basados en imidazol
CA2609319C (en) 2005-07-15 2014-02-04 Nissan Chemical Industries, Ltd. Thiophene compounds and thrombopoietin receptor activators
CN100494167C (zh) 2005-08-02 2009-06-03 天津大学 抗乙肝病毒的叔胺氧化物及制备方法和制备药物的应用
WO2007017093A1 (en) 2005-08-04 2007-02-15 Bayer Healthcare Ag Substituted 2-benzyloxy-benzoic acid amide derivatives
EP1764098A1 (en) 2005-09-17 2007-03-21 Speedel Experimenta AG Diaminoalcohols derivatives for the treatment of Alzheimer, malaria, HIV
CA2628875A1 (en) 2005-11-10 2007-05-18 Bayer Healthcare Ag Diaryl ureas for treating diabetic neuropathy
US20090176791A1 (en) 2005-11-10 2009-07-09 Bayer Healthcare Ag Diaryl Ureas for Treating Pulmonary Hypertension
US7888376B2 (en) 2005-11-23 2011-02-15 Bristol-Myers Squibb Company Heterocyclic CETP inhibitors
DE102005059479A1 (de) 2005-12-13 2007-06-14 Merck Patent Gmbh Hydroxychinolinderivate
EP1962829A1 (en) 2005-12-15 2008-09-03 Bayer HealthCare AG Diaryl ureas for treating virus infections
CA2633411A1 (en) 2005-12-15 2007-06-21 Bayer Healthcare Ag Diaryl ureas for treating inflammatory skin, eye and/or ear diseases
TWI412322B (zh) 2005-12-30 2013-10-21 Du Pont 控制無脊椎害蟲之異唑啉
JP2009524656A (ja) 2006-01-27 2009-07-02 アストラゼネカ・アクチエボラーグ アミド置換キノリン
JP2009527459A (ja) 2006-02-23 2009-07-30 武田薬品工業株式会社 縮合窒素含有複素環化合物
DE102006012251A1 (de) 2006-03-15 2007-11-08 Grünenthal GmbH Substituierte 4-Amino-chinazolin-Derivate und ihre Verwendung zur Herstellung von Arzneimitteln
EP2010493B1 (en) 2006-04-12 2016-01-27 Merck Sharp & Dohme Corp. Pyridyl amide t-type calcium channel antagonists
JP2009538317A (ja) 2006-05-26 2009-11-05 バイエル ヘルスケア リミティド ライアビリティ カンパニー 癌治療のための置換ジアリールウレアを用いた薬物の組み合わせ
GB0611152D0 (en) 2006-06-06 2006-07-19 Ucb Sa Therapeutic agents
WO2008003746A1 (en) 2006-07-06 2008-01-10 Bayer Cropscience Sa N-(4-pyridin-2-ylbutyl) carboxamide derivatives, their process of preparation and their use as fungicides
CN101611009A (zh) 2006-07-25 2009-12-23 伊维沃制药股份有限公司 喹啉衍生物
CA2661459A1 (en) * 2006-08-21 2008-02-28 F. Hoffmann-La Roche Ag Di-aromatic substituted amides as inhibitors for glyt1
US7834023B2 (en) 2006-09-20 2010-11-16 Portola Pharmaceuticals, Inc. Substituted dihydroquinazolines as platelet ADP receptor inhibitors
WO2008056687A1 (en) 2006-11-09 2008-05-15 Daiichi Sankyo Company, Limited Novel spiropiperidine derivative
AU2007321920A1 (en) 2006-11-20 2008-05-29 Alantos Pharmaceuticals Holding, Inc. Heterotricyclic metalloprotease inhibitors
WO2008063670A1 (en) 2006-11-20 2008-05-29 Alantos Pharmaceuticals Holding, Inc. Heterobicyclic matrix metalloprotease inhibitors
EP2121621B1 (en) 2006-12-08 2014-05-07 Exelixis Patent Company LLC Lxr and fxr modulators
US7872018B2 (en) 2006-12-21 2011-01-18 Plexxikon, Inc. Compounds and methods for kinase modulation, and indications therefor
US20080293711A1 (en) 2007-03-08 2008-11-27 Clark Michael P Chemokine receptor modulators
EP2146715A4 (en) 2007-04-11 2011-08-31 Merck Sharp & Dohme CGR-RECEPTOR ANTAGONISTS WITH TERTIARY AMID, SULFONAMIDE, CARBAMATE AND UREA END GROUPS
ES2504565T3 (es) 2007-06-05 2014-10-08 Merck Sharp & Dohme Corp. Antagonistas del receptor CGRP de carboxamida heterocíclica
US20100261723A1 (en) 2007-07-09 2010-10-14 Astrazeneca Ab Trisubstituted pyrimidine derivatives for the treatment of proliferative diseases
WO2009023179A2 (en) 2007-08-10 2009-02-19 Genelabs Technologies, Inc. Nitrogen containing bicyclic chemical entities for treating viral infections
EP2188295A4 (en) 2007-08-10 2011-11-16 Crystalgenomics Inc PYRIDINE DERIVATIVES AND METHODS OF USE
WO2009038812A1 (en) 2007-09-20 2009-03-26 Amgen Inc. Condensed piperidine derivatives useful as vanilloid receptor ligands
US8476297B2 (en) 2007-12-04 2013-07-02 Amgen Inc. TRP-M8 receptor ligands and their use in treatments
WO2009072621A1 (ja) 2007-12-07 2009-06-11 Nissan Chemical Industries, Ltd. 置換ジヒドロアゾール化合物及び有害生物防除剤
WO2009117269A1 (en) 2008-03-18 2009-09-24 Merck & Co., Inc. Substituted 4-hydroxypyrimidine-5-carboxamides
US20110015198A1 (en) 2008-03-28 2011-01-20 Banyu Pharmaceutical Co., Inc. Diarylmethylamide derivative having melanin-concentrating hormone receptor antagonism
AR071310A1 (es) 2008-04-11 2010-06-09 Merck Serono Sa Sulfonamidas
DE102008019838A1 (de) 2008-04-19 2009-12-10 Boehringer Ingelheim International Gmbh Neue Arylsulfonylglycin-Derivate, deren Herstellung und deren Verwendung als Arzneimittel
CA2727243A1 (en) 2008-06-12 2009-12-17 Merck Sharp & Dohme Corp. Branched 3- and 6-substituted quinolines as cgrp receptor antagonists
RU2011102471A (ru) 2008-06-25 2012-07-27 Байер Шеринг Фарма Акциенгезелльшафт (De) Диарилмочевины для лечения сердечной недостаточности
ES2610882T3 (es) * 2008-08-19 2017-05-03 Janssen Pharmaceutica, N.V. Antagonistas del receptor al mentol frío
CN101343313B (zh) 2008-09-03 2011-11-16 南京农业大学 一种葡萄糖二肽类化合物及其制备方法和用途
TWI389913B (zh) 2008-09-08 2013-03-21 Lg Life Sciences Ltd 并合雜環化合物
CN102209541B (zh) 2008-09-08 2016-05-18 小利兰·斯坦福大学托管委员会 醛脱氢酶活性调节剂和其使用方法
WO2010046780A2 (en) 2008-10-22 2010-04-29 Institut Pasteur Korea Anti viral compounds
TW201030001A (en) 2008-11-14 2010-08-16 Amgen Inc Pyridine and pyrimidine derivatives as phosphodiesterase 10 inhibitors
UY32525A (es) 2009-04-03 2010-10-29 Astrazeneca Ab Compuestos que tienen actividad agonista del receptor de glucocorticosteroides
MX2011011428A (es) * 2009-05-01 2011-11-29 Raqualia Pharma Inc Derivados de acido sulfamoilbenzoico como antagonistas de trpm8.
CA2761639C (en) 2009-05-29 2016-06-07 Raqualia Pharma Inc. Aryl substituted carboxamide derivatives as calcium or sodium channel blockers
WO2010141330A1 (en) 2009-06-02 2010-12-09 Boehringer Ingelheim International Gmbh DERIVATIVES OF 6,7-DIHYDRO-5H-IMIDAZO[1,2-a]IMIDAZOLE-3-CARBOXYLIC ACID AMIDES
TW201103941A (en) * 2009-06-10 2011-02-01 Janssen Pharmaceutica Nv Benzimidazole derivatives useful as TRPM8 channel modulators
CA2769512C (en) 2009-07-29 2019-07-09 Duke University Compositions comprising fp receptor antagonists and their use for inhibiting hair growth
DE102009028929A1 (de) 2009-08-27 2011-07-07 Bayer Schering Pharma Aktiengesellschaft, 13353 Heterocyclisch-substituierte 2-Acetamido-5-Aryl-1,2,4-triazolone und deren Verwendung
UY32940A (es) 2009-10-27 2011-05-31 Bayer Cropscience Ag Amidas sustituidas con halogenoalquilo como insecticidas y acaricidas
CA2786277A1 (en) 2010-01-06 2011-07-14 Joseph P. Errico Methods and compositions of targeted drug development
WO2011094890A1 (en) 2010-02-02 2011-08-11 Argusina Inc. Phenylalanine derivatives and their use as non-peptide glp-1 receptor modulators
US20110212969A1 (en) 2010-02-26 2011-09-01 Millennium Pharmaceuticals, Inc. Substituted hydroxamic acids and uses thereof
TW201211053A (en) 2010-05-10 2012-03-16 Nissan Chemical Ind Ltd Spiro compound and drug for activating adiponectin receptor
WO2011146300A1 (en) 2010-05-17 2011-11-24 Merck Sharp & Dohme Corp. Novel prolylcarboxypeptidase inhibitors
ES2660611T3 (es) 2010-05-27 2018-03-23 Bayer Cropscience Ag Derivados de ácido piridinilcarboxílico como fungicidas
JP2013540145A (ja) 2010-10-21 2013-10-31 ウニベルシテート デス ザールランデス コルチゾール依存性疾患の治療用の選択的ｃｙｐ１１ｂ１阻害剤
CN103201279A (zh) 2010-11-05 2013-07-10 赛诺米克斯公司 作为trpm8的调节剂有用的化合物
RS63320B1 (sr) 2010-12-08 2022-07-29 The U S A As Represented By The Secretary Department Of Health And Human Services Supstituisani pirazolopirimidini kao aktivatori glukocerebrozidaze
US20140088187A1 (en) 2010-12-14 2014-03-27 Beth Israel Deaconess Medical Center Androgen receptor inhibitors and methods of use thereof
PT2652025T (pt) 2010-12-15 2018-11-02 Ppg Europe B V Composição secante e a sua utilização
US20130324522A1 (en) 2010-12-17 2013-12-05 The Rockefeller University Insect odorant receptor antagonists
WO2012118850A1 (en) 2011-02-28 2012-09-07 Array Biopharma Inc. Serine/threonine kinase inhibitors
WO2012120398A1 (en) 2011-03-04 2012-09-13 Pfizer Limited Aryl substituted carboxamide derivatives as trpm8 modulators
WO2012177896A1 (en) 2011-06-24 2012-12-27 Amgen Inc. Trpm8 antagonists and their use in treatments

Also Published As

Publication number Publication date
KR20140045507A (ko) 2014-04-16
AU2012272895B2 (en) 2015-01-22
MX2013015274A (es) 2014-03-31
EP2723717A2 (en) 2014-04-30
US9096527B2 (en) 2015-08-04
CO6852073A2 (es) 2014-01-30
EA201490152A1 (ru) 2014-05-30
UY34160A (es) 2012-08-31
TW201311643A (zh) 2013-03-16
PE20140868A1 (es) 2014-07-18
MY157429A (en) 2016-06-15
CN103906733A (zh) 2014-07-02
MA35271B1 (fr) 2014-07-03
BR112013033316A2 (pt) 2017-01-31
CR20140037A (es) 2014-03-13
AU2012272895A1 (en) 2013-04-11
US20140171639A1 (en) 2014-06-19
CL2013003715A1 (es) 2014-06-27
CA2839699A1 (en) 2012-12-27
US20130157996A1 (en) 2013-06-20
US8710043B2 (en) 2014-04-29
TN2013000529A1 (en) 2015-03-30
WO2012177893A2 (en) 2012-12-27
AP2013007331A0 (en) 2013-12-31
JP2014527511A (ja) 2014-10-16
PH12013502611A1 (en) 2014-04-28
TWI448454B (zh) 2014-08-11
US20140171406A1 (en) 2014-06-19
WO2012177893A3 (en) 2013-06-13
TW201429948A (zh) 2014-08-01

Similar Documents

Publication Publication Date Title
AR086750A1 (es) Ligandos del receptor trpm8 y su uso en diversos tratamientos
AR094668A1 (es) Amidas como moduladores de canales de sodio
AR121016A2 (es) Sales de fenotiazindiaminio y su uso
AR095192A1 (es) Quinolina y quinazolinamidas como modulares de canales de sodio
AR102361A1 (es) Compuestos de metil-quinolina útiles para inhibir la sintasa-1 de prostaglandina microsomal e2
AR107032A1 (es) Inhibidores bicíclicos de pad4
MX383051B (es) Compuestos que inhiben eif4a y métodos relacionados a los mismos.
AR107694A1 (es) Heteroarilos inhibidores de pad4
AR086817A1 (es) Compuestos inhibidores de la fosfodiesterasa tipo 10a
AR099228A1 (es) Inhibidores macrocíclicos de fxia que tienen grupos heterocíclicos
AR092064A1 (es) Derivados de cromano como inhibidores del receptor transitorio potencial de la melastatina 8 (trpm8)
AR093759A1 (es) Dihidropiridona p1 como inhibidores del factor xia
AR106652A1 (es) Compuestos para tratar la esclerosis lateral amiotrófica
AR094929A1 (es) Derivados de fenilpirazol como inhibidores potentes de rock1 y rock2
CL2013002690A1 (es) Compuestos derivados de bis(fluoroalquil)-1,4-benzodiazepinona, inhibidores de notch; compuesto cristalino; composicion farmaceutica que los comprende; combinacion farmaceutica; y su uso para el tratamiento del cancer.
AR106806A1 (es) Inhibidores triazol de acc y usos de los mismos
AR083676A1 (es) Compuestos heterociclicos, útiles como inhibidores de quinasa y composiciones farmaceuticas que los contienen
AR107030A1 (es) Inhibidores aza-bencimidazol de pad4
AR089944A1 (es) Derivados de tetrahidro-quinazolinona
AR103170A1 (es) Compuestos y composiciones farmacéuticas de los mismos para el tratamiento de desordenes inflamatorios y osteoartritis
AR097325A1 (es) Pirroles anillados
AR097199A1 (es) Inhibidores de rorc2 y sus métodos de uso
AR093581A1 (es) Antibioticos macrociclicos de amplio espectro
EA201690135A1 (ru) Трициклические соединения бензоксаборола и их применение
CO2017008816A2 (es) Compuestos de benzoxaborol y usos de los mismos

Legal Events

Date Code Title Description
FA Abandonment or withdrawal