[go: up one dir, main page]
More Web Proxy on the site http://driver.im/

ES2613538T3 - Derivados de arilamida como bloqueadores de TTX-S - Google Patents

Derivados de arilamida como bloqueadores de TTX-S Download PDF

Info

Publication number
ES2613538T3
ES2613538T3 ES11834032T ES11834032T ES2613538T3 ES 2613538 T3 ES2613538 T3 ES 2613538T3 ES 11834032 T ES11834032 T ES 11834032T ES 11834032 T ES11834032 T ES 11834032T ES 2613538 T3 ES2613538 T3 ES 2613538T3
Authority
ES
Spain
Prior art keywords
independently selected
alkyl
substituted
unsubstituted
substituents independently
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Active
Application number
ES11834032T
Other languages
English (en)
Inventor
Tatsuya Yamagishi
Kiyoshi Kawamura
Yoshimasa Arano
Mikio Morita
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Raqualia Pharma Inc
Original Assignee
Raqualia Pharma 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 Raqualia Pharma Inc filed Critical Raqualia Pharma Inc
Application granted granted Critical
Publication of ES2613538T3 publication Critical patent/ES2613538T3/es
Active legal-status Critical Current
Anticipated expiration legal-status Critical

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
    • C07D213/62—Oxygen or sulfur atoms
    • C07D213/63—One oxygen atom
    • C07D213/64—One oxygen atom attached in position 2 or 6
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/18—Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • 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
    • 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
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/06—Antimigraine agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/08—Antiepileptics; Anticonvulsants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/22—Anxiolytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/24—Antidepressants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • 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
    • 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
    • A61P5/00—Drugs for disorders of the endocrine 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
    • A61P9/06—Antiarrhythmics
    • 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
    • C07D213/72—Nitrogen atoms
    • C07D213/75—Amino or imino radicals, acylated by carboxylic or carbonic acids, or by sulfur or nitrogen analogues thereof, e.g. carbamates
    • 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
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more 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, directly attached to ring carbon atoms
    • C07D239/32—One oxygen, sulfur or nitrogen atom
    • C07D239/42—One nitrogen atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—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
    • 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
    • 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
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12—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
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
    • 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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Cardiology (AREA)
  • Psychiatry (AREA)
  • Endocrinology (AREA)
  • Urology & Nephrology (AREA)
  • Immunology (AREA)
  • Psychology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Diabetes (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Pyridine Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

Un compuesto de la siguiente fórmula (II)**Fórmula** en la que R1 se selecciona independientemente entre el grupo que consiste en -CF3, -CHF2, -OCF3, - OCHF2, -OCH2CHF2, -OCH2CF3, -OCF2CHF2, -OCF2CF3, -OCH2CH2CF3, - OCH(CH3)CF3, -OCH2C(CH3)F2, -OCH2CF2CHF2, - OCH2CF2CF3, -OCH2CH2OCH2CF3, - NHCH2CF3, -SCF3, -SCH2CF3, -CH2CF3, 10 -CH2CH2CF3, -CH2OCH2CF3 y - OCH2CH2OCF3; R2 se selecciona independientemente entre el grupo que consiste en: (1) hidrógeno, (2) halógeno, (3) hidroxilo, (4) -On-alquilo C1-6, donde el alquilo está sin sustituir o sustituido con uno o más sustituyentes seleccionados independientemente entre R5, (5) -On-cicloalquilo C3-6, donde el cicloalquilo está sin sustituir o sustituido con uno o más sustituyentes seleccionados independientemente entre R5, (6) - On-alquenilo C2-4, donde el alquenilo está sin sustituir o sustituido con uno o más sustituyentes seleccionados independientemente entre R5, (7) -On-fenilo o -On-naftilo, donde el fenilo o el naftilo está sin sustituir o sustituido con uno o más sustituyentes seleccionados independientemente entre R5, (8) -On-grupo heterocíclico, donde el grupo heterocíclico está sin sustituir o sustituido con uno o más sustituyentes seleccionados independientemente entre R5, (9) -(C>=O)-NR7R8, (10) -NR7R8, (11) -S(O)2-NR7R8, (12) -NR7- S(O)2R8, (13) -S(O)t-R7, donde t es 0, 1 o 2, (14) - NR7(C>=O)R8, (15) -CN y (16) -NO2; en la que n es 0 o 1, cuando n es 0, está presente un enlace químico en el lugar de -On-; p es 1, 2, 3 o 4; cuando p es dos o más de dos, R2 puede ser igual o diferente; R3 y R4 son independientemente hidrógeno o alquilo C1-6 que está sin sustituir o sustituido con uno o más sustituyentes seleccionados independientemente entre halógeno, hidroxilo y -O-alquilo C1-6, ni R3 ni R4 son alquilo C1-6 al mismo tiempo. R5 se selecciona entre el grupo que consiste en: (1) hidrógeno, (2) halógeno, (3) hidroxilo, (4) -(C>=O)m-Ol-alquilo C1-6, donde el alquilo está sin sustituir o sustituido con uno o más sustituyentes seleccionados independientemente entre R6, (5) -Ol-perfluoroalquilo (C1-3), (6) -(C>=O)m-Ol-cicloalquilo C3-6, donde el cicloalquilo está sin sustituir o sustituido con uno o más sustituyentes seleccionados independientemente entre R6, (7) -(C>=O)m-Ol-alquenilo C2-4, donde el alquenilo está sin sustituir o sustituido con uno o más sustituyentes seleccionados independientemente entre R6, (8) - (C>=O)m-Ol-fenilo o -(C>=O)m-Ol-naftilo, donde el fenilo o el naftilo está sin sustituir o sustituido con uno o más sustituyentes seleccionados independientemente entre R6, (9) -(C>=O)m-Ol-grupo heterocíclico, donde el grupo heterocíclico está sin sustituir o sustituido con uno o más sustituyentes seleccionados independientemente entre R6, (10) -(C>=O)-NR7R8, (11) -NR7R8, (12) -S(O)2-NR7R8, (13) -S(O)t-R7, donde t es 0, 1 o 2, (14) -CO2H, (15) -CN y (16) -NO2; en la que I es 0 o 1 y m es 0 o 1; cuando I es 0 o m es 0, está presente un enlace químico en el lugar de -Ol- o -(C>=O)m- y cuando I es 0 y m es 0, está presente un enlace químico en el lugar de - (C>=O)m-Ol-; R6 se selecciona independientemente entre el grupo que consiste en: (1) hidrógeno, (2) hidroxilo, (3) halógeno, (4) -alquilo C1-6, (5) -cicloalquilo C3-6, (6) - O-alquilo C1-6, (7) - O(C>=O)-alquilo C1-6, (8) -NH-alquilo C1-6, (9) fenilo, (10) grupo heterocíclico y (11) -CN; R7 y R8 son independientemente hidrógeno, alquilo C1-6, alquenilo C2-6, cicloalquilo C3-7 o arilo, que está sin sustituir o sustituido con uno o más sustituyentes seleccionados independientemente entre halógeno, hidroxilo, alquilo C1-6 y -O-alquilo C1-6; o R7 forman un anillo de 4 a 7 miembros con R8 que puede contener un átomo de nitrógeno, un átomo de oxígeno, un átomo de azufre o un doble enlace, en la que el anillo de 4 a 7 miembros está opcionalmente sustituido con 1 a 6 sustituyentes seleccionados independientemente entre el grupo que consiste en: (1) hidrógeno, (2) hidroxilo, (3) halógeno, (4) alquilo C1-6, que está sin sustituir o sustituido con uno o más sustituyentes seleccionados independientemente entre R6, (5) cicloalquilo C3-6, que está sin sustituir o sustituido con uno o más sustituyentes seleccionados independientemente entre R6, (6) -O-alquilo C1-6, que está sin sustituir o sustituido con uno o más sustituyentes seleccionados independientemente entre R6, y (7) -Ocicloalquilo C3-6, que está sin sustituir o sustituido con uno o más sustituyentes seleccionados independientemente entre R6; X es un átomo de nitrógeno o un átomo de carbono; Z es un átomo de nitrógeno o un átomo de carbono; Y es hidrógeno o alquilo C1-6; R9 se selecciona independientemente entre el grupo que consiste en: (1) hidrógeno, (2) halógeno, (3) -On-alquilo C1-6, donde el alquilo está sin sustituir o sustituido con uno o más sustituyentes seleccionados independientemente entre R5, (4) - On-cicloalquilo C3-6, donde el cicloalquilo está sin sustituir o sustituido con uno o más sustituyentes seleccionados independientemente entre R5 y (5) -Onalquenilo C2-4, donde el alquenilo está sin sustituir o sustituido con uno o más sustituyentes seleccionados independientemente entre R5; en la que n es 0 o 1, cuando n es 0, está presente un enlace químico en el lugar de -On-; q es 1, 2 o 3; cuando q es dos o más de dos, R9 puede ser igual o diferente; R10 es independientemente hidrógeno, alquilo C1-6, alquenilo C2-6 o cicloalquilo C3-7, que está sin sustituir o sustituido con uno o más sustituyentes seleccionados independientemente entre halógeno, hidroxilo, alquilo C1-6, -O-alquilo C1-6, -cicloalquilo C3-7 y -O-cicloalquilo C3-7; o una sal farmacéuticamente aceptable del mismo.
ES11834032T 2010-10-18 2011-10-18 Derivados de arilamida como bloqueadores de TTX-S Active ES2613538T3 (es)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US39401710P 2010-10-18 2010-10-18
US41800210P 2010-11-30 2010-11-30
US201161522792P 2011-08-12 2011-08-12
PCT/JP2011/005802 WO2012053186A1 (en) 2010-10-18 2011-10-18 Arylamide derivatives as ttx-s blockers

Publications (1)

Publication Number Publication Date
ES2613538T3 true ES2613538T3 (es) 2017-05-24

Family

ID=45974916

Family Applications (1)

Application Number Title Priority Date Filing Date
ES11834032T Active ES2613538T3 (es) 2010-10-18 2011-10-18 Derivados de arilamida como bloqueadores de TTX-S

Country Status (12)

Country Link
US (1) US9302991B2 (es)
EP (1) EP2630122B1 (es)
JP (2) JP2013543480A (es)
KR (1) KR101458006B1 (es)
CN (2) CN103249721B (es)
BR (1) BR112013009365B1 (es)
CA (1) CA2813708C (es)
ES (1) ES2613538T3 (es)
MX (1) MX2013004307A (es)
RU (1) RU2535671C1 (es)
TW (1) TWI546286B (es)
WO (1) WO2012053186A1 (es)

Families Citing this family (23)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
RU2535671C1 (ru) * 2010-10-18 2014-12-20 Раквалиа Фарма Инк. Производные ариламидов в качестве блокаторов ttx-s
MX2014001862A (es) * 2011-09-12 2014-05-30 Hoffmann La Roche 5-cicloalquil-o 5-heterociclil-nicotinamidas.
WO2013161308A1 (en) * 2012-04-25 2013-10-31 Raqualia Pharma Inc. Amide derivatives as ttx-s blockers
CN104520296B (zh) * 2012-04-25 2016-11-16 拉夸里亚创药株式会社 作为ttx-s阻断剂的吡咯并吡啶酮衍生物
CA2887887C (en) 2012-10-31 2020-08-25 Raqualia Pharma Inc. Pyrazolopyridine derivatives as ttx-s blockers
US9452986B2 (en) * 2014-02-06 2016-09-27 Abbvie Inc. 6-heteroaryloxy- or 6-aryloxy-quinoline-2-carboxamides and method of use
CA3090492C (en) * 2015-10-07 2023-02-14 Arizona Board Of Regents On Behalf Of The University Of Arizona Crmp2 sumoylation inhibitors and uses thereof
US12084472B2 (en) 2015-12-18 2024-09-10 Ardelyx, Inc. Substituted 4-phenyl pyridine compounds as non-systemic TGR5 agonists
TWI773657B (zh) 2015-12-18 2022-08-11 美商亞德利克斯公司 作爲非全身ｔｇｒ５促效劑之經取代之4-苯基吡啶化合物
CA3228632A1 (en) * 2015-12-24 2017-06-29 Kyowa Kirin Co., Ltd. .alpha.,.beta.-unsaturated amide compound
CN106083813A (zh) * 2016-06-13 2016-11-09 太原理工大学 一种三唑‑喹啉类化合物的合成方法
US11046683B2 (en) 2016-12-15 2021-06-29 Ono Pharmaceutical Co., Ltd. Activator of TREK (TWIK RElated K+ channels) channels
WO2018175449A1 (en) 2017-03-21 2018-09-27 AbbVie Deutschland GmbH & Co. KG Proline amide compounds and their azetidine analogues carrying a specifically substituted benzyl radical
TWI769266B (zh) * 2017-06-20 2022-07-01 日商拉夸里亞創藥股份有限公司 作為Nav1.7及Nav1.8阻斷劑之醯胺衍生物
CN111132961A (zh) 2017-08-31 2020-05-08 拉夸里亚创药株式会社 作为ttx-s阻断剂的双芳氧基衍生物
DK3919486T3 (da) 2018-04-25 2023-09-04 Bayer Ag Hidtil ukendte heteroaryl-triazol- og heteroaryl-tetrazolforbindelser som pesticider
RU2761824C2 (ru) * 2018-08-03 2021-12-13 Закрытое Акционерное Общество "Биокад" Ингибиторы CDK8/19
CA3117927A1 (en) * 2018-11-02 2020-05-07 Merck Sharp & Dohme Corp. 2-amino-n-heteroaryl-nicotinamides as nav1.8 inhibitors
JP7413346B2 (ja) 2019-03-06 2024-01-15 第一三共株式会社 ピロロピラゾール誘導体
AR119009A1 (es) * 2019-05-29 2021-11-17 Syngenta Crop Protection Ag Derivados de alcoxipiridina y alcoxipirimidina microbicidas
GB201908453D0 (en) * 2019-06-12 2019-07-24 Enterprise Therapeutics Ltd Compounds for treating respiratory disease
KR20240024935A (ko) 2021-06-18 2024-02-26 알리고스 테라퓨틱스 인코포레이티드 Pd-l1을 표적화하기 위한 방법 및 조성물
WO2024059207A2 (en) * 2022-09-15 2024-03-21 Vanderbilt University Pyrazoloether analogs as mglu5 negative allosteric modulators and methods of making and using the same

Family Cites Families (25)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPH0725853A (ja) * 1993-07-14 1995-01-27 Ishihara Sangyo Kaisha Ltd アミド系化合物又はその塩、それらの製造方法及びそれらを含有する有害動物防除剤
GB9919588D0 (en) 1999-08-18 1999-10-20 Hoechst Schering Agrevo Gmbh Fungicidal compounds
BR0114122A (pt) 2000-09-18 2003-07-01 Du Pont Composto, composições fungicidas e método de controle de doenças vegetais causadas por patógenos vegetais fúngicos
CN1688546A (zh) * 2000-09-18 2005-10-26 纳幕尔杜邦公司 用作杀真菌剂的吡啶酰胺类和吡啶酰亚胺类
ATE455104T1 (de) * 2001-11-01 2010-01-15 Icagen Inc Pyrazolamide zur anwendung in der behandlung von schmerz
TW200306159A (en) 2002-03-19 2003-11-16 Du Pont Bicyclic fused pyridinyl amides and advantageous compositions thereof for use as fungicides
TW200306782A (en) 2002-03-19 2003-12-01 Du Pont Pyridinyl amides and advantageous compositions thereof for use as fungicides
TW200407075A (en) * 2002-03-19 2004-05-16 Du Pont Pyridinyl amides and advantageous compositions thereof for use as fungicides
JP4706482B2 (ja) 2004-01-13 2011-06-22 株式会社クレハ ２，６−ジクロロイソニコチン酸ピリジルメチル誘導体、その製造方法および農園芸用病害防除剤
WO2005070889A1 (en) 2004-01-23 2005-08-04 E.I. Dupont De Nemours And Company Herbicidal amides
DE102004022897A1 (de) 2004-05-10 2005-12-08 Bayer Cropscience Ag Azinyl-imidazoazine
US7507748B2 (en) * 2004-07-22 2009-03-24 Amgen Inc. Substituted aryl-amine derivatives and methods of use
US20070155738A1 (en) * 2005-05-20 2007-07-05 Alantos Pharmaceuticals, Inc. Heterobicyclic metalloprotease inhibitors
JP2007186435A (ja) 2006-01-12 2007-07-26 Astellas Pharma Inc ニコチンアミド誘導体
JP5361857B2 (ja) * 2007-03-23 2013-12-04 ファイザー・リミテッド イオンチャネルの阻害剤
GEP20125379B (en) * 2007-05-03 2012-01-10 Pfizer Ltd 2 -pyridine carboxamide derivatives as sodium channel modulators
AU2008319309B2 (en) * 2007-10-31 2012-09-06 Merck Sharp & Dohme Llc P2X3 receptor antagonists for treatment of pain
WO2009117269A1 (en) * 2008-03-18 2009-09-24 Merck & Co., Inc. Substituted 4-hydroxypyrimidine-5-carboxamides
TW201000446A (en) 2008-05-30 2010-01-01 Astrazeneca Ab New compounds useful in pain therapy
PE20110136A1 (es) 2008-06-27 2011-03-17 Novartis Ag Compuestos organicos
WO2010035166A1 (en) * 2008-09-23 2010-04-01 Pfizer Limited Benzamide derivatives
CN102271682B (zh) * 2008-10-31 2015-12-16 默沙东公司 用于治疗疼痛的p2x3受体拮抗剂
WO2010137351A1 (en) 2009-05-29 2010-12-02 Raqualia Pharma Inc. Aryl substituted carboxamide derivatives as calcium or sodium channel blockers
US8809380B2 (en) * 2009-08-04 2014-08-19 Raqualia Pharma Inc. Picolinamide derivatives as TTX-S blockers
RU2535671C1 (ru) * 2010-10-18 2014-12-20 Раквалиа Фарма Инк. Производные ариламидов в качестве блокаторов ttx-s

Also Published As

Publication number Publication date
MX2013004307A (es) 2013-07-17
CN106478497B (zh) 2020-05-08
CN106478497A (zh) 2017-03-08
JP2013543480A (ja) 2013-12-05
CA2813708A1 (en) 2012-04-26
RU2013122632A (ru) 2014-11-27
CN103249721A (zh) 2013-08-14
CN103249721B (zh) 2016-10-12
WO2012053186A1 (en) 2012-04-26
EP2630122A4 (en) 2014-04-30
BR112013009365A2 (pt) 2016-07-26
US9302991B2 (en) 2016-04-05
CA2813708C (en) 2019-09-17
JP2014177450A (ja) 2014-09-25
KR101458006B1 (ko) 2014-11-04
JP5581482B1 (ja) 2014-09-03
BR112013009365B1 (pt) 2021-10-26
EP2630122B1 (en) 2016-11-30
US20140336377A1 (en) 2014-11-13
TW201240968A (en) 2012-10-16
TWI546286B (zh) 2016-08-21
KR20130112896A (ko) 2013-10-14
EP2630122A1 (en) 2013-08-28
RU2535671C1 (ru) 2014-12-20

Similar Documents

Publication Publication Date Title
ES2613538T3 (es) Derivados de arilamida como bloqueadores de TTX-S
AR080314A1 (es) Derivado de 1,3,4,8-tetrahidro-2h-pirido (1,2-a) pirazina y su uso como inhibidor de la hiv integrasa
ES2531274T3 (es) Indazoles sustituidos con oxazol como inhibidores de PI3-cinasas
ES2600636T3 (es) Spiro-[1,3]-oxazinas y spiro-[1,4]-oxazepinas como inhibidores de BACE1 y/o BACE2
CO6321244A2 (es) Pirrolopiridinas como inhibidores de cinasa
PE20130155A1 (es) Derivados de ariletinilo
AR091519A1 (es) Inhibidores pirrolopirazona de tanquirasa
AR082519A1 (es) Fenilamidinas que tienen alta actividad fungicida, y su utilizacion
ES2626801T3 (es) Compuestos de triazolopiridina como inhibidores de pde10a
ES2561105T3 (es) Derivado heterocíclico como inhibidor de prostaglandina E sintasa microsómica (mPGES)
AR052568A1 (es) Derivados de pirazolo -pirimidina como antagonstas de mglur2
ES2618003T3 (es) Compuestos tricíclicos sustituidos como inhibidores de FGFR
AR085615A1 (es) Derivados de fluoropiridinona utiles como agentes antibacterianos y composiciones farmaceuticas que los contienen
AR118706A2 (es) Compuesto para el control de plagas y vegetación no deseada, procedimiento para prepararlo, composición que lo comprende, y compuesto intermediario relacionado
AR066107A1 (es) Derivados de triazolopiridin - carboxamidas y triazolopirimidin-carboxamidas, su preparacion y su aplicacion en terapeutica como inhibidores de la enzimamonoacil glicerol lipasa y composiciones qu los contienen.
AR069740A1 (es) Compuestos nucleosidos antivirales
CO6150181A2 (es) Compuesto 6-(bencilo sustituido con heterociclo)-4-oxoquinolina y su uso como inhibidor de integrasa vih
AR087148A1 (es) Imidazopiridazinas
AR087274A1 (es) Derivados de amidas heterociclicas como antagonistas de receptores p2x7
AR111682A1 (es) Derivados de imidazopirimidina con sustituyentes fenilo y piridilo que contienen azufre
ES2650372T3 (es) Compuestos tricíclicos como inhibidores de CFTR
CO6400145A2 (es) Derivados de 2-piridin-2-il pirazol-3(2h) -ona, su preparción y su aplicación terapeútica
AR088816A1 (es) Proceso para preparar derivados de 1-acil-4-fenilsulfonilprolinamida y compuestos intermediarios
AR111672A1 (es) Derivados heterocíclicos con sustituyentes que contienen azufre activos como plaguicidas
AR063357A1 (es) Derivados de pirimidinas como inhibidores de mapk/erk quinasa. procesos de obtencion y composiciones farmaceuticas.