DK2686302T3 - Sulfonamidforbindelser med TRPM8-antagonistisk aktivitet - Google Patents

Sulfonamidforbindelser med TRPM8-antagonistisk aktivitet Download PDF

Info

Publication number
DK2686302T3
DK2686302T3 DK12712777.7T DK12712777T DK2686302T3 DK 2686302 T3 DK2686302 T3 DK 2686302T3 DK 12712777 T DK12712777 T DK 12712777T DK 2686302 T3 DK2686302 T3 DK 2686302T3
Authority
DK
Denmark
Prior art keywords
compound
sulfonyl
amino
optionally substituted
halogen
Prior art date
Application number
DK12712777.7T
Other languages
English (en)
Inventor
Yasuyuki Tsuzuki
Daisuke Sawamoto
Toshiaki Sakamoto
Taku Kato
yasuki Niwa
Nobumasa Awai
Original Assignee
Mitsubishi Tanabe Pharma Corp
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 Mitsubishi Tanabe Pharma Corp filed Critical Mitsubishi Tanabe Pharma Corp
Application granted granted Critical
Publication of DK2686302T3 publication Critical patent/DK2686302T3/da

Links

Classifications

    • 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
    • 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
    • A61P1/12—Antidiarrhoeals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/08—Drugs for disorders of the urinary system of the prostate
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/10—Drugs for disorders of the urinary system of the bladder
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/04—Antipruritics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • 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
    • A61P25/06—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
    • A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • 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
    • A61P35/00—Antineoplastic 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
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/12—Antihypertensives
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms 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
    • C07D215/38—Nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D217/00—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems
    • C07D217/22—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems 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 carbon atoms of the nitrogen-containing ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • 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
    • 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

Landscapes

  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Medicinal Chemistry (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Urology & Nephrology (AREA)
  • Pain & Pain Management (AREA)
  • Pulmonology (AREA)
  • Dermatology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Psychiatry (AREA)
  • Vascular Medicine (AREA)
  • Rheumatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Quinoline Compounds (AREA)
  • Other In-Based Heterocyclic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Claims (16)

1. Forbindelse "f r~'----1-------"" *----'
omatisk heterocyclus bestående af pyridin kondenseret med benzen, én af Y og Z er CR2d, og den anden er en kemisk binding, I0 ringen B er (a) monocyclisk eller bicyclisk aromatisk kulbrinte med 6 til 11 carbonatomer som et ringatom; (b) monocyclisk eller bicyclisk alicyclisk kulbrinte med 3 til 12 carbonatomer som ringatom; (c) 5- til 11 -leddet monocyclisk eller bicyclisk aromatisk heterocyclus indeholdende carbonatomer og 1 til 4 heteroatomer valgt blandt oxygenatom, svovlatom og nitrogenatom; eller (d) 4- til 12-leddet monocyclisk eller bicyclisk 15 ikke-aromatisk heterocyclus indeholdende carbonatomer og 1 til 4 heteroatomer valgt blandt oxygenatom, svovlatom og nitrogenatom, ring C er (a) benzen; eller (b) 5- til 6-leddet monocyclisk aromatisk heterocyclus indeholdende carbonatomer og 1 til 4 heteroatomer valgt blandt oxygenatom, svovlatom og nitrogenatom, >0 R1 er (a) hydrogen; (b) Ci-Cealkyl, som eventuelt kan være substitueret med 1 til 7 grupper valgt blandt C3-C7cycloalkyl, Ci-Cealkoxy, halogen, oxo og hydroxy; (c) C3-C7cycloalkyl, som eventuelt kan være substitueret med 1 til 7 grupper valgt blandt Ci-C6alkyl, Ci-C6alkoxy og halogen; (d) Ci-C6alkoxy, som eventuelt kan være substitueret med 1 til 7 grupper valgt blandt C3-C7cycloalkyl, Ci-C6alkoxy, halogen og 15 hydroxy; (e) phenyl, som eventuelt kan være substitueret med 1 til 3 grupper valgt blandt Ci-C6alkyl, Ci-Cehalogenalkyl, C3-C7cycloalkyl, C3-C7halogencycloalkyl, Ci-C6alkoxy, Ci-Cehalogenalkoxy og halogen; (f) halogen; eller (g) nitril, R2a, R2b, R2c og R2d er hver især uafhængigt (a) hydrogen; (b) Ci-Cealkyl, som eventuelt kan være substitueret med 1 til 7 grupper valgt blandt Ci-C6alkoxy, C3-C7cycloalkyl, 50 halogen, oxo og hydroxy; (c) C3-C7cycloalkyl, som eventuelt kan være substitueret med 1 til 7 grupper valgt blandt Ci-Cealkyl, Ci-Cealkoxy og halogen; (d) Ci-Cealkoxy, som eventuelt kan være substitueret med 1 til 7 grupper valgt blandt CrCealkoxy, C3-C7cycloalkyl og halogen; (e) phenyl, som eventuelt kan være substitueret med 1 til 3 grupper valgt blandt CrCealkyl, CrCehalogenalkyl, C3-C7cycloalkyl, C3-C7halogen-cycloalkyl, CrCealkoxy, CrCehalogenalkoxy og halogen; (f) 5- til 6-leddet monocyclisk aromatisk heterocyclisk gruppe, som eventuelt kan være substitueret med 1 til 3 grupper valgt blandt CrCealkyl, CrCehalogenalkyl, C3-C7cycloalkyl, C3-C7halogencycloalkyl, CrCealkoxy, CrCehalogenalkoxy og halogen; (g) 4- til 7-leddet monocyclisk ikke-aromatisk heterocyclisk gruppe, som eventuelt kan være substitueret med 1 til 3 grupper valgt blandt CrCealkyl, CrCehalogenalkyl, C3-C7cycloalkyl, C3-C7halogencycloalkyl, CrCealkoxy, CrCehalogenalkoxy og halogen; (h) halogen; eller (i) nitril, R3a, R3b, R3c og R3d er hver især uafhængigt (a) hydrogen; (b) CrCealkyl, som eventuelt kan være substitueret med 1 til 7 grupper valgt blandt C3-C7cycloalkyl, C3-C7halogen-cycloalkyl (hvori cycloalkylet og halogencycloalkylet hver især uafhængigt eventuelt kan være substituerede med 1 til 3 grupper valgt blandt CrCealkyl og CrCehalogenalkyl), CrCealkoxy, CrCehalogenalkoxy, phenyl, 5- til 6-leddet monocyclisk aromatisk heterocyclisk gruppe, 4- til 7-leddet monocyclisk ikke-aromatisk heterocyclisk gruppe (hvori phenylet, den aromatiske heterocycliske gruppe og den ikke-aromatiske heterocycliske gruppe hver især uafhængigt eventuelt kan være substituerede med 1 til 3 grupper valgt blandt CrCealkyl, CrCehalogenalkyl, C3-C7cycloalkyl, C3-C7halogen-cycloalkyl, CrCealkoxy, CrCehalogenalkoxy og halogen), halogen, oxo og hydroxy; (c) C3-C7cycloalkyl, som eventuelt kan være substitueret med 1 til 7 grupper valgt blandt CrCealkyl, CrCehalogenalkyl, CrCealkoxy, CrCehalogenalkoxy, halogen og hydroxy; (d) CrCealkoxy, som eventuelt kan være substitueret med 1 til 7 grupper valgt blandt C3-C7cycloalkyl, C3-C7halogencycloalkyl (hvori cycloalkylet og halogencycloalkylet hver især uafhængigt eventuelt kan være substituerede med 1 til 3 grupper valgt blandt CrCealkyl og CrCehalogenalkyl), CrCealkoxy, CrCehalogenalkoxy, phenyl, 5- til 6-leddet monocyclisk aromatisk heterocyclisk gruppe, 4- til 7-leddet monocyclisk ikke-aromatisk heterocyclisk gruppe (hvori phenylet, den aromatiske heterocycliske gruppe og den ikke-aromatiske heterocycliske gruppe hver især uafhængigt eventuelt kan være substituerede med 1 til 3 grupper valgt blandt CrCealkyl, CrCehalogenalkyl, C3-C7cycloalkyl, C3-C7halogencycloalkyl, CrCealkoxy, CrCehalogenalkoxy og halogen), halogen og hydroxy; (e) C3-C7cycloalkoxy, som eventuelt kan være substitueret med 1 til 7 grupper valgt blandt CrCealkyl, CrCehalogenalkyl, CrCealkoxy, CrCehalogenalkoxy, halogen og hydroxy; (f) phenyl, som eventuelt kan være substitueret med 1 til 3 grupper valgt blandt CrCealkyl, CrCehalogenalkyl, C3-C7cycloalkyl, C3-C7halogencycloalkyl, CrCealkoxy, CrCehalogenalkoxy og halogen; (g) 5- til 6-leddet monocyclisk aromatisk heterocyclisk gruppe som eventuelt kan være substitueret med 1 til 3 grupper valgt blandt Ci-Cealkyl, CrCehalogenalkyl, C3-C7cycloalkyl, C3-C7halogencycloalkyl, CrCealkoxy, CrCealkoxy og halogen; (h)4- til 7-leddet monocyclisk ikke-aromatisk heterocyclisk gruppe, som eventuelt kan være substitueret med 1 til 3 grupper valgt blandt CrCealkyl, CrCehalogenalkyl, C3-C7cycloalkyl, C3-C7halogencycloalkyl, CrCealkoxy, CrCehalogenalkoxy og halogen; (i) phenoxy, som eventuelt kan være substitueret med 1 til 3 grupper valgt blandt CrCealkyl, CrCehalogenalkyl, C3-C7cycloalkyl, C3-C7halogencycloalkyl, CrCealkoxy, CrCehalogenalkoxy og halogen; (j) halogen; eller (k) hydroxy, eller to substituentgrupper valgt blandt R3a, R3b, R3c og R3d kombinerer indbyrdes for dannelse af oxo, R5 og R6 er hver især uafhængigt (a) hydrogen; (b) CrCealkyl; (c) CrCehalogenalkyl; (d) C3-C7cycloalkyl; eller (e) C3-C7halogencycloalkyl, eller R5 og R6 kombinerer indbyrdes ved deres terminaler med det tilstødende carbonatom for dannelse af 3- til 7-leddet monocyclisk alicyclisk kulbrinte, n er O, 1 eller 2, X er (a) carboxy; (b) CrCealkoxycarbonyl; (c) hydroxy-CrCealkyl; (d) aminocarbonyl, hvor et nitrogenatom eventuelt kan være substitueret med en gruppe valgt blandt CrCealkyl, CrCealkoxy og nitril; eller (e) C2-C7alkanoyl, som eventuelt kan være substitueret med 1 til 3 halogener; eller et farmaceutisk acceptabelt salt deraf.
2. Forbindelse ifølge krav 1, hvor ring C er benzen, og X er carboxy og binder til ring C ved 4-positionen til aminosulfonylenheden, eller et farmaceutisk acceptabelt salt deraf.
3. Forbindelse ifølge krav 2, hvor ring B er (a) monocyclisk eller bicyclisk aromatisk kulbrinte med 6 til 11 carbonatomer som ringatom; eller (b) 5- til 11-leddet monocyclisk eller bicyclisk aromatisk heterocyclus indeholdende carbonatomer og 1 til 4 hetero-atomer valgt blandt oxygenatom, svovlatom og nitrogenatom, og n er O eller 1, eller et farmaceutisk acceptabelt salt deraf.
4. Forbindelse ifølge krav 2, hvor ring B er (a) monocyclisk aromatisk kulbrinte med 6 til 11 carbonatomer som ringatom; eller (b) 5- til 11-leddet monocyclisk aromatisk heterocyclus indeholdende carbonatomer og 1 til 4 heteroatomer valgt blandt oxygenatom, svovlatom og nitrogenatom, og n er 1, eller et farmaceutisk acceptabelt salt deraf.
5. Forbindelse ifølae enten krav 3 eller 4, hvor en delstruktur:
5 er en gruppe af følgende formel (A):
eller et farmaceutisk acceptabelt salt deraf. 0
6. Forbindelse ifølge enten krav 4 eller 5, hvor en delstruktur:
5 er en gruppe af følgende formel (B):
eller et farmaceutisk acceptabelt salt deraf. 0
7. Forbindelse ifølge krav 5, hvor R1 er (a) Ci-C6alkyl, som eventuelt kan være substitueret med 1 til 7 halogener; (b) Cs-Czcycloalkyl; (c) Ci-C6alkoxy; eller (d) halogen, R2a, R2b og R2c er hydrogen, R2d er (a) hydrogen; (b) Ci-C6alkyl. som eventuelt kan være substitueret med 1 til 7 5 halogener; (c) C3-C7cycloalkyl; eller (d) Ci-C6alkoxy, R3a og R3b er hver især uafhængigt (a) hydrogen; (b) CrCealkyl, som eventuelt kan være substitueret med 1 til 7 grupper valgt blandt C3-C7cycloalkyl (hvori cycloalkylet eventuelt kan være substitueret med 1 til 3 grupper valgt blandt CrCealkyl og Ci-C6halogenalkyl), CrCealkoxy, Ci-Cehalogenalkoxy, og halogen; (c) C3-C7cycloalkyl, som eventuelt kan være substitueret med 1 til 7 grupper valgt blandt Ci-Cealkyl, Ci-Cehalogenalkyl, og halogen; (d) CrCealkoxy, som eventuelt kan være substitueret med 1 til 7 grupper valgt blandt C3-C7cycloalkyl, CrCealkoxy, Ci-Cehalogenalkoxy, og halogen; eller (e) halogen, R3c og R3d er hydrogen, R5 og R6 er hydrogen, n er 1, eller et farmaceutisk acceptabelt salt deraf.
8. Forbindelse ifølge krav 7, hvor ring B er benzen eller pyridin, R1 er methyl, triflu orm ethyl, isopropyl, cyclopropyl, eller methoxy, R3a og R3b er hver især uafhængigt (a) hydrogen; (b) Ci-Cealkyl, som eventuelt kan være substitueret med 1 til 7 grupper valgt blandt C3-C7cycloalkyl (hvori cycloalkylet eventuelt kan være substitueret med 1 til 3 grupper valgt blandt Ci-Cealkyl og Ci-Cehalogenalkyl), CrCealkoxy, Ci-Cehalogenalkoxy, og halogen; (c) C3-C7cycloalkyl; (d) CrCealkoxy, som eventuelt kan være substitueret med 1 til 7 halogener; eller (e) halogen, eller et farmaceutisk acceptabelt salt deraf.
9. Forbindelse ifølge krav 1, som er valgt fra gruppen bestående af 4-({(4-methylisoquinolin-3-yl)[4-(trifluormethoxy)benzyl]amino}sulfonyl)benzoesyre; 4-{[[3-fluor-4-(trifluormethoxy)benzyl](4-methylisoquinolin-3-yl)amino]sulfonyl}-benzoesyre; 4-({(1-cyclopropyl-4-methylisoquinolin-3-yl)[4-(trifluormethoxy)benzyl]amino}sulfonyl)- benzoesyre; 4-{[[4-(1-ethoxy-2,2,2-trifluor-1-methylethyl)benzyl](4-methylisoquinolin-3-yl)amino]- sulfonyljbenzoesyre; 4-({(3-methylquinolin-2-yl)[4-(trifluormethoxy)benzyl]amino}sulfonyl)benzoesyre; 4-{[[4-fluor-3-(trifluormethyl)benzyl](3-methylquinolin-2-yl)amino]sulfonyl}benzoesyre; 4-{[(4-t-butylbenzyl)(4-methylisoquinolin-3-yl)amino]sulfonyl}benzoesyre; 4-{[[4-(cyclopropylmethyl)benzyl](4-methylisoquinolin-3-yl)amino]sulfonyl}benzoesyre; 4-{[[4-fluor-3-(trifluormethyl)benzyl](4-methylisoquinolin-3-yl)amino]sulfonyl}- benzoesyre; 4-{[(4-methylisoquinolin-3-yl)(2-naphthylmethyl)amino]sulfonyl}benzoesyre; 4-({(1-methoxy-4-methylisoquinolin-3-yl)[4-(trifluormethoxy)benzyl]amino}sulfonyl)- benzoesyre; 4-({(4-chlorisoquinolin-3-yl)[4-(trifluormethoxy)benzyl]amino}sulfonyl)benzoesyre; 4-{[(4-methylisoquinolin-3-yl)(5,6,7,8-tetrahydronaphthalen-2-ylmethyl)amino]sulfonyl}- benzoesyre; 4-{[(2,3-dihydro-1H-inden-5-ylmethyl)(4-methylisoquinolin-3-yl)amino]sulfonyl}- benzoesyre; 4-{[[(1,1-dimethyl-2,3-dihydro-1H-inden-5-yl)methyl](4-methylisoquinolin-3-yl)amino]- sulfonyljbenzoesyre; 4-{[[(2,2-dimethyl-2,3-dihydro-1H-inden-5-yl)methyl](4-methylisoquinolin-3-yl)amino]- sulfonyl}benzoesyre; 4-{[[(3,3-dimethyl-2,3-dihydro-1-benzofuran-6-yl)methyl](4-methylisoquinolin-3-yl)- amino]sulfonyl}benzoesyre; 4-{[[(1-benzothiophen-2-yl)methyl](4-methylisoquinolin-3-yl)amino]sulfonyl}- benzoesyre; 4-({(1,4-dimethylisoquinolin-3-yl)[4-(trifluormethoxy)benzyl]amino}sulfonyl)benzoesyre; og 4-({(4-methylisoquinolin-3-yl)[4-(2,2,2-trifluor-1-methoxy-1-methylethyl)benzyl]amino}-sulfonyl)benzoesyre; eller et farmaceutisk acceptabelt salt deraf.
10. Forbindelse ifølge krav 1, som er valgt fra gruppen bestående af 4-({(1-cyclopropyl-4-methylisoquinolin-3-yl)[4-(trifluormethoxy)benzyl]amino}sulfonyl)- benzoesyre; 4-({(1-methoxy-4-methylisoquinolin-3-yl)[4-(trifluormethoxy)benzyl]amino}sulfonyl)- benzoesyre; 4-({(1-isopropyl-4-methylisoquinolin-3-yl)[4-(trifluormethoxy)benzyl]amino}sulfonyl)- benzoesyre; 4-{[{3-chlor-4-[cyclopropyl(difluor)methyl]benzyl}(4-methylisoquinolin-3-yl)amino]- sulfonyljbenzoesyre; 4-({(4-cyclopropylisoquinolin-3-yl)[4-(trifluormethoxy)benzyl]amino}sulfonyl)- benzoesyre; 4-{[{3-chlor-4-[cyclopropyl(difluor)methyl]benzyl}(1-cyclopropyl-4-methylisoquinolin-3- yl)amino]sulfonyl}benzoesyre; 4-{[{4-[cyclopropyl(difluor)methyl]-3-fluorbenzyl}(4-methylisoquinolin-3-yl)amino]- sulfonyl}benzoesyre; 4-({[4-(trifluormethoxy)benzyl][4-(trifluormethyl)isoquinolin-3-yl]amino}sulfonyl)- benzoesyre; 4-[((4-cyclopropylisoquinolin-3-yl){[5-(trifluormethyl)pyridin-2-yl]methyl}amino)sulfonyl]- benzoesyre; 4-{[{3-chlor-4-[cyclopropyl(difluor)methyl]benzyl}(4-cyclopropylisoquinolin-3-yl)amino]- sulfonyljbenzoesyre; 4-{[{4-[cyclopropyl(difluor)methyl]-3-fluorbenzyl}(4-cyclopropylisoquinolin-3-yl)amino]- sulfonyl}benzoesyre; 4-({(4-cyclopropylisoquinolin-3-yl)[5-(trifluormethoxy)-2,3-dihydro-1H-inden-1-yl]- amino}-sulfonyl)benzoesyre; 4-({{3-chlor-4-[cyclopropyl(difluor)methyl]benzyl}[4-(trifluormethyl)isoquinolin-3-yl]-amino}sulfonyl)benzoesyre; og 4-({{4-[cyclopropyl(difluor)methyl]-3-fluorbenzyl}[4-(trifluormethyl)isoquinolin-3-yl]-amino}sulfonyl)benzoesyre; eller et farmaceutisk acceptabelt salt deraf.
11. Farmaceutisk sammensætning, der som aktivt stof omfatter forbindelsen ifølge ethvert af kravene 1 til 10 eller et farmaceutisk acceptabelt salt deraf.
12. Forbindelse ifølge et hvert af kravene 1 til 10 eller et farmaceutisk acceptabelt salt deraf, til anvendelse som et medikament.
13. Farmaceutisk sammensætning ifølge krav 11, hvor den farmaceutiske sammensætning er til brug ved forebyggelse eller behandling af en sygdom eller tilstand valgt blandt kronisk smerte, cephalalgia, urologisk sygdom, carcinom, respiratorisk sygdom, gastrointestinal sygdom, psykiatrisk sygdom, neurologisk sygdom, og dermatose.
14. Farmaceutisk sammensætning ifølge krav 11, hvor den farmaceutiske sammensætning er til brug ved forebyggelse eller behandling af en sygdom eller tilstand valgt blandt kronisk smerte og urologisk sygdom.
15. Farmaceutisk sammensætning ifølge krav 11, hvor den farmaceutiske sammensætning er til anvendelse ved forebyggelse eller behandling af en sygdom eller tilstand */algt blandt neuropatisk smerte, nociceptiv smerte, og blandet smerte.
16. Forbindelse til anvendelse ifølge krav 12, kendetegnet ved, at medikamentet er til forebyggelse eller behandling af en sygdom eller tilstand valgt blandt kronisk smerte, cephalalgia, urologisk sygdom, carcinom, respiratorisk sygdom, gastrointestinal sygdom, psykiatrisk sygdom, neurologisk sygdom, og dermatose.
DK12712777.7T 2011-03-16 2012-03-15 Sulfonamidforbindelser med TRPM8-antagonistisk aktivitet DK2686302T3 (da)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201161453396P 2011-03-16 2011-03-16
PCT/JP2012/057412 WO2012124825A1 (en) 2011-03-16 2012-03-15 Sulfonamide compounds having trpm8 antagonistic activity

Publications (1)

Publication Number Publication Date
DK2686302T3 true DK2686302T3 (da) 2016-10-24

Family

ID=45932480

Family Applications (1)

Application Number Title Priority Date Filing Date
DK12712777.7T DK2686302T3 (da) 2011-03-16 2012-03-15 Sulfonamidforbindelser med TRPM8-antagonistisk aktivitet

Country Status (17)

Country Link
US (2) US8987445B2 (da)
EP (1) EP2686302B1 (da)
JP (1) JP5684401B2 (da)
KR (1) KR101638672B1 (da)
CN (1) CN103443080B (da)
AU (1) AU2012229813B2 (da)
BR (1) BR112013023330B8 (da)
CA (1) CA2826678C (da)
DK (1) DK2686302T3 (da)
ES (1) ES2588752T3 (da)
HU (1) HUE031585T2 (da)
MX (1) MX342882B (da)
PL (1) PL2686302T3 (da)
PT (1) PT2686302T (da)
RU (1) RU2563030C2 (da)
TW (1) TWI519520B (da)
WO (1) WO2012124825A1 (da)

Families Citing this family (18)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8987445B2 (en) 2011-03-16 2015-03-24 Mitsubishi Tanabe Pharma Corporation Sulfonamide compounds having TRPM8 antagonistic activity
WO2014042238A1 (ja) * 2012-09-14 2014-03-20 田辺三菱製薬株式会社 スルホンアミド化合物
JP5985453B2 (ja) * 2012-09-14 2016-09-06 田辺三菱製薬株式会社 医薬組成物
CN102924344A (zh) * 2012-10-10 2013-02-13 北京康正康仁生物科技有限公司 丙磺舒钠、丙磺舒钾的合成制备方法
EP2774919A1 (en) * 2013-03-06 2014-09-10 Pharmeste S.R.L. In Liquidazione Novel sulfonamide TRPA1 receptor antagonists
ES2645847T3 (es) * 2013-05-08 2017-12-11 Kissei Pharmaceutical Co., Ltd. Derivado de glicinamida alfa-sustituido
TW201605852A (zh) * 2013-09-26 2016-02-16 美國禮來大藥廠 新穎化合物及其製備ｔａｕ造影劑及ｔａｕ造影調配物之用途
CN104529895B (zh) * 2014-12-11 2017-02-08 温州大学 一种取代含氮杂环化合物的合成方法
CN104557701B (zh) * 2014-12-11 2016-05-04 温州大学 一种异喹啉衍生物的制备方法
CN105315357A (zh) * 2015-10-14 2016-02-10 韩蕾 Trpm8蛋白和相关多肽片段及其抗体的新用途
WO2017171107A1 (ko) * 2016-03-28 2017-10-05 엘지전자(주) 인터 예측 모드 기반 영상 처리 방법 및 이를 위한 장치
CN113398124A (zh) 2016-06-13 2021-09-17 田边三菱制药株式会社 用于治疗或预防血管舒缩症状的组合物
TW201929855A (zh) 2017-12-19 2019-08-01 日商田邊三菱製藥股份有限公司 用於治療或預防血管舒縮症狀的組成物及方法
JP6985137B2 (ja) * 2017-12-27 2021-12-22 田辺三菱製薬株式会社 スルホンアミド化合物の結晶形
US10553537B2 (en) * 2018-02-17 2020-02-04 Sandisk Technologies Llc Interconnects containing serpentine line structures for three-dimensional memory devices and methods of making the same
KR20210125471A (ko) 2018-10-05 2021-10-18 안나푸르나 바이오, 인코포레이티드 Apj 수용체 활성과 관련된 병태를 치료하기 위한 화합물 및 조성물
RU2726793C1 (ru) * 2020-02-12 2020-07-15 Федеральное государственное бюджетное учреждение науки Федеральный исследовательский центр "КОМИ научный центр Уральского отделения Российской академии наук" Хиральные 18-сульфопроизводные дегидроабиетана и способ их получения
CN115784857B (zh) * 2022-12-09 2024-05-24 长沙贝塔医药科技有限公司 一种4-氟苯基环丙基甲酮-14c及其制备方法

Family Cites Families (17)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4952722A (en) 1982-02-12 1990-08-28 Ici Australia Limited Compounds and compositions
DE19831878C2 (de) 1998-07-17 2001-05-17 Aventis Pharma Gmbh Polycyclische Thiazolidin-2-yliden Amine, Verfahren zu ihrer Herstellung und ihre Verwendung als Arzneimittel
DE10164139A1 (de) 2001-12-27 2003-07-10 Bayer Ag 2-Heteroarylcarbonsäureamide
CN1859908A (zh) 2003-10-01 2006-11-08 默克公司 作为s1p受体激动剂的3,5－芳基、杂芳基或环烷基取代的－1,2,4－噁二唑类化合物
DE602005008079D1 (de) * 2004-07-28 2008-08-21 Hoffmann La Roche Aryl-pyridinderivate als 11-beta-hsd1-hemmer
KR100854864B1 (ko) 2004-08-05 2008-08-28 에프. 호프만-라 로슈 아게 인돌, 인다졸 또는 인돌린 유도체
WO2006067445A2 (en) 2004-12-22 2006-06-29 Astrazeneca Ab Csf-1r kinase inhibitors
US7776877B2 (en) * 2007-06-22 2010-08-17 Chemocentryx, Inc. N-(2-(hetaryl)aryl) arylsulfonamides and N-(2-(hetaryl) hetaryl arylsulfonamides
CA2693159C (en) * 2007-07-18 2016-05-24 Shawn T. Branum Sulfonamides as trpm8 modulators
ES2499017T3 (es) 2007-10-23 2014-09-26 F. Hoffmann-La Roche Ag Nuevos inhibidores de quinasa
WO2010010435A2 (en) 2008-07-22 2010-01-28 Glenmark Pharmaceutical S.A. Fused oxazole and thiazole derivatives as trpms modulators
JP2012516885A (ja) 2009-02-04 2012-07-26 ファイザー・インク ４−アミノ−７，８−ジヒドロピリド［４，３−ｄ］ピリミジン−５（６Ｈ）−オン誘導体
RU2011148937A (ru) * 2009-05-01 2013-06-10 Раквалиа Фарма Инк. Производные сульфамоилбензойной кислоты в качестве антагонистов trpm8
TW201103941A (en) * 2009-06-10 2011-02-01 Janssen Pharmaceutica Nv Benzimidazole derivatives useful as TRPM8 channel modulators
US8829026B2 (en) 2010-10-01 2014-09-09 Raqualia Pharma Inc. Sulfamoyl benzoic acid heterobicyclic derivatives as TRPM8 antagonists
CN103354812A (zh) 2010-12-09 2013-10-16 詹森药业有限公司 作为trpm8调节剂的咪唑并[1,2-a]吡啶磺酰胺
US8987445B2 (en) 2011-03-16 2015-03-24 Mitsubishi Tanabe Pharma Corporation Sulfonamide compounds having TRPM8 antagonistic activity

Also Published As

Publication number Publication date
CN103443080B (zh) 2016-10-12
AU2012229813A1 (en) 2013-08-29
HUE031585T2 (en) 2017-07-28
MX2013010572A (es) 2013-10-03
EP2686302A1 (en) 2014-01-22
CA2826678C (en) 2016-07-26
KR101638672B1 (ko) 2016-07-11
PL2686302T3 (pl) 2017-01-31
CA2826678A1 (en) 2012-09-20
ES2588752T3 (es) 2016-11-04
CN103443080A (zh) 2013-12-11
PT2686302T (pt) 2016-11-02
US20150218143A1 (en) 2015-08-06
JP5684401B2 (ja) 2015-03-11
US20140005393A1 (en) 2014-01-02
TWI519520B (zh) 2016-02-01
WO2012124825A1 (en) 2012-09-20
AU2012229813B2 (en) 2015-09-03
JP2014508105A (ja) 2014-04-03
EP2686302B1 (en) 2016-08-10
KR20140011385A (ko) 2014-01-28
MX342882B (es) 2016-10-14
BR112013023330A2 (pt) 2017-07-18
BR112013023330B8 (pt) 2022-09-27
US8987445B2 (en) 2015-03-24
RU2563030C2 (ru) 2015-09-20
BR112013023330B1 (pt) 2021-09-08
RU2013146011A (ru) 2015-04-27
TW201300362A (zh) 2013-01-01
US9540360B2 (en) 2017-01-10

Similar Documents

Publication Publication Date Title
DK2686302T3 (da) Sulfonamidforbindelser med TRPM8-antagonistisk aktivitet
KR101699991B1 (ko) 신규의 아미노 아자헤테로시클릭 카르복사미드
JP5375824B2 (ja) アミド化合物
JP5134368B2 (ja) アリール窒素含有二環式化合物およびそれのキナーゼ阻害薬としての使用
JP2018145196A (ja) Ｐｄｋ１インヒビターとして有用な複素環式化合物
JP6552061B2 (ja) 代謝型グルタミン酸受容体の負のアロステリックモジュレーター（ｎａｍｓ）とその使用
TW201422605A (zh) 新穎之胺衍生物或其鹽
JP7395807B2 (ja) アミド類化合物の調製方法及びその医薬分野の使用
JP7170996B2 (ja) スルホンアミド誘導体またはその薬学的に許容される酸付加塩
JP5985453B2 (ja) 医薬組成物
JP6127056B2 (ja) スルホンアミド化合物
WO2019242689A1 (zh) 一种氰基取代吡啶及氰基取代嘧啶类化合物、制备方法及其应用
KR101667277B1 (ko) Trpm8 수용체 조절제로서 유용한 치환된 아자-바이사이클릭 이미다졸 유도체
JP2007511570A (ja) 不適切なａｌｋ５に関連する疾患を治療するための１−アミノ−イソキノリン誘導体
TW200815407A (en) Substituted 3-cyanopyridines as protein kinase inhibitors