DK1807077T3 - Inhibitorer af c-fms kinase - Google Patents

Inhibitorer af c-fms kinase Download PDF

Info

Publication number
DK1807077T3
DK1807077T3 DK05815361.0T DK05815361T DK1807077T3 DK 1807077 T3 DK1807077 T3 DK 1807077T3 DK 05815361 T DK05815361 T DK 05815361T DK 1807077 T3 DK1807077 T3 DK 1807077T3
Authority
DK
Denmark
Prior art keywords
phenyl
cyano
carboxylic acid
amide
enyl
Prior art date
Application number
DK05815361.0T
Other languages
English (en)
Inventor
Jinsheng Chen
Sanath Meegalla
Ken Wilson
Renee Desjarlais
Christopher Molloy
Carl Manthey
Christopher Flores
Carl R Illig
Shelley K Ballentine
M Jonathan Rudolph
Mark J Wall
Original Assignee
Janssen Pharmaceutica Nv
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 Janssen Pharmaceutica Nv filed Critical Janssen Pharmaceutica Nv
Application granted granted Critical
Publication of DK1807077T3 publication Critical patent/DK1807077T3/da

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D307/00—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
    • C07D307/02—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings
    • C07D307/34—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D307/38—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D307/54—Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • 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
    • 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
    • A61K31/16—Amides, e.g. hydroxamic acids
    • A61K31/165—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
    • 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
    • A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • 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
    • A61P1/18—Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—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
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • 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
    • A61P25/18—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
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A61P31/18—Antivirals for RNA viruses for HIV
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D307/00—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
    • C07D307/02—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings
    • C07D307/34—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D307/56—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D307/68—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
    • 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
    • C07D407/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00
    • C07D407/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 containing two hetero rings
    • C07D407/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 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
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings

Landscapes

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

Claims (25)

1. Forbindelse med formel I:
eller et solvat, hydrat, tautomer eller farmaceutisk acceptabelt salt deraf, hvor: A er phenyl der kan være substitueret med én af chlor, fluor, eller methyl; W er pyrrolyl, imidazolyl, isoxazolyl, oxazolyl, eller furanyl, der hver kan være bundet til et hvilket som helst carbonatom, hvor pyrrolyl, imidazolyl, isoxazolyl, oxazolyl, eller furanyl kan indeholde en -Cl-, -CN-, -NO2-, -OMe-, eller -CF3-substitution, bundet til et hvilket som helst andet carbon; R2 er cycloalkyl, thiophenyl, dihydrosulfonopyranyl, phenyl, furanyl, tetrahydropyridyl, eller dihydropyranyl, hvilke som helst kan være uafhængigt substitueret med én eller to af hver af de følgende: chlor, fluor, og C(i-3)alkyl, med det forbehold at tetrahydropyridyl er bundet til ringen A gennem en carbon-carbon-binding; hvor udtrykket "cycloalkyl" betegner en mættet eller delvis umættet ring sammensat af fra 3 til 8 carbonatomer; X er
og er bundet til phenyl A-ringen para til nitrogensubstituenten, som afbildet i formel II:
Z er CH eller N; D1 og D2 er hver hydrogen eller sammen danner en dobbeltbinding til et oxygen: D3 og D4 er hydrogen; E er N eller SO2, med det forbehold at E ikke kan være N hvis de følgende tre betingelser er til stede samtidig: Qa er fraværende, Qb er fraværende, og R3 er en aminogruppe eller cyclisk aminoradikal hvor vedhæftningspunktet til E er N; Qa er fraværende, -CH2-, -CH2CH2-, eller -C(O)-; Qb er fraværende, -NH-, -CH2-, -CH2CH2-, eller -C(O)-, med det forbehold at Qb ikke kan være C(O) hvis Qa er C(O), og yderligere forudsat at Qb ikke kan være -NH- hvis E er N og Qa er fraværende, yderligere forudsat at Qb ikke kan være -NH- hvis R3 er en aminogruppe eller cyclisk aminoradikal hvor vedhæftningspunktet til Qb er N; R3 er hydrogen, piperidinyl, alkylamino, dialkylamino, hydroxyalkylamino, (hydroxyalkyl)2amino, imidazolyl, 1-methyl imidazolyl, pyridyl, pyridyl N-oxid, hydroxyalkyl, -COOH, -CONH2, -CN, -SO2CH3, -NH2, morpholinyl; R3 kan også være fraværende, med det forbehold at R3 ikke er fraværende når E er nitrogen.
2. Forbindelse ifølge krav 1, hvor: A er phenyl; W er furan-2-yl, lAV-pyrrol-2-yl, eller lfy-imidazol-2-yl, hvilke som helst kan være substitueret ved det 4. eller 5.carbonatom med -CN; R2 er cycloalkyl, dihydrosulfonopyranyl, phenyl, furanyl, tetrahydropyridyl, eller dihydropyranyl, hvilke som helst kan være uafhængigt substitueret med én eller to af hver af substituenterne valgt fra gruppen bestående af chlor, fluor, og C(i-3)alkyl, med det forbehold at tetrahydropyridyl skal være bundet til ringen A gennem en carbon-carbon-binding.
3. Forbindelse ifølge krav 2 hvor: W er 3F/-2-imidazolyl-4-carbonitril eller 5-cyano-lW-pyrrol-2-yl; R2 er cyclohexenyl, eller cyclopentenyl, der hver kan være substitueret med chlor, fluor eller én eller to Qi-3)alkylgrupper; E er N, med det forbehold at E ikke kan være N hvis de følgende tre betingelser er til stede samtidigt: Qa er fraværende, Qb er fraværende, og R3 er en aminogruppe eller cyclisk aminoradikal hvor vedhæftningspunktet til E er N; Z er CH.
4. Forbindelse ifølge krav 3, hvor: W er 3F/-2-imidazolyl-4-carbonitril; Qa er CO; R3 er hydrogen, piperidinyl, hydroxyalkylamino, (hydroxyalkyl)2amino, alkylamino, dialkylamino, imidazolyl, 1-methyl imidazolyl, pyridinyl, pyridinyl N-oxide, hydroxyalkyl, -COOH, -CONH2, -CN, -SC>2CH3,-NH2, morpholinyl.
5. Forbindelse ifølge krav 1, valgt fra gruppen bestående af: 5-cyano-furan-2-carboxylsyre-[4-(4-methyl-piperazin-l-yl)-2-(3-methyl-thiophen-2-yl)-phenyl]-amid, og 5-cyano-furan-2-carboxylsyre-[4-(4-methyl-piperazin-l-yl)-2-(2-methyl- thiophen-3-yl)-phenyl]-amid, og solvater, hydrater, tautomerer og farmaceutisk acceptable salte deraf.
6. Forbindelse ifølge krav 2, valgt fra gruppen bestående af: 4-cyano-lH-imidazol-2-carboxylsyre-[4-(l-acetyl-piperidin-4-yl)-2- (l,2,5,6-tetrahydro-pyridin-3-yl)-phenyl]-amid, 4- cyano-lF/-imidazol-2-carboxylsyre-[2-cyclohex-l-enyl-4-(l,l-dioxo-hexahydro-lA6-thiopyran-4-yl)-phenyl]-amid, 5- cyano-furan-2-carboxylsyre-[2-cyclohex-l-enyl-4-(4-methyl-piperazin-l-yl)-phenyl]-amid, 5-cyano-furan-2-carboxylsyre-[2-(3,6-dihydro-2H-pyran-4-yl)-4-(4- methyl-piperazin-l-yl)-phenyl]-amid, 5-cyano-furan-2-carboxylsyre-[2'-methyl-5-(4-methyl-piperazin-l-yl)-biphenyl-2-yl]-amid, og 5-cyano-furan-2-carboxylsyre-[2'-fluor-5-(4-methyl-piperazin-l-yl)- biphenyl-2-yl]-amid, og solvater, hydrater, tautomerer og farmaceutisk acceptable salte deraf.
7. Forbindelse ifølge krav 3, valgt fra gruppen bestående af: (4-{4-[(4-cyano-lH-imidazol-2-carbonyl)-amino]-3-cyclohex-l-enyl- phenyl}-piperidin-l-yl)-eddikesyre, 4-cyano-lH-imidazol-2-carboxylsyre-[4-(l-carbamoylmethyl-piperidin-4- yl)-2-cyclohex-l-enyl-phenyl]-amid, 4-cyano-lH-imidazol-2-carboxylsyre-[2-(4-methyl-cyclohex-l-enyl)-4- piperidin-4-yl-phenyl]-amid, 4-cyano-lH-imidazol-2-carboxylsyre-{2-cyclohex-l-enyl-4-[l-(2-hydroxy- ethyl)-piperidin-4-yl]-phenyl>-amid, 4-cyano-lH-imidazol-2-carboxylsyre-[2-(4-methyl-cyclohex-l-enyl)-4-(l- pyridin-2-ylmethyl-piperidin-4-yl)-phenyl]-amid, 4-cyano-lH-imidazol-2-carboxylsyre-{2-cyclohex-l-enyl-4-[l-(2-hydroxy- 1- hydroxymethyl-ethyl)-piperidin-4-yl]-phenyl}-amid, 4-cyano-lH-imidazol-2-carboxylsyre-{4-[l-(2-cyano-ethyl)-piperidin-4-yl]- 2- cyclohex-l-enyl-phenyl}-amid, 4-cyano-lH-imidazol-2-carboxylsyre-{2-cyclohex-l-enyl-4-[l-(2- morpholin-4-yl-ethyl)-piperidin-4-yl]-phenyl}-amid, 4-cyano-lH-imidazol-2-carboxylsyre-(2-cyclohex-l-enyl-4-piperidin-4-yl- phenyl)-amid, 4-cyano-lH-imidazol-2-carboxylsyre-{2-cyclohex-l-enyl-4-[l-(2- methansulfonyl-ethyl)-piperidin-4-yl]-phenyl>-annid, 4-cyano-lH-imidazol-2-carboxylsyre-[2-cyclohex-l-enyl-4-(l-pyridin-2- ylmethyl-piperidin-4-yl)-phenyl]-amid, 4-cyano-lH-imidazol-2-carboxylsyre-{2-cyclopent-l-enyl-4-[l-(l-methyl- lH-imidazol-2-ylmethyl)-piperidin-4-yl]-phenyl}-amid, 4-cyano-lH-imidazol-2-carboxylsyre-(2-cyclopent-l-enyl-4-piperidin-4-yl- phenyl)-amid, 4-cyano-lH-pyrrol-2-carboxylsyre-(2-cyclohex-l-enyl-4-piperidin-4-yl- phenyl)-amid, 4-cyano-lH-imidazol-2-carboxylsyre-[2-cyclohex-l-enyl-4-(3,4,5,6-tetrahydro-2H-[l,2']bipyridinyl-4-yl)-phenyl]-amid, og 4-cyano-lH-pyrrol-2-carboxylsyre-[4-(l-acetyl-piperidin-4-yl)-2-cyclohex- l-enyl-phenyl]-amid, og solvater, hydrater, tautomerer og farmaceutisk acceptable salte deraf.
8. Forbindelse ifølge krav 4 valgt fra gruppen bestående af: 4-cyano-lH-imidazol-2-carboxylsyre-{2-cyclohex-l-enyl-4-[l-(l-oxy- pyridin-3-carbonyl)-piperidin-4-yl]-phenyl}-amid, 4-cyano-lH-imidazol-2-carboxylsyre-{2-cyclohex-l-enyl-4-[l-(l-oxy- pyridin-4-carbonyl)-piperidin-4-yl]-phenyl}-amid, 4-cyano-lH-imidazol-2-carboxylsyre-{2-cyclohex-l-enyl-4-[l-(3- morpholin-4-yl-propionyl)-piperidin-4-yl]-phenyl}-amid, 4-{4-[(4-cyano-lH-imidazol-2-carbonyl)-amino]-3-cyclohex-l-enyl- phenyl}-piperidin-l-carboxylsyre-amid, 4-cyano-lH-imidazol-2-carboxylsyre-{2-cyclohex-l-enyl-4-[l-(pyridin-3- carbonyl)-piperidin-4-yl]-phenyl>-amid, 4-{4-[(4-cyano-lH-imidazol-2-carbonyl)-amino]-3-cyclohex-l-enyl- phenyl}-piperidin-l-carboxylsyre-(2-hydroxy-ethyl)-amid, 4-cyano-lH-imidazol-2-carboxylsyre-{2-cyclohex-l-enyl-4-[l-(2-3H- imidazol-4-yl-acetyl)-piperidin-4-yl]-phenyl}-amid, 4-cyano-lH-imidazol-2-carboxylsyre-{2-cyclohex-l-enyl-4-[l-(2-pyridin-4- yl-acetyl)-piperidin-4-yl]-phenyl}-amid, 4-cyano-lH-imidazol-2-carboxylsyre-(2-cyclohex-l-enyl-4-{l-[2-(l- methyl-lH-imidazol-4-yl)-acetyl]-piperidin-4-yl}-phenyl)-amid, 4-cyano-lH-imidazol-2-carboxylsyre-{2-cyclohex-l-enyl-4-[l-(2-pyridin-3- yl-acetyl)-piperidin-4-yl]-phenyl>-amid, 4-cyano-lH-imidazol-2-carboxylsyre-{2-cyclohex-l-enyl-4-[l-(2- methansulfonyl-acetyl)-piperidin-4-yl]-phenyl}-amid, 4-cyano-lH-imidazol-2-carboxylsyre-{2-cyclohex-l-enyl-4-[l-(2-pyridin-2-yl-acetyl)-piperidin-4-yl]-phenyl}-amid, og 4-cyano-lH-imidazol-2-carboxylsyre-[4-(l-acetyl-piperidin-4-yl)-2- cyclohex-l-enyl-phenyl]-amid, og solvater, hydrater, tautomerer og farmaceutisk acceptable salte deraf.
9. Forbindelse ifølge krav 1, som er: 4-cyano-lH-imidazol-2-carboxylsyre-[2-cyclohex-l-enyl-4-(l-{2-[(2- hydroxy-ethyl)-methyl-amino]-acetyl}-piperidin-4-yl)-phenyl]-amid, og solvater, hydrater, tautomerer og farmaceutisk acceptable salte deraf.
10. Forbindelse ifølge krav 1, som er: 4-cyano-lH-imidazol-2-carboxylsyre-{2-cyclohex-l-enyl-4-[l-(2- dimethylamino-acetyl)-piperidin-4-yl]-phenyl}-amid, og solvater, hydrater, tautomerer og farmaceutisk acceptable salte deraf.
11. Forbindelse ifølge krav 1, som er: 4-cyano-lH-imidazol-2-carboxylsyre-{2-cyclohex-l-enyl-4-[l-(2- morpholin-4-yl-acetyl)-piperidin-4-yl]-phenyl}-amid, og solvater, hydrater, tautomerer og farmaceutisk acceptable salte deraf.
12. Farmaceutisk sammensætning, omfattende en forbindelse ifølge krav 1 og en farmaceutisk acceptabel bærer.
13. Farmaceutisk doseringsform omfattende en farmaceutisk acceptabel bærer og fra ca. 0,5 mg til ca. 10 g af mindst en forbindelse ifølge krav 1.
14. Doseringsform ifølge krav 13 tilpasset til parenteral eller oral administration.
15. Forbindelse ifølge krav 1 til anvendelse i terapi.
16. Forbindelse ifølge krav 1 til anvendelse i inhibering af proteintyrosinasekinaseaktivitet.
17. Forbindelse til anvendelse ifølge krav 16, hvor proteintyrosinasekinasen er c-fms.
18. Forbindelse ifølge krav 1 til anvendelse i behandling af inflammation i et pattedyr.
19. Forbindelse ifølge krav 1 til anvendelse i behandling af cancer i et pattedyr.
20. Forbindelse ifølge krav 1 til anvendelse i behandling af kardiovaskulær sygdom i et pattedyr.
21. Forbindelse ifølge krav 1 til anvendelse i behandling af sygdomme med en inflammatorisk komponent herunder glomerulonephritis, inflammatorisk tarmsygdom, protesefejl, sarcoidose, kongestiv obstruktiv pulmonær sygdom, astma, pankreatitis, HIV-infektion, psoriasis, diabetes, tumor-beslægtet angiogenese, alder-relateret makulær degeneration, diabetisk retinopati, restenose, schizofreni eller Alzheimer's demens i et pattedyr.
22. Forbindelse ifølge krav 1 til anvendelse i behandling af smerte, herunder knoglesmerte forårsaget af tumormetastase eller osteoarthritis, eller visceral, inflammatorisk, og neurogen smerte hos et pattedyr.
23. Forbindelse ifølge krav 1 til anvendelse i behandling af osteoporose, Paget's sygdom, og andre sygdomme i hvilke knogleresorption medierer morbiditet herunder arthritis, protesefejl, osteolytisk sarcom, myelom, og tumormetastaser til knogler.
24. Forbindelse ifølge krav 1 til anvendelse i behandling afog til forebyggelse af metastaser fra æggestokcancer, livmodercancer, brystcancer, tyktarm cancer, mavecancer, hårcelleleukæmi og ikke-småcellet lungecarcinom.
25. Forbindelse ifølge krav 1 til anvendelse i behandling af autoimmune sygdomme såsom systemisk lupus erythematosus, rheumatoid arthritis, Sjøgren's syndrom, multipel sclerose, eller uveitis.
DK05815361.0T 2004-10-22 2005-10-20 Inhibitorer af c-fms kinase DK1807077T3 (da)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US62121104P 2004-10-22 2004-10-22
PCT/US2005/037868 WO2006047277A2 (en) 2004-10-22 2005-10-20 Inhibitors of c-fms kinase

Publications (1)

Publication Number Publication Date
DK1807077T3 true DK1807077T3 (da) 2017-01-23

Family

ID=36228272

Family Applications (1)

Application Number Title Priority Date Filing Date
DK05815361.0T DK1807077T3 (da) 2004-10-22 2005-10-20 Inhibitorer af c-fms kinase

Country Status (18)

Country Link
EP (1) EP1807077B1 (da)
JP (1) JP5046950B2 (da)
KR (1) KR101273434B1 (da)
CN (1) CN101437514B (da)
AU (1) AU2005299837A1 (da)
BR (1) BRPI0516947A (da)
CA (1) CA2585053C (da)
DK (1) DK1807077T3 (da)
EA (1) EA013250B1 (da)
ES (1) ES2611604T3 (da)
HU (1) HUE033089T2 (da)
MX (1) MX2007004784A (da)
NO (1) NO339555B1 (da)
PL (1) PL1807077T3 (da)
PT (1) PT1807077T (da)
UA (1) UA88648C2 (da)
WO (1) WO2006047277A2 (da)
ZA (1) ZA200704106B (da)

Families Citing this family (45)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7790724B2 (en) 2003-04-25 2010-09-07 Janssen Pharmaceutica N.V. c-fms kinase inhibitors
WO2004096795A2 (en) 2003-04-25 2004-11-11 3-Dimensional Pharmaceuticals, Inc. C-fms kinase inhibitors
US7427683B2 (en) 2003-04-25 2008-09-23 Ortho-Mcneil Pharmaceutical, Inc. c-fms kinase inhibitors
TW200526626A (en) 2003-09-13 2005-08-16 Astrazeneca Ab Chemical compounds
ATE437864T1 (de) * 2004-10-22 2009-08-15 Janssen Pharmaceutica Nv Aromatische amide als hemmer der c-fms-kinase
EP1853586B1 (en) 2005-02-18 2013-07-24 AstraZeneca AB Antibacterial piperidine derivatives
CN101171247A (zh) * 2005-03-04 2008-04-30 阿斯利康(瑞典)有限公司 作为dna促旋酶和拓扑异构酶抑制剂的吡咯衍生物
US7705002B2 (en) 2005-05-19 2010-04-27 Vertex Pharmaceuticals Incorporated Biaryls useful as modulators of ion channels
US7880008B2 (en) 2005-05-31 2011-02-01 Vertex Pharmaceuticals Incorporated Heterocycles useful as modulators of ion channels
US20060281788A1 (en) * 2005-06-10 2006-12-14 Baumann Christian A Synergistic modulation of flt3 kinase using a flt3 inhibitor and a farnesyl transferase inhibitor
US20070004660A1 (en) * 2005-06-10 2007-01-04 Baumann Christian A Synergistic Modulation of Flt3 Kinase Using Alkylquinolines and Alkylquinazolines
CA2626623C (en) * 2005-10-18 2016-08-30 Janssen Pharmaceutica N.V. Method of inhibiting flt3 kinase
KR101367645B1 (ko) 2006-04-20 2014-02-27 얀센 파마슈티카 엔.브이. Ｃ-ｆｍｓ 키나제의 저해제로서의 복소환식 화합물
AU2006342509A1 (en) * 2006-04-20 2007-11-01 Janssen Pharmaceutica, N.V. c-fms kinase inhibitors
EP2016070B1 (en) 2006-04-20 2016-01-13 Janssen Pharmaceutica N.V. Inhibitors of c-fms kinase
CA2649755C (en) * 2006-04-20 2014-12-02 Janssen Pharmaceutica N.V. Method of inhibiting c-kit kinase
US8697716B2 (en) * 2006-04-20 2014-04-15 Janssen Pharmaceutica Nv Method of inhibiting C-KIT kinase
JO2972B1 (en) * 2007-06-08 2016-03-15 جانسين فارماسوتيكا ان. في Piperidine / piperazine derivatives
CA2687754C (en) 2007-06-08 2015-12-08 Janssen Pharmaceutica N.V. Piperidine, piperazine derivatives for use as dgat inhibitors
US8633197B2 (en) 2007-06-08 2014-01-21 Janssen Pharmaceutica N.V. Piperidine/piperazine derivatives
CA2687912C (en) 2007-06-08 2015-11-03 Janssen Pharmaceutica N.V. Piperidine/piperazine derivatives
AU2013203813B2 (en) * 2007-10-17 2014-07-31 Janssen Pharmaceutica, N.V. Inhibitors of C-FMS kinase
JO3240B1 (ar) * 2007-10-17 2018-03-08 Janssen Pharmaceutica Nv c-fms مثبطات كيناز
CA2704517A1 (en) * 2007-11-02 2009-05-07 Janssen Pharmaceutica, N.V. Use of cfms inhibitor for treating or preventing bone cancer and the bone loss and bone pain associated with bone cancer
TWI498115B (zh) 2007-12-27 2015-09-01 Daiichi Sankyo Co Ltd 咪唑羰基化合物
UY31863A (es) 2008-06-05 2010-01-05 Janssen Pharmaceutica Nv Combinaciones de drogas que comprenden un inhibidor de dgat y un agonista de ppar
WO2011149841A1 (en) 2010-05-25 2011-12-01 Janssen Pharmaceutica Nv SUBSTITUTED THIAZOLIDINEDIONE INDAZOLES, INDOLES AND BENZOTRIAZOLES AS ESTROGEN-RELATED RECEPTOR-α MODULATORS
ES2611504T3 (es) 2012-03-07 2017-05-09 Institute Of Cancer Research: Royal Cancer Hospital (The) Compuestos de isoquinolin-1-ona 3-aril-5-sustituida y sus usos terapéuticos
JOP20180012A1 (ar) 2012-08-07 2019-01-30 Janssen Pharmaceutica Nv عملية السلفنة باستخدام نونافلوروبوتانيسولفونيل فلوريد
EP2882757B1 (en) 2012-08-07 2016-10-05 Janssen Pharmaceutica, N.V. Process for the preparation of heterocyclic ester derivatives
CA2879176C (en) * 2012-09-17 2020-10-27 F.Hoffmann-La Roche Ag Triazole carboxamide derivatives
CN103664957A (zh) * 2012-09-25 2014-03-26 杨子娇 一类治疗房角狭窄的化合物及其用途
CN103804349A (zh) * 2012-11-01 2014-05-21 杨子娇 一类治疗青光眼的化合物及其用途
CN104370881A (zh) * 2013-01-24 2015-02-25 韩冰 一类具有神经保护作用的化合物及其制备方法和用途
CN104370880A (zh) * 2013-01-24 2015-02-25 韩冰 一类蛋白酶抑制剂及其制备方法和用途
CN104370882A (zh) * 2013-01-24 2015-02-25 韩冰 一类降低眼压的化合物及其制备方法和用途
HUE036925T2 (hu) 2013-03-15 2018-08-28 Janssen Pharmaceutica Nv C-fms kináz inhibitorként használható helyettesített piridin származékok
TWI630205B (zh) 2013-07-22 2018-07-21 瑞士商愛杜西亞製藥有限公司 １－（哌－１－基）－２－（［１，２，４］三唑－１－基）－乙酮衍生物
AU2014320149A1 (en) 2013-09-11 2016-04-07 Institute Of Cancer Research: Royal Cancer Hospital (The) 3-aryl-5-substituted-isoquinolin-1-one compounds and their therapeutic use
HUE042559T2 (hu) 2015-01-15 2019-07-29 Idorsia Pharmaceuticals Ltd Hidroxialkil-piperazin származékok mint cxcr3 receptor modulátorok
AR103399A1 (es) 2015-01-15 2017-05-10 Actelion Pharmaceuticals Ltd Derivados de (r)-2-metil-piperazina como moduladores del receptor cxcr3
JP7012822B2 (ja) * 2017-08-10 2022-02-14 中国科学院上海薬物研究所 フタラジノン系化合物、その製造方法、医薬組成物及びその使用
US10930064B2 (en) 2018-02-08 2021-02-23 Covidien Lp Imaging reconstruction system and method
AU2019407650B2 (en) 2018-12-17 2022-10-27 Tolremo Therapeutics Ag Heterocyclic derivatives, pharmaceutical compositions and their use in the treatment, amelioration or prevention of cancer
WO2021144360A1 (en) 2020-01-17 2021-07-22 F. Hoffmann-La Roche Ag Small molecule csf-1r inhibitors in therapeutic and cosmetic uses

Family Cites Families (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB9523675D0 (en) * 1995-11-20 1996-01-24 Celltech Therapeutics Ltd Chemical compounds
JP2002520324A (ja) * 1998-07-10 2002-07-09 メルク エンド カムパニー インコーポレーテッド 新規な血管形成インヒビター
GB9824579D0 (en) * 1998-11-10 1999-01-06 Novartis Ag Organic compounds
ES2206191T3 (es) * 1999-01-11 2004-05-16 Princeton University Inhibidores de alta afinidad para validacion de dianas y usos de los mismos.
ATE449764T1 (de) * 1999-12-28 2009-12-15 Pharmacopeia Inc Cytokine, insbesondere tnf-alpha, hemmer
US7105682B2 (en) * 2001-01-12 2006-09-12 Amgen Inc. Substituted amine derivatives and methods of use
WO2003099796A1 (en) * 2002-05-23 2003-12-04 Cytopia Pty Ltd Protein kinase inhibitors
AU2003282726B2 (en) * 2002-10-03 2010-10-07 Targegen, Inc. Vasculostatic agents and methods of use thereof
US20050113566A1 (en) * 2003-04-25 2005-05-26 Player Mark R. Inhibitors of C-FMS kinase
WO2004096795A2 (en) * 2003-04-25 2004-11-11 3-Dimensional Pharmaceuticals, Inc. C-fms kinase inhibitors
ATE437864T1 (de) * 2004-10-22 2009-08-15 Janssen Pharmaceutica Nv Aromatische amide als hemmer der c-fms-kinase
CA2626623C (en) * 2005-10-18 2016-08-30 Janssen Pharmaceutica N.V. Method of inhibiting flt3 kinase

Also Published As

Publication number Publication date
PL1807077T3 (pl) 2017-05-31
NO339555B1 (no) 2017-01-02
KR101273434B1 (ko) 2013-06-11
UA88648C2 (en) 2009-11-10
ES2611604T3 (es) 2017-05-09
JP5046950B2 (ja) 2012-10-10
MX2007004784A (es) 2007-09-11
CA2585053A1 (en) 2006-05-04
CN101437514B (zh) 2012-04-25
ZA200704106B (en) 2009-09-30
EP1807077A4 (en) 2011-09-21
KR20070085382A (ko) 2007-08-27
HUE033089T2 (en) 2017-11-28
CN101437514A (zh) 2009-05-20
PT1807077T (pt) 2017-01-06
EA200700918A1 (ru) 2008-06-30
EP1807077B1 (en) 2016-11-23
AU2005299837A1 (en) 2006-05-04
WO2006047277A3 (en) 2009-05-07
WO2006047277A2 (en) 2006-05-04
JP2008517926A (ja) 2008-05-29
CA2585053C (en) 2011-07-12
NO20072489L (no) 2007-06-29
BRPI0516947A (pt) 2008-09-23
EA013250B1 (ru) 2010-04-30
EP1807077A2 (en) 2007-07-18

Similar Documents

Publication Publication Date Title
DK1807077T3 (da) Inhibitorer af c-fms kinase
US7645755B2 (en) Inhibitors of c-fms kinase
EP1807407B1 (en) Aromatic amides as inhibitors of c-fms kinase
KR102438302B1 (ko) 리신 특이적 데메틸라제-1의 억제제
AU2021203497B2 (en) Pyran derivatives as cyp11a1 (cytochrome p450 monooxygenase 11a1) inhibitors
US7662837B2 (en) Inhibitors of c-fms kinase
JP5221453B2 (ja) イミダゾール誘導体
JP2005539001A (ja) ヒストンデアセチラーゼインヒビターとしての置換チエニルヒドロキサム酸
KR20120049940A (ko) 키나제 억제제로서의 헤테로아릴 화합물
BRPI0710548B1 (pt) INIBIDORES DE c-FMS CINASE, COMPOSIÇÃO FARMACÊUTICA E FORMA DE DOSAGEM FARMACÊUTICA
JP5595727B2 (ja) Ｃ−ｋｉｔキナーゼ阻害法
AU2011203515B2 (en) Inhibitors of c-fms kinase