[go: up one dir, main page]

HRP20150839T1 - Spojevi aril-fenil-sulfonamido-cikloalkila i njihova uporaba - Google Patents

Spojevi aril-fenil-sulfonamido-cikloalkila i njihova uporaba Download PDF

Info

Publication number
HRP20150839T1
HRP20150839T1 HRP20150839TT HRP20150839T HRP20150839T1 HR P20150839 T1 HRP20150839 T1 HR P20150839T1 HR P20150839T T HRP20150839T T HR P20150839TT HR P20150839 T HRP20150839 T HR P20150839T HR P20150839 T1 HRP20150839 T1 HR P20150839T1
Authority
HR
Croatia
Prior art keywords
independently
image
cancer
compound according
independent
Prior art date
Application number
HRP20150839TT
Other languages
English (en)
Inventor
Iain Robert Greig
Rose Mary Sheridan
Raymond Fisher
Matthew John Tozer
Juha Andrew Clase
Andrew Smith
Andrew Robert Tuffnell
Robert Jurgen Van 't Hof
Original Assignee
Pimco 2664 Limited
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 Pimco 2664 Limited filed Critical Pimco 2664 Limited
Publication of HRP20150839T1 publication Critical patent/HRP20150839T1/hr

Links

Classifications

    • 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
    • A61K31/18—Sulfonamides
    • 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
    • A61K31/4418—Non condensed pyridines; Hydrogenated derivatives thereof having a carbocyclic group directly attached to the heterocyclic ring, e.g. cyproheptadine
    • 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
    • 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
    • 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
    • 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
    • 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
    • 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
    • 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
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C311/00—Amides of sulfonic acids, i.e. compounds having singly-bound oxygen atoms of sulfo groups replaced by nitrogen atoms, not being part of nitro or nitroso groups
    • C07C311/15—Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of six-membered aromatic rings
    • C07C311/20—Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the sulfonamide groups bound to a carbon atom of a ring other than a six-membered aromatic ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C311/00—Amides of sulfonic acids, i.e. compounds having singly-bound oxygen atoms of sulfo groups replaced by nitrogen atoms, not being part of nitro or nitroso groups
    • C07C311/22—Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound oxygen atoms
    • C07C311/28—Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound oxygen atoms having the sulfur atom of at least one of the sulfonamide groups bound to a carbon atom of a ring other than a six-membered aromatic ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C311/00—Amides of sulfonic acids, i.e. compounds having singly-bound oxygen atoms of sulfo groups replaced by nitrogen atoms, not being part of nitro or nitroso groups
    • C07C311/22—Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound oxygen atoms
    • C07C311/29—Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound oxygen atoms having the sulfur atom of at least one of the sulfonamide groups bound to a carbon atom of a six-membered aromatic ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/04—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/24—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D213/28—Radicals substituted by singly-bound oxygen or sulphur atoms
    • C07D213/32—Sulfur atoms
    • C07D213/34—Sulfur atoms to which a second hetero atom is attached
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/24—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D213/44—Radicals substituted by doubly-bound oxygen, sulfur, or nitrogen atoms, or by two such atoms singly-bound to the same carbon atom
    • C07D213/52—Sulfur atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/61—Halogen atoms or nitro radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • 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
    • C07D239/26—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 only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • 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
    • C07D239/30—Halogen atoms or nitro radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/04—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
    • C07D295/12—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly or doubly bound nitrogen atoms
    • C07D295/135—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly or doubly bound nitrogen atoms with the ring nitrogen atoms and the substituent nitrogen atoms separated by carbocyclic rings or by carbon chains interrupted by carbocyclic rings

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Epidemiology (AREA)
  • Immunology (AREA)
  • Rheumatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Hematology (AREA)
  • Urology & Nephrology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Oncology (AREA)
  • Pain & Pain Management (AREA)
  • Cardiology (AREA)
  • Vascular Medicine (AREA)
  • Transplantation (AREA)
  • Pulmonology (AREA)
  • Dermatology (AREA)
  • Diabetes (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Pyridine Compounds (AREA)

Claims (29)

1. Spoj, naznačen time, da je odabran od spojeva sljedeće formule, i njegove farmaceutski prihvatljive soli, njegovi hidrati i solvati: [image] gdje: - A je neovisno: [image] - Ar je neovisno fenil, piridinil ili pirimidinil; i p je neovisno cijeli broj od 0 do 3; i gdje: q je neovisno cijeli broj od 0 do 3; i gdje: -RSN je neovisno -H ili zasićeni alifatski C1-4alkil; i gdje: -DQ je neovisno -D1-Q1 ili D2=O; -D1- je neovisno ciklopentan-di-il, cikloheksan-di-il, cikloheptan-di-il, biciklo[3.1.1]heptan-di-il ili biciklo[3.2.1]oktan-di-il, te je po želji supstituiran s jednom ili više skupina -R°; -D2= je neovisno ciklopentan-il-iliden, cikloheksan-il-iliden, cikloheptan-il-iliden, biciklo[3.1.1]heptan-il-iliden ili biciklo[3.2.1]oktan-il-iliden, te je po želji supstituiran s jednom ili više skupina -RD; svaki -RD je neovisno odabran od sljedećih: -F, -Cl, -Br, -I, -RDD, -CF3, -OH, -ORDD, -NH2, -NHRDD i -NRDD; i svaki -RDD je neovisno zasićeni alifatski C1-4alkil; i gdje -Q1 je neovisno odabran od sljedećih: [image] [image] pri čemu: svaki -R1N je neovisno -H, -RCN ili -RCF; svaki -R2N je neovisno -H, -RCN ili -RCF; svaki -RCN je neovisno zasićeni alifatski C1-4alkil; i svaki -RCF ako je prisutan, neovisno je zasićeni alifatski C1-4fluoroalkil; ili: -NR1NR2N je neovisno azetidino, pirolidino, imidazolidino, pirazolidino, piperidino, piperazino, morfolino, tiomorfolino, azepino ili diazepino, od kojih je svaki po želji supstituiran s jednom ili više skupina neovisno odabranih od zasićenog alifatskog C1-4alkila; -R1A je neovisno -H, -RC ili -RF; i -R2A je neovisno -H, -RC ili -RF; ili -R1A i -R2A zajedno tvore zasićenu alifatsku C2-4alkilen-skupinu; -R1B je neovisno -H, -RC ili -RF; i -R2B je neovisno -H, -RC ili -RF; ili -R1B i -R2B zajedno tvore zasićenu alifatsku C2-4alkilen-skupinu; ili -R1B i -R2B zajedno tvore =O; -R3A je neovisno -H, -RC ili -RF; i -R4A je neovisno -H, -RC ili -RF; ili -R3A i -R4A zajedno tvore zasićenu alifatsku C2-4alkilen-skupinu; -R5A je neovisno -H, -RC, -RF ili -RJ; i -R6A je neovisno -H, -RC ili -RF; ili -R5A i -R6A zajedno tvore zasićenu alifatsku C2-4alkilen-skupinu; -R3B je neovisno -H, -RC ili -RF; i -R4B je neovisno -H, -RC ili -RF; ili -R3B i -R4B zajedno tvore zasićenu alifatsku C2-4alkilen-skupinu; -R5B je neovisno -H, -RC, -RF, -OH ili -OR°; i -R6b je neovisno -H, -RC ili -RF; ili -R5B i -R6B zajedno tvore zasićenu alifatsku C2-4alkilen-skupinu; svaki -RC je neovisno zasićeni alifatski C1-4alkil; svaki -RF je neovisno zasićeni alifatski C1-4fluoroalkil; -R° je neovisno zasićeni alifatski C1-4alkil; -RJ je neovisno -NH2, -NHRJN1, -NRJN1 ili -NRJN2RJN3; svaki -RJN1 je neovisno zasićeni alifatski C1-4alkil; i -NRJN2RJN3 je neovisno azetidino, pirolidino, imidazolidino, pirazolidino, piperidino, piperazino, morfolino, tiomorfolino, azepino ili diazepino, od kojih je svaki po želji supstituiran s jednom ili više skupina neovisno odabranih od zasićenog alifatskog C1-4alkila; te pri čemu je svaki -RX neovisno sljedeće: -F, -Cl, -Br, -I, -RXX, -OH, -ORXX, -SH, -SRXX, -CF3, -OCF3, -SCF3, -NH2, -NHRXX, -NRXX –NRYYRZZ, -C(=O)RXX, -OC(=O)RXX, -C(=O)OH, -C(=O)ORXX, -C(=O)NH2, -C(=O)NHRXX, -C(=O)NRXX2, -C(=O)ORYYRZZ, -OC(=O)NH2, -OC(=O)NHRXX, -OC(=O)NRXX2, -OC(=O)NRYYRZZ, -NHC(=O)RXX, -NRXXC(=O)RXX, -NHC(=O)ORXX, -NRXXC(=O)ORXX, -NHC(=O)NH2, -NHC(=O)NHRXX, -NHC(=O)NRXX2, -NHC(=O)NRYYRZZ, -NRXXC(=O)NH2, -NRXXC(=O)NHRXX, -NRXXC(=O)NRXX2, -NRXXC(=O)NRYYRZZ, -CN, -NO2, -S(=O)2NH2, -S(=O)2NHRXX, -S(=O)2NRXX2, -S(=O)2NRYYRZZ, -S(=O)RXX, -S(=O)2RXX, -OS(=O)2RXX, -S(=O)2OH ili -S(=O)2ORXX; gdje: svaki –RXX je neovisno zasićeni alifatski C1-6alkil, fenil ili benzil, pri čemu su navedeni fenil i benzil po želji supstituirani s jednom ili više skupina odabranih od sljedećih: -F, -Cl, -Br, -I, -CF3, -OCF3, -RXXX, -OH, -ORXXX ili -SRXXX, gdje svaki -RXXX je neovisno zasićeni alifatski C1-4alkil; i svaki –NRYYRZZ je neovisno azetidino, pirolidino, imidazolidino, pirazolidino, piperidino, piperazino, morfolino, tiomorfolino, azepino ili diazepino, svaki po želji supstituiran s jednom ili više skupina neovisno odabranih od zasićenog alifatskog C1-4alkila.
2. Spoj prema zahtjevu 1, naznačen time, da: svaki –RX je neovisno sljedeći: -F, -Cl, -Br, -I, -RXX, -OH, -ORXX, -SRXX, -CF3, -OCF3, -CN ili -NO2; i svaki –RXX je neovisno zasićeni alifatski C1-4alkil.
3. Spoj prema zahtjevu 1 ili 2, naznačen time, da -A je neovisno: [image] gdje: =W- je -CH= i -Y= je -CH=; -RX2 je neovisno -H ili –RX2S; -RX4 je neovisno -H ili -RX4S; -RX2S je neovisno –RX-; i -RX4S je neovisno –RX.
4. Spoj prema zahtjevu 1 ili 2, naznačen time, da -A je neovisno: [image] gdje: =W- je -CH= i -Y= je -N=; -RX2 je neovisno -H ili –RX2S; -RX4 je neovisno -H ili -RX4S; -RX2S je neovisno –RX; i -RX4S je neovisno –RX.
5. Spoj prema zahtjevu 3 ili 4, naznačen time, da: -RX2 je neovisno -RX2S; -RX4 je neovisno -RX4S.
6. Spoj prema bilo kojem od zahtjeva 3 do 5, naznačen time, da: -rx2S je neovisno -F, -Cl ili -CF3; i -RX4S je neovisno -F, -Cl ili -CF3.
7. Spoj prema bilo kojem od zahtjeva 3 do 5, naznačen time, da: -RX2S je neovisno -F; i -RX4S je neovisno -F.
8. Spoj prema bilo kojem od zahtjeva 3 do 5, naznačen time, da: -Rx2s je neovisno -Cl; i -Rx4S je neovisno -Cl.
9. Spoj prema bilo kojem od zahtjeva 1 do 8, naznačen time, da vodeća fenilna skupina je: [image] koja je [image] gdje: -RXC1 je neovisno -H ili –RXCC; -RXC2 je neovisno -H; svaki –RXCC je neovisno -F, -Cl ili –RXCCC; i svaki -RXCCC je neovisno -Me ili -Et.
10. Spoj prema zahtjevu 9, naznačen time, da: -RXC1 je neovisno -H; i -RXC2 je neovisno -H.
11. Spoj prema bilo kojem od zahtjeva 1 do 10, naznačen time, da -RSN je neovisno -H.
12. Spoj prema zahtjevu 1, naznačen time, da -DQ je neovisno -D1-Q1.
13. Spoj prema bilo kojem od zahtjeva 1 do 12, naznačen time, da -D1- je neovisno cikloheksan-1,4-di-il.
14. Spoj prema bilo kojem od zahtjeva 1 do 12, naznačen time, da -D1- je neovisno 4-metil- cikloheksan-1,4-di-il.
15. Spoj prema bilo kojem od zahtjeva 1 do 14, naznačen time, da -Q1 je neovisno: [image]
16. Spoj prema bilo kojem od zahtjeva 1 do 14, naznačen time, da -Q1 je neovisno: [image] gdje: -R1A je neovisno -H ili –RC; -R2A je neovisno -H ili –RC; i svaki -RC je neovisno -Me ili -Et.
17. Spoj prema bilo kojem od zahtjeva 1 do 14, naznačen time, da -Q1 je neovisno: [image] gdje: ili: -R1N je neovisno -H ili -RCN; -R2N je neovisno -H ili -RCN; i svaki -RCN je neovisno -Me ili -Et; ili: -NR1NR2N je neovisno pirolidino, piperidino, piperazino ili morfolino, od kojih je svaki po želji supstituiran s jednom ili više skupina odabranih od zasićenog alifatskog C1-4alkila.
18. Spoj prema bilo kojem od zahtjeva 1 do 14, naznačen time, da -Q1 je neovisno: [image] gdje: -R1B je neovisno -H ili -RC; -R2B je neovisno -H ili -RC; i svaki -RC je neovisno -Me ili -Et; i pri čemu: -R1N je neovisno -H ili -RCN; -R2N je neovisno -H ili -RCN; i svaki -RCN je neovisno -Me ili -Et; ili: -NR1NR2N je neovisno pirolidino, piperidino, piperazino ili morfolino, od kojih je svaki po želji supstituiran s jednom ili više skupina neovisno odabranih od zasićenog alifatskog C1-4alkila.
19. Spoj prema zahtjevu 1, naznačen time, da: -A je neovisno: [image] gdje: =W-je -CH= i -Y= je -CH=; -RX2 je neovisno -RX2S; -RX4 je neovisno -RX4S; -R je neovisno -F; i -RX4S je neovisno -F; vodeća fenilen-skupina: [image] je: [image] gdje: -RXC1 je neovisno -H; i -RXC2 je neovisno -H; -RSN je neovisno -H; -DQ je neovisno -D1-Q1; -D1- je neovisno 4-metil-cikloheksan-1,4-di-il; i -Q1 je neovisno: [image]
20. Spoj prema zahtjevu 1, naznačen time, da je odabran od sljedećih spojeva, i njihovih farmaceutski prihvatljivih soli, njihovih hidrata i solvata: [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image]
21. Spoj prema zahtjevu 1, naznačen time, da je to sljedeći spoj ili njegova farmaceutski prihvatljiva sol, njegov hidrat ili solvat: [image]
22. Spoj prema zahtjevu 1, naznačen time, da je to sljedeći spoj ili njegova farmaceutski prihvatljiva sol, njegov hidrat ili solvat: [image]
23. Spoj prema zahtjevu 1, naznačen time, da je to sljedeći spoj ili njegova farmaceutski prihvatljiva sol, njegov hidrat ili solvat: [image]
24. Spoj prema zahtjevu 1, naznačen time, da je to sljedeći spoj ili njegova farmaceutski prihvatljiva sol, njegov hidrat ili solvat: [image]
25. Farmaceutski sastav, naznačen time, da obuhvaća spoj prema bilo kojem od zahtjeva 1 do 24 i farmaceutski prihvatljiv nosač, razrjeđivač ili pomoćno sredstvo.
26. Postupak za proizvodnju farmaceutskog sastava, naznačen time, da obuhvaća spajanje miješanjem spoja prema bilo kojem od zahtjeva 1 do 24 i farmaceutski prihvatljivog nosača, razrjeđivača ili pomoćnog sredstva.
27. Spoj prema bilo kojem od zahtjeva 1 do 24, naznačen time, da se upotrebljava u postupku liječenja ljudskog ili životinjskog tijela pomoću terapije.
28. Spoj prema bilo kojem od zahtjeva 1 do 24, naznačen time, da se upotrebljava u postupku liječenja sljedećih stanja: upalni poremećaj ili autoimuni poremećaj; poremećaj povezan s upalom i/ili s aktiviranjem imunološkog sustava; poremećaj posredovan prekomjernim i/ili neprikladnim i/ili produljenim aktiviranjem imunološkog sustava; upala; poremećaj povezan s upalom ili s aktiviranjem imunološkog sustava; reumatoidni artritis; psorijaza; psorijatički artritis; kronična opstrukcijska plućna bolest (COPD); ateroskleroza; ankilozantni spondilitis; upalna bolest crijeva; imunološka reakcija koja vodi do odbacivanja organa ili usatka nakon transplantacije; tumor koji prekomjerno izražava TNFa, IL-1, RANKL ili NFkB, ili u kojem inhibicija TNFa, IL-1, RANKL ili NFkB, olakšava ili poboljšava djelovanje citotoksičnih tumorocidnih sredstava; hematološka malignost; hematološka malignost povezana s aktiviranjem NFkB, s neprirodnom signalizacijom od NFkB, ili s upalom; višestruki mijelom, leukemija ili limfom; višestruki mijelom, leukemija ili limfom povezan s aktiviranjem NFkB, s neprirodnom signalizacijom od NFkB, ili s upalom; rak čvrstog tumora; rak čvrstog tumora povezan s aktiviranjem NFkB, s neprirodnom signalizacijom od NFkB, ili s upalom; rak mjehura, rak dojke (ženski i/ili muški), rak debelog crijeva, rak bubrega, rak pluća, rak gušterače, rak prostate, rak mozga, rak kože, rak štitnjače ili melanom; rak mjehura, rak dojke (ženski i/ili muški), rak debelog crijeva, rak bubrega, rak pluća, rak gušterače, rak prostate, rak mozga, rak kože, rak štitnjače ili melanom povezan s aktiviranjem NFkB, s neprirodnom signalizacijom od NFkB, ili s upalom; limfoblastični limfom T-stanica, limfom plaštenih stanica ili akutna limfoblastična leukemija; hematološka malignost povezana s deaktiviranjem ili oštećenjem kaspazne indukcije ili s neprirodnom kaspaznom signalizacijom; limfoblastični limfom T-stanica, limfom plaštenih stanica ili akutna limfoblastična leukemija povezana s deaktiviranjem ili oštećenjem kaspazne indukcije ili s neprirodnom kaspaznom signalizacijom; karcinom renalnih stanica, rak dojke (ženski i/ili muški), rak želudca, rak prostate, rak debelog crijeva ili ameloblastom bazalnih stanica; rak čvrstog tumora povezan s deaktiviranjem ili oštećenjem kaspazne indukcije ili s neprirodnom kaspaznom signalizacijom; karcinom renalnih stanica, rak dojke (ženski i/ili muški), rak želudca, rak prostate, rak debelog crijeva ili ameloblastom bazalnih stanica povezan s deaktiviranjem ili oštećenjem kaspazne indukcije ili s neprirodnom kaspaznom signalizacijom; gubitak kostiju; razaranje zglobova; gubitak kostiju povezan s reumatoidnim artritisom, s osteoporozom, s bolesti kostiju povezane s rakom ili s Pagetovom bolesti kostiju; reumatoidni artritis, osteoporoza, bolest kostiju povezana s rakom ili Pagetova bolest kostiju; neoplazija kostiju; ili aseptično opuštanje prostetičkih implantata.
29. Uporaba spoja prema bilo kojem od zahtjeva 1 do 24, naznačena time, da je za proizvodnju lijeka za liječenje sljedećih stanja: upalni poremećaj ili autoimuni poremećaj; poremećaj povezan s upalom i/ili s aktiviranjem imunološkog sustava; poremećaj posredovan prekomjernim i/ili neprikladnim i/ili produljenim aktiviranjem imunološkog sustava; upala; poremećaj povezan s upalom ili s aktiviranjem imunološkog sustava; reumatoidni artritis; psorijaza; psorijatički artritis; kronična opstrukcijska plućna bolest (COPD); ateroskleroza; ankilozantni spondilitis; upalna bolest crijeva; imunološka reakcija koja vodi do odbacivanja organa ili usatka nakon transplantacije; tumor koji prekomjerno izražava TNFα, IL-1, RANKL ili NFkB, ili u kojem inhibicija TNFα, IL-1, RANKL ili NFkB, olakšava ili poboljšava djelovanje citotoksičnih tumorocidnih sredstava; hematološka malignost; hematološka malignost povezana s aktiviranjem NFkB, s neprirodnom signalizacijom od NFkB, ili s upalom; višestruki mijelom, leukemija ili limfom; višestruki mijelom, leukemija ili limfom povezan s aktiviranjem NFkB, s neprirodnom signalizacijom od NFkB, ili s upalom; rak čvrstog tumora; rak čvrstog tumora povezan s aktiviranjem NFkB, s neprirodnom signalizacijom od NFkB, ili s upalom; rak mjehura, rak dojke (ženski i/ili muški), rak debelog crijeva, rak bubrega, rak pluća, rak gušterače, rak prostate, rak mozga, rak kože, rak štitnjače ili melanom; rak mjehura, rak dojke (ženski i/ili muški), rak debelog crijeva, rak bubrega, rak pluća, rak gušterače, rak prostate, rak mozga, rak kože, rak štitnjače ili melanom povezan s aktiviranjem NFkB, s neprirodnom signalizacijom od NFkB, ili s upalom; limfoblastični limfom T-stanica, limfom plaštenih stanica ili akutna limfoblastična leukemija; hematološka malignost povezana s deaktiviranjem ili oštećenjem kaspazne indukcije ili s neprirodnom kaspaznom signalizacijom; limfoblastični limfom T-stanica, limfom plaštenih stanica ili akutna limfoblastična leukemija povezana s deaktiviranjem ili oštećenjem kaspazne indukcije ili s neprirodnom kaspaznom signalizacijom; karcinom renalnih stanica, rak dojke (ženski i/ili muški), rak želudca, rak prostate, rak debelog crijeva ili ameloblastom bazalnih stanica; rak čvrstog tumora povezan s deaktiviranjem ili oštećenjem kaspazne indukcije ili s neprirodnom kaspaznom signalizacijom; karcinom renalnih stanica, rak dojke (ženski i/ili muški), rak želudca, rak prostate, rak debelog crijeva ili ameloblastom bazalnih stanica povezan s deaktiviranjem ili oštećenjem kaspazne indukcije ili s neprirodnom kaspaznom signalizacijom; gubitak kostiju; razaranje zglobova; gubitak kostiju povezan s reumatoidnim artritisom, s osteoporozom, s bolesti kostiju povezane s rakom ili s Pagetovom bolesti kostiju; reumatoidni artritis, osteoporoza, bolest kostiju povezana s rakom ili Pagetova bolest kostiju; neoplazija kostiju; ili aseptično opuštanje prostetičkih implantata.
HRP20150839TT 2008-09-19 2009-09-18 Spojevi aril-fenil-sulfonamido-cikloalkila i njihova uporaba HRP20150839T1 (hr)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US9827108P 2008-09-19 2008-09-19
GBGB0817207.4A GB0817207D0 (en) 2008-09-19 2008-09-19 therapeutic apsac compounds and their use
PCT/GB2009/002221 WO2010032009A1 (en) 2008-09-19 2009-09-18 Aryl-phenyl-sulfonamido-cycloalkyl compounds and their use
EP09785121.6A EP2344449B1 (en) 2008-09-19 2009-09-18 Aryl-phenyl-sulfonamido-cycloalkyl compounds and their use

Publications (1)

Publication Number Publication Date
HRP20150839T1 true HRP20150839T1 (hr) 2015-09-11

Family

ID=39951895

Family Applications (1)

Application Number Title Priority Date Filing Date
HRP20150839TT HRP20150839T1 (hr) 2008-09-19 2009-09-18 Spojevi aril-fenil-sulfonamido-cikloalkila i njihova uporaba

Country Status (14)

Country Link
US (5) US8435968B2 (hr)
EP (1) EP2344449B1 (hr)
JP (1) JP5771524B2 (hr)
CA (1) CA2736971C (hr)
CY (1) CY1116650T1 (hr)
DK (1) DK2344449T3 (hr)
ES (1) ES2544511T3 (hr)
GB (1) GB0817207D0 (hr)
HR (1) HRP20150839T1 (hr)
PL (1) PL2344449T3 (hr)
PT (1) PT2344449E (hr)
SI (1) SI2344449T1 (hr)
SM (1) SMT201500218B (hr)
WO (1) WO2010032009A1 (hr)

Families Citing this family (19)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB0705400D0 (en) * 2007-03-21 2007-05-02 Univ Aberdeen Therapeutic compounds andm their use
GB0817207D0 (en) 2008-09-19 2008-10-29 Pimco 2664 Ltd therapeutic apsac compounds and their use
GB0817208D0 (en) 2008-09-19 2008-10-29 Pimco 2664 Ltd Therapeutic apsap compounds and their use
US8394858B2 (en) 2009-12-03 2013-03-12 Novartis Ag Cyclohexane derivatives and uses thereof
JP6088491B2 (ja) 2012-04-10 2017-03-01 大日本住友製薬株式会社 新規１位置換インダゾール誘導体
GB201311361D0 (en) * 2013-06-26 2013-08-14 Pimco 2664 Ltd Compounds and their therapeutic use
LT3262028T (lt) 2014-12-17 2022-01-10 Pimco 2664 Limited N-(4-hidroksi-4-metil-cikloheksil)-4-fenil-benzensulfonamido ir n-(-4-hidroksi-4-metil-cikloheksil)-4-(2-piridil)-benzensulfonamido junginiai ir jų terapinis panaudojimas
CN116854630A (zh) 2018-02-16 2023-10-10 吉利德科学公司 用于制备可用于治疗逆转录病毒科病毒感染的治疗性化合物的方法和中间体
CA3216031A1 (en) 2018-07-16 2020-01-23 Gilead Sciences, Inc. Capsid inhibitors for the treatment of hiv
GB201813312D0 (en) 2018-08-15 2018-09-26 Modern Biosciences Ltd Compounds and their therapeutic use
GB201905520D0 (en) * 2019-04-18 2019-06-05 Modern Biosciences Ltd Compounds and their therapeutic use
TWI854067B (zh) 2019-11-26 2024-09-01 美商基利科學股份有限公司 預防hiv之蛋白殼抑制劑
TW202412779A (zh) 2021-12-03 2024-04-01 美商基利科學股份有限公司 用於hiv病毒感染之治療性化合物
EP4440700A1 (en) 2021-12-03 2024-10-09 Gilead Sciences, Inc. Therapeutic compounds for hiv virus infection
EP4431090A1 (en) 2023-03-15 2024-09-18 Istesso 1 Limited Solfonamides acting as mitochondrial complex i modulator compounds
GB202308547D0 (en) 2023-06-08 2023-07-26 Istesso 2 Ltd Tnf inhibitor combination therapies
GB202309515D0 (en) 2023-06-23 2023-08-09 Istesso 2 Ltd JAK inhibitor and IL-6 inhibitor combination therapies
GB202315822D0 (en) 2023-10-16 2023-11-29 Istesso 3 Ltd Anti-fibrotic combination therapeutics
GB202317050D0 (en) 2023-11-07 2023-12-20 Istesso 2 Ltd Disease modifying anti-rheumatic drug combination therapies

Family Cites Families (67)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB597810A (en) 1943-04-12 1948-02-04 Gen Printing Ink Corp Improvements in or relating to derivatives of diphenyl
DE1046220B (de) 1956-04-21 1958-12-11 Bayer Ag Verfahren zur Herstellung von Monoazofarbstoffen und deren Metallkomplexverbindungen
US4119784A (en) 1977-07-01 1978-10-10 American Cyanamid Company Anionic substituted sulfonamido biphenyls
DE3000519A1 (de) 1979-02-01 1980-08-14 Byk Gulden Lomberg Chem Fab Sulfonamido-alkansaeuren, ihre verwendung und herstellung sowie sie enthaltende arzneimittel
DE3535167A1 (de) 1985-10-02 1987-04-09 Boehringer Mannheim Gmbh Neue sulfonyl-phenyl(alkyl)amine, verfahren zu ihrer herstellung sowie arzneimittel
IL118325A0 (en) 1995-05-25 1996-10-31 Pont Merck And Pharmaceutical Integrin receptor antagonists and pharmaceutical compositions containing them
WO1997016433A1 (en) 1995-10-30 1997-05-09 Smithkline Beecham Corporation Protease inhibitors
US5760028A (en) 1995-12-22 1998-06-02 The Dupont Merck Pharmaceutical Company Integrin receptor antagonists
JP2001527513A (ja) 1996-03-15 2001-12-25 デュポン ファーマシューティカルズ カンパニー スピロ環インテグリン阻害剤
NZ333825A (en) 1996-07-22 2000-10-27 Monsanto Co Metalloprotease inhibitors particularly MMP-13
IL129147A0 (en) 1996-10-16 2000-02-17 American Cyanamid Co The preparation and use of ortho-sulfonamide aryl hydroxamic acids as matrix metalloproteinase and tace inhibitors
AU5362998A (en) 1996-11-27 1998-06-22 Du Pont Pharmaceuticals Company Novel integrin receptor antagonists
WO1998043962A1 (en) 1997-03-28 1998-10-08 Du Pont Pharmaceuticals Company Heterocyclic integrin inhibitor prodrugs
CN1255119A (zh) 1997-05-08 2000-05-31 史密丝克莱恩比彻姆公司 蛋白酶抑制剂
DE59802394D1 (de) 1997-05-09 2002-01-24 Hoechst Ag Substituierte Diaminocarbonsäuren
DE19719621A1 (de) 1997-05-09 1998-11-12 Hoechst Ag Sulfonylaminocarbonsäuren
US6291425B1 (en) 1999-09-01 2001-09-18 Guilford Pharmaceuticals Inc. Compounds, methods and pharmaceutical compositions for treating cellular damage, such as neural or cardiovascular tissue damage
YU47200A (sh) 1998-01-23 2002-11-15 Aventis Pharma Deutschland Gmbh. Novi derivati sulfonamida kao inhibitori koštane resorpcije i kao inhibitori ćelijske adhezije
CN1195735C (zh) 1998-02-04 2005-04-06 诺瓦提斯公司 抑制使基质退化的金属蛋白酶的磺酰氨基衍生物
JPH11246527A (ja) 1998-03-02 1999-09-14 Shionogi & Co Ltd Ｍｍｐ−８阻害剤
DE19815547C1 (de) 1998-04-07 1999-12-02 Joachim Schmidt Haftmittel für Zahnprothesen
EP0960882A1 (en) 1998-05-19 1999-12-01 Hoechst Marion Roussel Deutschland GmbH Thienyl substituted acylguanidines as inhibitors of bone resorption and vitronectin receptor antagonists
MXPA02009309A (es) 2000-03-21 2003-03-12 Procter & Gamble Inhibidores de las metaloproteasas n-sustituidas que contienen cadenas laterales carboxiclicas.
AU2001264595A1 (en) 2000-05-19 2001-12-03 Guilford Pharmaceuticals Inc. Sulfonamide and carbamide derivatives of 6(5h)phenanthridinones and their uses
WO2002060867A2 (en) 2001-01-29 2002-08-08 Insight Strategy And Marketing Ltd Carbazole derivatives and their uses as heparanase inhibitors
JPWO2002074298A1 (ja) 2001-03-21 2004-07-08 小野薬品工業株式会社 Ｉｌ−６産生阻害剤
US6849635B2 (en) 2001-05-07 2005-02-01 Smithkline Beecham Corporation Sulfonamides
CN101284773A (zh) 2001-08-09 2008-10-15 小野药品工业株式会社 羧酸衍生物及以它为活性成分的药剂
HU227543B1 (en) * 2001-09-28 2011-08-29 Richter Gedeon Nyrt N-[4-(2-piperazin- and 2-piperidin-1-yl-ethyl)-cyclohexyl]-sulfon- and sulfamides, process for their preparation, their use and pharmaceutical compositions containing them
GB0126157D0 (en) 2001-10-31 2002-01-02 Univ Aberdeen Therapeutic compounds
WO2003080042A1 (fr) 2002-03-27 2003-10-02 Shionogi & Co., Ltd. Inhibiteur de decomposition pour matrice extracellulaire de cartilage
DE10228103A1 (de) 2002-06-24 2004-01-15 Bayer Cropscience Ag Fungizide Wirkstoffkombinationen
DK1537116T3 (da) 2002-09-04 2010-09-27 Schering Corp Pyrazolopyrimidiner egnede til behandling af cancersygdomme
DE10251170A1 (de) 2002-10-31 2004-05-13 Boehringer Ingelheim Pharma Gmbh & Co. Kg Neue Beta-Agonisten, Verfahren zu deren Herstellung und deren Verwendung als Arzneimittel
WO2004073619A2 (en) 2003-02-14 2004-09-02 Smithkline Beecham Corporation Ccr8 antagonists
ATE380025T1 (de) 2003-05-07 2007-12-15 Univ Aberdeen Ketone und reduzierte ketone als therapeutische mittel zur behandlung von knochenerkrankungen
WO2004106290A1 (ja) 2003-05-14 2004-12-09 Kissei Pharmaceutical Co., Ltd. アミノアルコール誘導体、それを含有する医薬組成物およびそれらの用途
US7563748B2 (en) 2003-06-23 2009-07-21 Cognis Ip Management Gmbh Alcohol alkoxylate carriers for pesticide active ingredients
TW200530157A (en) 2003-09-09 2005-09-16 Japan Tobacco Inc Dipeptidyl peptidase iv inhibitor
GB0324792D0 (en) 2003-10-23 2003-11-26 Sterix Ltd Compound
EA200600990A1 (ru) 2003-12-19 2006-10-27 Пфайзер Инк. Производные бензосульфониламинопиридин-2-ила и родственные соединения в качестве ингибиторов 11-бета-гидроксистероид-дегидрогеназы 1 типа (11-бета-hsd-1) для лечения диабета и ожирения
WO2005080367A1 (en) 2004-02-12 2005-09-01 Pharmagene Laboratories Limited Ep2 receptor agonists
GB0405193D0 (en) 2004-03-08 2004-04-21 Medical Res Council Compounds
KR20070046025A (ko) * 2004-03-22 2007-05-02 써던 리서취 인스티튜트 매트릭스 메탈로프로테이나제의 비펩티드 억제제
WO2005105712A1 (en) 2004-05-05 2005-11-10 Novo Nordisk A/S Sulfonamide derivatives
GB0412553D0 (en) 2004-06-04 2004-07-07 Univ Aberdeen Therapeutic agents for the treatment of bone conditions
US7470722B2 (en) 2004-06-10 2008-12-30 Kalypsys, Inc. Multicyclic sulfonamide compounds as inhibitors of histone deacetylase for the treatment of disease
WO2006000020A1 (en) 2004-06-29 2006-01-05 European Nickel Plc Improved leaching of base metals
US20090093485A1 (en) 2004-10-29 2009-04-09 Astrazeneca Ab Novel Sulphonamide Derivatives as Glucocorticoid Receptor Modulators for the Treatment of Inflammatory Diseases
EP1659113A1 (en) 2004-11-08 2006-05-24 Evotec AG Inhibitors of 11beta-hydroxy steroid dehydrogenase type 1 (11beta-HSD1)
CA2610903A1 (en) 2005-06-16 2006-12-21 Pfizer Inc. N-(pyridin-2-yl)-sulfonamide derivatives
DE602006020138D1 (de) 2005-06-29 2011-03-31 Compumedics Ltd Sensoranordnung mit leitfähiger brücke
WO2007008541A2 (en) 2005-07-08 2007-01-18 Kalypsys, Inc. Cellular cholesterol absorption modifiers
TW200720261A (en) 2005-08-31 2007-06-01 Sankyo Co Phenylene derivatives
HUE032640T2 (en) 2005-11-08 2017-10-30 Vertex Pharma Heterocyclic modulator of ATP-binding cassette transcripts
EP1984344B1 (en) 2005-12-29 2012-09-26 Lexicon Pharmaceuticals, Inc. Multicyclic amino acid derivatives and methods of their use
EP2035372A1 (en) * 2006-06-29 2009-03-18 Arena Pharmaceuticals, Inc. Modulators of the histamine h3-receptor useful for the treatment of disorders related thereto
TW200801513A (en) 2006-06-29 2008-01-01 Fermiscan Australia Pty Ltd Improved process
EP2069312B1 (en) * 2006-07-25 2012-11-07 Cephalon, Inc. Pyridizinone derivatives
US7560597B2 (en) 2007-03-08 2009-07-14 The University Court Of The University Of Aberdeen 2′,4′-dichloro-biphenyl-4-yl-hydroxy-ketones and related compounds and their use as therapeutic agents
GB0705400D0 (en) 2007-03-21 2007-05-02 Univ Aberdeen Therapeutic compounds andm their use
WO2010000020A1 (en) 2008-06-30 2010-01-07 Cathrx Ltd A catheter
WO2010025235A1 (en) 2008-08-29 2010-03-04 Regents Of The University Of Michigan Selective ligands for the dopamine 3 (d3) receptor and methods of using the same
TWI453207B (zh) 2008-09-08 2014-09-21 Signal Pharm Llc 胺基三唑并吡啶，其組合物及使用其之治療方法
GB0817207D0 (en) 2008-09-19 2008-10-29 Pimco 2664 Ltd therapeutic apsac compounds and their use
GB0817208D0 (en) 2008-09-19 2008-10-29 Pimco 2664 Ltd Therapeutic apsap compounds and their use
GB201311361D0 (en) 2013-06-26 2013-08-14 Pimco 2664 Ltd Compounds and their therapeutic use

Also Published As

Publication number Publication date
US9050329B1 (en) 2015-06-09
WO2010032009A1 (en) 2010-03-25
US20150141472A1 (en) 2015-05-21
US20150266815A1 (en) 2015-09-24
US9616037B2 (en) 2017-04-11
JP5771524B2 (ja) 2015-09-02
US8822507B2 (en) 2014-09-02
ES2544511T3 (es) 2015-08-31
EP2344449A1 (en) 2011-07-20
US20130245018A1 (en) 2013-09-19
US8435968B2 (en) 2013-05-07
JP2012502964A (ja) 2012-02-02
US20160206578A1 (en) 2016-07-21
EP2344449B1 (en) 2015-05-13
DK2344449T3 (en) 2015-08-17
SI2344449T1 (sl) 2015-09-30
US9302984B2 (en) 2016-04-05
CY1116650T1 (el) 2017-03-15
US20110172189A1 (en) 2011-07-14
GB0817207D0 (en) 2008-10-29
CA2736971A1 (en) 2010-03-25
SMT201500218B (it) 2015-10-30
PL2344449T3 (pl) 2015-10-30
CA2736971C (en) 2017-06-20
PT2344449E (pt) 2015-09-16

Similar Documents

Publication Publication Date Title
HRP20150839T1 (hr) Spojevi aril-fenil-sulfonamido-cikloalkila i njihova uporaba
JP2012502964A5 (hr)
JP2012502965A5 (hr)
JP6703632B2 (ja) 細胞傷害性ベンゾジアゼピン誘導体
AU2022200542B2 (en) Inositol derivatives for use in pathological crystallization
HRP20160183T1 (hr) Arilamidi bifenil-4-il-sulfonske kiseline i njihova uporaba kao terapeutskih sredstava
JP2020508302A5 (hr)
TW200510394A (en) Heterocyclic compounds for preventing and treating disorders associated with excessive bone loss
US20150315193A1 (en) Cytotoxic benzodiazepine derivatives
JP2007530526A5 (hr)
JP2019513809A5 (hr)
TOI The radiologic findings in synovial chondromatosis (chondrometaplasia) of the temporomandibular joint
TW201808936A (zh) 吡咯并苯并二氮呯類及其共軛物
RU2017139515A (ru) Фармацевтически активные соединения в качестве ингибиторов рецепторной тирозинкиназы семейства там
WO2014134483A2 (en) Conjugates comprising cell-binding agents and cytotoxic agents
JP2005511556A5 (hr)
JP2012532879A5 (hr)
Vélez et al. High affinity zoledronate-based metal complex nanocrystals to potentially treat osteolytic metastases
CA2424884A1 (en) Substituted (e)-styryl benzylsulfones for treating proliferative disorders
AU2019206132B2 (en) Cytotoxic benzodiazepine derivatives
CN104086763A (zh) 用作表面活性剂的含氨基双膦酸盐修饰Brij化合物及其制备方法
WO2013005154A1 (en) Anticancer agent
Khaled et al. Treatment of malignant colonic obstruction with self-expanding metallic stents
NZ750974A (en) Antibody and checkpoint inhibitor combination therapy
NZ750974B2 (en) Antibody and checkpoint inhibitor combination therapy