ME01507B - Imidazotriazini i imidazopirimidini kao inhibitori kinaze - Google Patents
Imidazotriazini i imidazopirimidini kao inhibitori kinazeInfo
- Publication number
- ME01507B ME01507B MEP-2013-35A MEP3513A ME01507B ME 01507 B ME01507 B ME 01507B ME P3513 A MEP3513 A ME P3513A ME 01507 B ME01507 B ME 01507B
- Authority
- ME
- Montenegro
- Prior art keywords
- imidazo
- quinolin
- ylcyclopropyl
- pyrimidin
- benzamide
- Prior art date
Links
Classifications
-
- 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
-
- 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
- A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
- A61K31/19—Carboxylic acids, e.g. valproic acid
- A61K31/195—Carboxylic acids, e.g. valproic acid having an amino group
- A61K31/197—Carboxylic acids, e.g. valproic acid having an amino group the amino and the carboxyl groups being attached to the same acyclic carbon chain, e.g. gamma-aminobutyric acid [GABA], beta-alanine, epsilon-aminocaproic acid or pantothenic acid
- A61K31/198—Alpha-amino acids, e.g. alanine or edetic acid [EDTA]
-
- 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
- A61K31/47—Quinolines; Isoquinolines
- A61K31/4709—Non-condensed quinolines and containing further heterocyclic 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
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic 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
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/53—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
-
- 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
- A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
-
- 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
- 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
- A61P19/00—Drugs for skeletal disorders
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- 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
- A61P35/00—Antineoplastic agents
- A61P35/04—Antineoplastic agents specific for metastasis
-
- 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
-
- 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
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/08—Antiallergic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
-
- 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
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Immunology (AREA)
- Epidemiology (AREA)
- Urology & Nephrology (AREA)
- Rheumatology (AREA)
- Oncology (AREA)
- Pulmonology (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Transplantation (AREA)
- Hematology (AREA)
- Pain & Pain Management (AREA)
- Vascular Medicine (AREA)
- Biomedical Technology (AREA)
- Physical Education & Sports Medicine (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Neurosurgery (AREA)
- Gastroenterology & Hepatology (AREA)
- Neurology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Cosmetics (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Claims (66)
1.Spoj formule 1: ili njegova farmaceutski prihvatljiva sol ili njegov predlijek, naznačeni time da: A je N ili CR3; i (a) pri čemu, kada A je N; Cy1 je aril, heteroaril, cykloalkil, ili heterocikloalkil, svaki izborno zamijenjen s 1, 2, 3, 4 ili 5 -W-X-Y-Z; Cy2 je aril, heteroaril, cikloalkil, ili heterokicloalkil, svaki izborno zamijenjen s 1, 2, 3, 4 ili 5 -W’-X’-Y’-Z’; L1 je CH2, CH2CH2, cikloalkilen, O ili S L2 je (CR7R8)r, (CR7R8)s-(cikloalkilen)-(CR7R8)t, (CR7R8)s-(arilen)-(CR7R8)t, (CR7R8)s-(heteroci- kloalkilen)-(CR7R8)t, (CR7R8)s-(heteroarilen)-(CR7R8)t, (CR7R8)sO(CR7R8)t, (CR7R8)sS(CR7R8)t, (CR7R8)sC(O)(CR7R8)t, (CR7R8)sC(O)NR9(CR7R8)t, (CR7R8)sC(O)O(CR7R8)t, (CR7R8)sOC(O)(CR7R8)t, (CR7R8)sOC(O)NR9(CR7R8)t, (CR7R8)sNR9(CR7R8)t, (CR7R8)sNR9C(O)NR9(CR7R8)t, (CR7R8)sS(O) (CR7R8)t, (CR7R8)sS(O)NR7(CR8R9)t, (CR7R8)sS(O)2(CR7R8)t, or (CR7R8)sS(O)2NR9(CR7R8)t, pri čemu je navedeni cikloalkilen, arilen, heterocikloalkilen, ili heteroarilen izborno zamijenjen s 1, 2 ili 3 supstituenta nezavisno odabrana od Cy4, halo, C1-6 alkila, C2-6 alkenila, C2-6 alkinila, C1-6 haloalkila, halosulfanila, CN, NO2, N3, ORa1, SRa1, C(O)Rb1, C(O)NRc1Rd1, C(O)ORa1, OC(O)Rb1, OC(O)NRc1Rd1, NRc1Rd1, NRc1C(O)Rb1, NRc1C(O)NRc1Rd1, NRc1C(O)ORa1, C(=NRg)NRc1Rd1, NRc1C(=NRg)NRc1Rd1, P(Rf1)2, P(ORe1)2, P(O)Re1Rf1, P(O)ORe1ORf1, S(O)Rb1, S(O)NRc1Rd1, S(O)2Rb1, NRc1S(O)2Rb1, i S(O)2NRc1Rd1; R1 je H ili ⎯W"-X"-Y"-Z"; R2 je H, halo, C1-6 alkil, C2-6 alkenil, C2-6 alkinil, C1-6 haloalkil, CN, NO2, ORA, SRA, C(O)RB, C(O)NRCRD, C(O)ORA, OC(O)RB, OC(O)NRCRD, NRCRD, NRCC(O)RB, NRCC(O)NRCRD, NRCC(O)ORA, S(O)RB, S(O)NRCRD, S(O)2RB, NRCS(O)2RB ili S(O)2NRCRD; R3 je H, cikloalkil, aril, heterocikloalkil, heteroaril, halo, C1-6 alkil, C2-6 alkenil, C2-6 alkinil, C1-6 haloalkil, CN, NO2, ORA, SRA, C(O)RB, C(O)NRCRD, C(O)ORA, OC(O)RB, OC(O)NRCRD, NRCRD, NRCC(O)RB, NRCC(O)NRCRD, NRCC(O)ORA, S(O)RB, S(O)NRCRD, S(O)2RB, NRCS(O)2RB i S(O)2NRCRD; gdje je navedeni cikloalkil, aril, heterocikloalkil, heteroaril ili C1-6 alkil izborno zamijenjen s 1,2 ili 3 supstituenta nezavisno odabrana od Cy5, halo, C1-6 alkila, C2-6 alkenila, C2-6 alkinila, C1-6 haloalkila, halosulfanila, CN, NO2, N3, ORa1, SRa1, C(O)Rb1, C(O)NRc1Rd1, C(O)ORa1, OC(O)Rb1, OC(O)NRc1Rd1, NRc1Rd1, NRc1C(O)Rb1, NRc1C(O)NRc1Rd1, NRc1C(O)ORa1, C(=NRg)NRc1Rd1, NRc1C(=NRg)NRc1Rd1, P(Rf1)2, P(ORe1)2, P(O)Re1Rf1, P(O)ORe1ORf1, S(O)Rb1, S(O)NRc1Rd1, S(O)2Rb1, NRc1S(O)2Rb1 i S(O)2NRc1Rd1; ili R2 i ⎯L2-Cy2 su povezani zajedno kako bi formirali skupinu formule: pri čemu je prsten B fuzionirani arilni ili fuzionirani heteroarilni prsten, svaki izborno zamijenjen s 1, 2 ili 3 -W’-X’-Y’-Z’; R4 je nezavisno odabran od H, halo, OH, C1-6 alkila, C2-6 alkenila, C2-6 alkinila, C1-6 alkoksija, alkoksialkila, cianoalkila, heterocikloalkila, cikloalkila, C1-6 haloalkila, CN, i NO2; R7 i R8 su nezavisno odabrani od H, halo, OH, C1-6 alkila, C2-6 alkenila, C2-6 alkinila, C1-6 alkoksija, C1-6 haloalkila, CN i NO2; ili R7 i R8 zajedno s C atomom za koji su povezani formiraju 3, 4, 5, 6 ili 7-člani cikloalkilni ili heterocikloalkilni prsten, svaki izborno zamijenjen s 1, 2 ili 3 supstituenta nezavisno odabrana od halo, OH, C1-6 alkila, C2-6 alkenila, C2-6 alkinila, C1-6 alkoksija, C1-6 haloalkila, CN i NO2; R9 je H, C1-6 alkila, C2-6 alkenila ili C2-6 alkinila; W, W’ i W" su nezavisno odsutni ili nezavisno odabrani od C1-6 alkilena, C2-6 alkenilena, C2-6 alkinilena, O, S, NRh, CO, COO, CONRh, SO, SO2, SONRh i NRhCONRi, pri čemu je svaki od C1-6 alkilena, C2-6 alkenilena i C2-6 alkinilena izborno zamijenjen s 1, 2 ili 3 supstituenta odabrana od halo, C1-6 alkila, C1-6 haloalkila, OH, C1-6 alkoksija, C1-6 haloalkoksija, amina, C1-6 alkilamina i C2-8 dialkilamina; X, X’ i X" su nezavisno odsutni ili nezavisno odabrani od C1-6 alkilena, C2-6 alkenilena, C2-6 alkinilena, arilena, cikloalkilena, heteroarilena i heterocikloalkilena, pri čemu svaki od C1-6 alkilena, C2-6 alkenilena, C2-6 alkinilena, arilena, cikloalkilena, heteroarilena i heterocikloalkilena je izborno zamijenjen s 1, 2 ili 3 supstituenta nezavisno odabrana od halo, CN, NO2, OH, C1-6 alkila, C1-6 haloalkila, C2-8 alkoksialkila, C1-6 alkoksija, C1-6 haloalkoksija, C2-8 alkoksialkoksija, cikloalkila, heterocikloalkila, C(O)ORj, C(O)NRhRi, amina, C1-6 alkilamina i C2-8 dialkilamina; Y, Y’ i Y" su nezavisno odsutni ili nezavisno odabrani od C1-6 alkilena, C2-6 alkenilena, C2-6 alkinilena, O, S, NRh, CO, COO, CONRh, SO, SO2, SONRh, i NRhCONRi, pri čemu je svaki od C1-6 alkilena, C2-6 alkenilena i C2-6 alkinilena izborno zamijenjen s 1, 2 ili 3 supstituenta nezavisno odabrana od halo, C1-6 alkila, C1-6 haloalkila, OH, C1-6 alkoksija, C1-6 haloalkoksija, amina, C1-6 alkilamina i C2-8 dialkilamina; Z, Z’ i Z" su nezavisno odabrani od H, halo, C1-6 alkila, C2-6 alkenila, C2-6 alkinila, C1-6 haloalkila, halosulfanila, CN, NO2, N3, ORa2, SRa2, C(O)Rb2, C(O)NRc2Rd2, C(O)ORa2, OC(O)Rb2, OC(O)NRc2Rd2, NRc2Rd2, NRc2C(O)Rb2, NRc2C(O)NRc2Rd2, NRc2C(O)ORa2, C(=NR9)NRc2Rd2, NRc2C(=NR9)NRc2Rd2, P(Rf2)2, P(ORe2)2, P(O)Re2Rf2, P(O)ORe2ORf2, S(O)Rb2, S(O)NRc2Rd2, S(O)2Rb2, NRc2S(O)2Rb2, S(O)2NRc2Rd2, arila, cikloalkila, heteroarila i heterocikloalkila, gdje su navedeni C1-6 *alkil, C2-6 alkenil, C2-6 alkinil, aril, cikloalkil, heteroaril i heterocikloalkil izborno zamijenjeni s 1, 2, 3, 4 ili 5 supstituenta nezavisno odabrana od halo, C1-6 alkila, C2-6 alkenila, C2-6 alkinila, C1-6 haloalkila, halosulfanila, CN, NO2, N3, ORa2, SRa2, C(O)Rb2, C(O)NRc2Rd2, C(O)ORa2, OC(O)Rb2, OC(O)NRc2Rd2, NRc2Rd2, NRc2C(O)Rb2, NRc2C(O)NRc2Rd2, NRc2C(O)ORa2, C(=NRg)NRc2Rd2, NRc2C(=NRg)NRc2Rd2, P(Rf2)2, P(ORe2)2, P(O)Re2Rf2, P(O)ORe2ORf2, S(O)Rb2, S(O)NRc2Rd2, S(O)2Rb2 , NRc2S(O)2Rb2 i S(O)2NRc2Rd2; pri čemu dva susjedna ⎯W-X-Y-Z, zajedno s atomima s kojima su povezani, izborno formiraju fuzionirani cikloalkilni prsten od 4-20 članova ili fuzionirani heterocikloalkilni prsten od 4-20 članova, svaki izborno zamijenjen s 1, 2 ili 3 supstituenta nezavisno odabrana od halo, C1-6 alkila, C2-6 alkenila, C2-6 alkinila, C1-6 haloalkila, halosulfanila, CN, NO2, ORa3, SRa3, C(O)Rb3, C(O)NRc3Rd3, C(O)ORa3, OC(O)Rb3, OC(O)NRc3Rd3, NRc3Rd3, NRc3C(O)Rb3, NRc3C(O)NRc3Rd3, NRc3C(O)ORa3, C(=NRg)NRc3Rd3, NRc3C(=NRg)NRc3Rd3, S(O)Rb3, S(O)NRc3Rd3, S(O)2Rb3, NRc3S(O)2Rb3, S(O)2NRc3Rd3, arila, cikloalkila, heteroarila i heterocikloalkila; pri čemu dva susjedna ⎯W’-X’-Y’-Z’, zajedno s atomima s kojima su povezani, izborno formiraju fuzionirani cikloalkilni prsten od 4-20 članova ili spojeni heterocikloalkilni prsten od 4-20 članova, svaki izborno zamijenjen s 1, 2 ili 3 supstituenta nezavisno odabrana od halo, C1-6 alkila, C2-6 alkenila, C2-6 alkinila, C1-6 haloalkila, halosulfanila, CN, NO2, ORa3, SRa3, C(O)Rb3, C(O)NRc3Rd3, C(O)ORa3, OC(O)Rb3, OC(O)NRc3Rd3, NRc3Rd3 , NRc3C(O)Rb3, NRc3C(O)NRc3Rd3, NRc3C(O)ORa3, C(=NRg)NRc3Rd3, NRc3C(=NRg)NRc3Rd3, S(O)Rb3, S(O)NRc3Rd3, S(O)2Rb3, NRc3S(O)2Rb3, S(O)2NRc3Rd3, arila, cikloalkila, heteroarila i heterocikloalkila; Cy4 i Cy5 su nezavisno odabrani od arila, cikloalkila, heteroarila i heterocikloalkila, svaki izborno zamijenjen s 1, 2, 3, 4 ili 5 supstituenta nezavisno odabrana od halo, C1-6 alkila, C2-6 alkenila, C2-6 alkinila, C1-6 haloalkila, halosulfanila, CN, NO2, N3, ORa4, SRa4, C(O)Rb4, C(O)NRc4Rd4, C(O)ORa4, OC(O)Rb4, OC(O)NRc4Rd4, NRc4Rd4, NRc4C(O)Rb4, NRc4C(O)NRc4Rd4, NRc4C(O)ORa4, C(=NRg)NRc4Rd4, NRc4C(=NRg)NRc4Rd4, P(Rf4)2, P(OR4)2, P(O)Re4Rf4, P(O)ORe4ORf4, S(O)b4, S(O)NRc4Rd4, S(O)2Rb4, NRc4S(O)2Rb4 i S(O)2NRc4Rd4; RA je H, C1-4 alkil, C2-4 alkenil, C2-4 alkinil, cikloalkil, heterocikloalkil, aril ili heteroaril gdje je navedeni C1-4 alkil, C2-4 alkenil, C2-4 alkinil, cikloalkil, heterocikloalkil, aril ili heteroaril izborno zamijenjen s 1, 2 ili 3 supstituenta nezavisno odabrana od OH, CN, amino, halo i C1-4 alkila; RB je H, C1-4 alkil, C2-4 alkenil, C2-4 alkinil, cicloalkil, heterocikloalkil, aril, ili heteroaril gdje je navedeni C1-4 alkil, C2-4 alkenil, ili C2-4 alkinil, cikloalkil, heterocikloalkil, aril, ili heteroaril izborno zamijenjen s 1, 2 ili 3 supstituenta nezavisno odabrana od OH, CN, amino, halo i C1-4 alkila; RC i RD su nezavisno odabrana od H, C1-4 alkila, C2-4 alkenila, ili C2-4 alkinila, gdje je navedeni C1-4 alkil, C2-4 alkenil, ili C2-4 alkinil izborno zamijenjen s 1, 2 ili 3 supstituenta nezavisno odabrana od OH, CN, amino, halo i C1-4 alkila; ili RC i RD zajedno s N atomom s kojim su povezani formiraju 4-, 5-, 6- ili 7-članu heterocikloalkilnu skupinu ili heteroarilnu skupinu, svaku izborno zamijenjenu s 1, 2 ili 3 supstituenta nezavisno odabrana od OH, CN, amino, halo i C1-4 alkila; Ra, Ra1, Ra2, Ra3, i Ra4 su nezavisno odabrani od H, C1-6 alkila, C1-6 haloalkila, C2-6 alkenila, C2-6 alkinila, arila, cikloalkila, heteroarila, heterocikloalkila, arilalkila, heteroarilalkila, cikloalkilalkila i heterocikloalkilalkila, gdje je navedeni C1-6 alkil, C1-6 haloalkil, C2-6 alkenil, C2-6 alkinil, aril, cikloalkil, heteroaril, heterocikloalkil, arilalkil, heteroarilalkil, cikloalkilalkil, ili heterocikloalkilalkil izborno zamijenjen s 1, 2 ili 3 supstituenta nezavisno odabrana od OH, CN, amino, halo, C1-6 alkila, C1-6 alkoksija, C1-6 haloalkila i C1-6 haloalkoksija; Rb, Rb1, Rb2, Rb3 i Rb4 su nezavisno odabrani od H, C1-6 alkila, C1-6 haloalkila, C2-6 alkenila, C2-6 alkinila, arila, cikloalkila, heteroarila, heterocikloalkila, arilalkila, heteroarilalkila, cikloalkilalkila i heterocikloalkilalkila, pri čemu je navedeni C1-6 alkil, C1-6 haloalkil, C2-6 alkenil, C2-6 alknil, aril, cikloalkil, heteroaril, heterocikloalkil, arilalkil, heteroarilalkil, cikloalkilalkil ili heterocikloalkilalkil izborno zamijenjen s 1, 2 ili 3 supstituenta nezavisno odabrana od OH, CN, amino, halo, C1-6 alkila, C1-6 alkoksija, C1-6 haloalkila i C1-6 haloalkoksija; Rc i Rd su nezavisno odabrani od H, C1-10 alkila, C1-6 haloalkila, C2-6 alkenila, C2-6 alkinila, arila, heteroarila, cikloalkila, heterocikloalkila, arilalkila, heteroarilalkila, cikloalkilalkila ili heterocikloalkilalkila, pri čemu je navedeni C1-10 alkil, C1-6 haloalkil, C2-6 alkenil, C2-6 alkinil, aril, heteroaril, cikloalkil, heterocikloalkil, arilalkil, heteroarilalkil, cikloalkilalkil ili heterocikloalkilalkil izborno zamijenjen s 1, 2 ili 3 supstituenta nezavisno odabrana od OH, CN, amino, halo, C1-6 alkila, C1-6 alkoksija, C1-6 haloalkila i C1-6 haloalkila; ili Rc i Rd zajedno s N atomom s kojim su povezani formiraju 4-, 5-, 6- ili 7-članu heterocikloalkilnu skupinu ili heteroarilnu skupinu, svaku izborno zamijenjenu s 1, 2 ili 3 supstituenta nezavisno odabrana od OH, CN, amino, halo, C1-6 alkila, C1-6 alkoksija, C1-6 haloalkila i C1-6 haloalkoksija; Rc1 i Rd1 su nezavisno odabrani od H, C1-10 alkila, C1-6 haloalkila, C2-6 alkenila, C2-6 alkinila, arila, heteroarila, cicloalkila, heterocikloalkila, arilalkila, heteroarilalkila, cikloalkilalkila ili heterocikloalkilalkila, pri čemu je navedeni C1-10 alkil, C1-6 haloalkil, C2-6 alkenil, C2-6 alkinil, aril, heteroaril, cikloalkil, heterocikloalkil, arilalkil, heteroarilalkil, cicloalkilalkil ili heterocicloalkilalkil izborno zamijenjen s 1, 2 ili 3 supstituenta nezavisno odabrana od OH, CN, amino, halo, C1-6 alkila, C1-6 alkoksija, C1-6 haloalkila, i C1-6 haloalkoksija; ili Rc1 i Rd1 zajedno s N atomom s kojim su povezani formiraju 4-, 5-, 6- ili 7-članu heterocikloalkilnu skupinu ili heteroarilnu skupinu, svaku izborno zamijenjenu s 1, 2 ili 3 supstituenta nezavisno odabrana od OH, CN, amino, halo, C1-6 alkila, C1-6 alkoksija, C1-6 haloalkila i C1-6 haloalkoksija; Rc2 i Rd2 su nezavisno odabrani od H, C1-10 alkila, C1-6 haloalkila, C2-6 alkenila, C2-6 alkinila, arila, heteroarila, cikloalkila, heterocikloalkila, arilalkila, heteroarilalkila, cikloalkilalkila, heterocikloalkilalkila, arilcikloalkila, arilheterocikloalkila, arilheteroarila, biarila, heteroarilcikloalkila, heteroarilheterocikloalkila, heteroarilarila i biheteroarila, pri čemu je navedeni C1-10 alkil, C1-6 haloalkil, C2-6 alkenil, C2-6 alkinil, aril, heteroaril, cikloalkil, heterocikloalkil, arilalkil, heteroarilalkil, cikloalkilalkil, heterocikloalkilalkil, arilcikloalkil, arilheterocikloalkil, arilheteroaril, biaril, heteroarilcikloalkil, heteroarilheterocikloalkil, heteroarilaril i biheteroaril svaki izborno zamijenjen s 1, 2 ili 3 supstituenta nezavisno odabrana od OH, CN, amino, halo, C1-6 alkila, C1-6 alkoksija, C1-6 haloalkila, C1-6 haloalkoksija, hidroksialkila, cianoalkila, arila, heteroarila, C(O)ORa4, C(O)Rb4, S(O)2Rb3,alkoksialkila i alkoksialkoksija; ili Rc2 ili Rd2 zajedno sa N atomom s kojim su povezani formiraju 4-, 5-, 6- ili 7-članu heterocikloalkilnu skupinu ili heteroarilnu skupinu, svaku izborno zamijenjenu s 1, 2 ili 3 supstituenta nezavisno odabrana od OH, CN, amino, halo, C1-6 alkila, C1-6 alkoksija, C1-6 haloalkila, C1-6 haloalkoksija, hidroksialkila, cianoalkila, arila, heteroarila, C(O)ORa4, C(O) Rb4, S(O)2Rb3, alkoksialkila i alkoksialkoksija; Rc3 i Rd3 su nezavisno odabrani od H, C1-10 alkila, C1-6 haloalkila, C2-6 alkenila, C2-6 alkinila, arila, heteroarila, cikloalkila, heterocikloalkila, arilalkila, heteroarilalkila, cikloalkilalkila ili heterocikloalkilalkila, pri čemu je navedeni C1-10 alkil, C1-6 haloalkil, C2-6 alkenil, C2-6 alkinil, aril, heteroaril, cikloalkil, heterocikloalkil, arilalkil, heteroarilalkil, cikloalkilalkil ili heterocikloalkilalkil izborno zamijenjen s 1, 2 ili 3 supstituenta nezavisno odabrana od OH, CN, amino, halo, C1-6 alkila, C1-6 alkoksija, C1-6 haloalkila i C1-6 haloalkoksi; ili Rc3 i Rd3 zajedno s N atomom s kojim su povezani formiraju 4-, 5-, 6- ili 7-članu heterocikloalkilnu skupinu ili heteroarilnu skupinu, svaku izborno zamijenjenu s 1, 2 ili 3 supstituenta nezavisno odabrana od OH, CN, amino, halo, C1-6 alkila, C1-6 alkoksija, C1-6 haloalkila i C1-6 haloalkoksija; Rc4 i Rd4 su nezavisno odabrani od H, C1-10 alkila, C1-6 haloalkila, C2-6 alkenila, C2-6 alkinila, arila, heteroarila, cikloalkila, heterocikloalkila, arilalkila, heteroarilalkila, cikloalkilalkila ili heterocikloalkilalkila, pri čemu je navedeni C1-10 alkil, C1-6 haloalkil, C2-6 alkenil, C2-6 alkinil, aril, heteroaril, cikloalkil, heterocikloalkil, arilalkil, heteroarilalkil, cikloalkilalkil ili heterocikloalkilalkil izborno zamijenjen s 1, 2 ili 3 supstituenta nezavisno odabrana od OH, CN, amino, halo, C1-6 alkila, C1-6 alkoksija, C1-6 haloalkila, i C1-6 haloalkoksija; ili Rc4 i Rd4 zajedno sa N atomom s kojim su povezani formiraju 4-, 5-, 6- ili 7-članu heterocikloalkilnu skupinu ili heteroarilnu skupinu, svaku izborno zamijenjen s 1, 2 ili 3 supstituenta nezavisno odabrana od OH, CN, amino, halo, C1-6 alkila, C1-6 alkoksija, C1-6 haloalkila i C1-6 haloalkoksija; Re, Re1, Re2 i Re4 su nezavisno odabrani od H, C1-6 alkila, C1-6 haloalkila, C2-6 alkenila, (C1-6 alkoksi)-C1-6 alkila, C2-6 alkinila, arila, cikloalkila, heteroarila, heterocikloalkila, arilalkila, cikloalkilalkila, heteroarilalkila i heterocikloalkilalkila; Rf, Rf1, Rf2 i Rf4 su nezavisno odabrani od H, C1-6 alkila, C1-6 haloalkila, C2-6 alkenila, C2-6 alkinila, arila, cikloalkila, heteroarila i heterocikloalkila; Rg je H, CN i NO2; Rh i Ri su nezavisno odabrani od H i C1-6 alkila; Rj je H, C1-6 alkil, C1-6 haloalkil, C2-6 alkenil, C2-6 alkinil, aril, cikloalkil, heteroaril, heterocikloalkil, arilalkil, heteroarilalkil, cikloalkilalkil ili heterocikloalkilalkil; r je 0, 1, 2, 3, 4, 5 ili 6; s je 0, 1, 2, 3 ili 4; i t je 0, 1, 2, 3 ili 4; i (b) pri čemu, kada je A CR3: L’ je cikloalkilen, O ili S; a sve druge varijable su definirane kao pod (a)
2.Spoj prema zahtjevu 1 ili njegova farmaceutski prihvatljiva sol, naznačeni time da A jest N.
3.Spoj prema zahtjevu 1 ili njegova farmaceutski prihvatljiva sol, naznačeni time da A jest CR3.
4.Spoj prema zahtjevu 1 ili njegova farmaceutski prihvatljiva sol, naznačeni time da A jest CH.
5.Spoj prema zahtjevu 1 ili njegova farmaceutski prihvatljiva sol, naznačeni time da Cy1 jest aril ili heteroaril, svaki izborno zamijenjen s 1, 2, 3, 4 ili 5 -W-X-Y-Z.
6.Spoj prema zahtjevu 1 ili njegova farmaceutski prihvatljiva sol, naznačeni time da Cy1 jest aril izborno zamijenjen s 1, 2, 3, 4 ili 5 -W-X-Y-Z.
7.Spoj prema zahtjevu 1 ili njegova farmaceutski prihvatljiva sol, naznačen time da Cy1 jest heteroaril izborno zamijenjen s 1, 2, 3, 4 ili 5 -W-X-Y-Z.
8.Spoj prema zahtjevu 1 ili njegova farmaceutski prihvatljiva sol, naznačeni time da Cy1 jest kinonlinil izborno zamijenjen s 1, 2, 3, 4 ili 5 -W-X-Y-Z.
9.Spoj prema zahtjevu 1 ili njegova farmaceutski prihvatljiva sol, naznačeni time da Cy1 jest kinolinil.
10.Spoj prema zahtjevu 1 ili njegova farmaceutski prihvatljiva sol, naznačeni time da Cy2 jest aril ili heteroaril, svaki izborno zamijenjen s 1, 2, 3, 4 ili 5 -W’-X’-Y’-Z’.
11.Spoj prema zahtjevu 1 ili njegova farmaceutski prihvatljiva sol, naznačeni time da Cy2 jest aril ili heteroaril, svaki izborno zamijenjen s 1, 2, 3, 4 ili 5 -W’-X’-Y’-Z’ pri čemu najmanje jedan od navedenih -W’-X’-Y’-Z’ je C(O)NRc2Rd2.
12.Spoj prema zahtjevu 1 ili njegova farmaceutski prihvatljiva sol, naznačeni time da Cy2 jest aril izborno zamijenjen s 1, 2, 3, 4 ili 5 -W’-X’-Y’-Z’.
13.Spoj prema zahtjevu 1 ili njegova farmaceutski prihvatljiva sol, naznačeni time da Cy2 jest heteroaril izborno zamijenjen s 1, 2, 3, 4 ili 5 -W’-X’-Y’-Z’.
14.Spoj prema zahtjevu 1 ili njegova farmaceutski prihvatljiva sol, naznačeni time da L1 jest O ili S.
15.Spoj prema zahtjevu 1 ili njegova farmaceutski prihvatljiva sol, naznačeni time da L1 jest CH2 ili CH2CH2 ili cikloalkilen.
16.Spoj prema zahtjevu 1 ili njegova farmaceutski prihvatljiva sol, naznačeni time da L1 jest CH2 ili ciklopropilen.
17.Spoj prema zahtjevu 1 ili njegova farmaceutski prihvatljiva sol, naznačeni time da L1 jest cikloalkilen.
18.Spoj prema zahtjevu 1 ili njegova farmaceutski prihvatljiva sol, naznačeni time da L1 jest ciklopropilen.
19.Spoj prema zahtjevu 1 ili njegova farmaceutski prihvatljiva sol, naznačeni time da L2 jest (CR7R8)r.
20.Spoj prema zahtjevu 1 ili njegova farmaceutski prihvatljiva sol, naznačeni time da L2 jest (CR7R8)r i r je 0.
21.Spoj prema zahtjevu 1 ili njegova farmaceutski prihvatljiva sol, naznačeni time da L2 jest (CR7R8)r, (CR7R8)s-(cikloalkilen)-(CR7R8)t, (CR7R8)s-(arilen)-(CR7R8)t,(CR7R8)s-(heterocikloalkilen)-(CR7R8)t ili (CR7R8)s-(heteroarilen)-(CR7R8)t, gdje je navedeni cikloalkilen, arilen, heterocikloalkilen ili heteroarilen izborno zamijenjen s 1, 2 ili 3 supstituenta nezavisno odabrana od Cy4, halo, C1-6 alkila, C2-6 alkenila, C2-6 alkinila, C1-6 haloalkila, halosulfanila, CN, NO2, N3, ORa1, SRa1, C(O)Rb1, C(O)NRc1Rd1, C(O)ORa1, OC(O)Rb1, OC(O)NRc1Rd1, NRc1Rd1, NRc1C(O)Rb1, NRc1C(O)NRc1Rd1, NRc1C(O)ORa1, C(=NRg)NRc1Rd1, NRc1C(=NRg)NRc1Rd1, P(Rf1)2, P(ORe1)2, P(O)Re1Rf1, P(O)ORelORfi, S(O)Rb1, S(O)NRc1Rd1, S(O)2Rb1, NRc1S(O)2Rb1, i S(O)2NRc1Rd1.
22.Spoj prema zahtjevu 1 ili njegova farmaceutski prihvatljiva sol, naznačeni time da L2 jest (CR7R8)r, (CR7R8)s-(cikloalkilen)-(CR7R8)t ili (CR7R8)-(arilen)-(CR7R8)t, gdje je navedeni cikloalkilen ili arilen izborno zamijenjen s 1, 2 ili 3 supstituenta nezavisno odabrana od Cy4, halo, C1-6 alkila, C2-6 alkenila, C2-6 alkinila, C1-6 haloalkila, halosulfanila, CN, NO2, N3, ORa1, SRa1, C(O)Rb1, C(O)NRclRad1, C(O)ORa1, OC(O)Rb1, OC(O)NRc1Rd1, NRc1Rd1, NRc1C(O)Rb1, NRc1C(O)NRc1Rd1, NRc1C(O)ORa1, C(=NRg)NRc1Rd1, NRc1C(=NRg)NRc1Rd1, P(Rf1)2, P(ORe1)2,P(O)Re1Rf1, P(O)ORe1ORf1, S(O)Rb1, S(O)NRc1Rd1, S(O)2Rb1, NRc1S(O)2Rb1 i S(O)2NRc1Rd1.
23.Spoj prema zahtjevu 1 ili njegova farmaceutski prihvatljiva sol, naznačeni time da L2 jest (CR7R8)s-(cikloalkilen)-(CR7R8)t ili (CR7R8)s-(arilen)-(CR7R8)t, gdje je navedeni cikloalkilen ili arilen izborno zamijenjen s 1, 2 ili 3 supstituenta nezavisno odabrana od Cy4, halo, C1-6 alkila, C2-6 alkenila, C2-6 alkinila, C1-6 haloalkila, halosulfanila, CN, NO2, N3, ORa1, SRa1, C(O)Rb1, C(O)NRc1Rd1, C(O)ORa1, OC(O)Rb1, OC(O)NRc1Rd1, NRc1Rd1, NRc1C(O)Rb1, NRc1C(O)NRc1Rd1, NRc1C(O)ORa1, C(=NRg)NRc1Rd1, NRc1C(=NRg)NRc1Rd1, P(Rf1)2, P(ORe1)2, P(O)Re1Rf1. P(O)ORe1ORf1, S(O)Rb1, S(O)NRc1Rd1, S(O)2Rb1, NRc1S(O)2 Rb1 i S(O)2NRc1Rd1.
24.Spoj prema zahtjevu 1 ili njegova farmaceutski prihvatljiva sol, naznačeni time da L2 jest cikloalkilen ili arilen.
25.Spoj prema zahtjevu 1 ili njegova farmaceutski prihvatljiva sol, naznačeni time da L2 jest arilen.
26.Spoj prema zahtjevu 1 ili njegova farmaceutski prihvatljiva sol, naznačeni time da Cy2 jest aril izborno zamijenjen s 1, 2, 3, 4 ili 5 -W’-X’-Y’-Z’.
27.Spoj prema zahtjevu 1 ili njegova farmaceutski prihvatljiva sol, naznačeni time da Cy2 jest heteroaril izborno zamijenjen s 1, 2, 3, 4 ili 5 -W’-X’-Y’-Z’.
28.Spoj prema zahtjevu 1 ili njegova farmaceutski prihvatljiva sol, naznačeni time da Cy2 jest cikloalkil izborno zamijenjen s 1, 2, 3, 4 ili 5 -W’-X’-Y’-Z’.
29.Spoj prema zahtjevu 1 ili njegova farmaceutski prihvatljiva sol, naznačeni time da Cy2 jest heterocikloalkil izborno zamijenjen s 1, 2, 3, 4 ili 5 -W’-X’-Y’-Z’.
30.Spoj prema zahtjevu 1 ili njegova farmaceutski prihvatljiva sol, naznačeni time da R1 jest H.
31.Spoj prema zahtjevu 1 ili njegova farmaceutski prihvatljiva sol, naznačeni time da R2 jest H.
32.Spoj prema zahtjevu 1 ili njegova farmaceutski prihvatljiva sol, naznačeni time da R3 jest H.
33.Spoj prema zahtjevu 1 ili njegova farmaceutski prihvatljiva sol, naznačeni time da R4 jest H.
34.Spoj prema zahtjevu 1 ili njegova farmaceutski prihvatljiva sol, naznačeni time da R7 jest H.
35.Spoj prema zahtjevu 1 ili njegova farmaceutski prihvatljiva sol, naznačeni time da R8 jest H.
36.Spoj prema zahtjevu 1 ili njegova farmaceutski prihvatljiva sol, naznačeni time da R9 jest H.
37.Spoj prema zahtjevu 1 ili njegova farmaceutski prihvatljiva sol, naznačeni time da -W-X-Y-Z jest halo, C1-6 alkil, C2-6 alkenil, C2-6 alkinil, C1-6 haloalkil, halosulfanil, CN, NO2, N3, ORa2, SRa2, C(O)Rb2, C(O)NRc2Rd2, C(O)ORa2, OC(O)Rb2, OC(O)NRc2Rd2, NRc2Rd2, NRc2C(O)Rb2, NRc2C(O)NRc2Rd2, NRc2C(O)ORa2, C(=NRg)NRc2Rd2, NRc2C(=NRg)NRc2Rd2, P(Rf2)2, P(ORe2)2, P(O)Re2Rf2, P(O)ORe2ORf12, S(O)Rb2, S(O)NRc2Rd2, S(O)2Rb2, NRc2S(O)2Rb2, S(O)2NRc2Rd2, aril, cikloalkil, heteroaril i heterocicloalkil, pri čemu je navedeni C1-6 alkil, C2-6 alkenil, C2-6 alkinil, aril, cikloalkil, heteroaril i heterocikloalkil izborno zamijenjen s 1, 2, 3, 4 ili 5 supstituenta nezavisno odabrana od halo, C1-6 alkila, C2-6 alkenila, C2-6 alkinila, C1-6 haloalkila, halosulfanila, CN, NO2, N3, ORa2, SRa2, C(O)Rb2, C(O)NRc2Rd2, C(O)ORa2, OC(O)Rb2, OC(O)NRc2Rd2, NRc2Rd2, NRc2C(O)Rb2, NRc2C(O)NRc2Rd2, NRc2C(O)ORa2, C(=NRg)NRc2Rd2, NRc2C(=NRg)NRc2Rd2, P(Rf2)2, P(ORe2)2, P(O)Re2Rf2, P(O)ORe2ORf2, S(O)Rb2, S(O)NRc2Rd2, S(O)2Rb2,NRc2S(O)2Rb2 i S(O)2NRc2Rd2.
38.Spoj prema zahtjevu 1 ili njegova farmaceutski prihvatljiva sol, naznačeni time da -W-X-Y-Z jest halo, C1-6 alkil, C2-6 alkenil, C2-6 alkinil, C1-6 haloalkil, halosulfanil, CN, NO2, N3, ORa2, SRa2, C(O)Rb2, C(O)NRc2Rd2, C(O)ORa2, OC(O)Rb2, OC(O)NRc2Rd2, NRc2Rd2, NRc2C(O)Rb2, NRc2C(O)NRc2Rd2, NRc2C(O)ORa2, C(=NRg)NRc2Rd2, NRc2C(=NRg)NRc2Rd2, P(Rf2)2, P(ORe2)2, P(O)Re2Rf2, P(O)ORe2ORf2, S(O)Rb2, S(O)NRc2Rd2, S(O)2Rb2, NRc2S(O)2Rb2 ili S(O)2NRc2Rd2.
39.Spoj prema zahtjevu 1 ili njegova farmaceutski prihvatljiva sol, naznačeni time da -W-X-Y-Z jest halo, C1-6 alkil, C1-6 haloalkil, CN, NO2, N3 ili ORa2.
40.Spoj prema zahtjevu 1 ili njegova farmaceutski prihvatljiva sol, naznačeni time da –W-X-Y-Z jest ORa2.
41.Spoj prema zahtjevu 1 ili njegova farmaceutski prihvatljiva sol, naznačeni time da –W-X-Y-Z jest metoksi.
42.Spoj prema zahtjevu 1 ili njegova farmaceutski prihvatljiva sol, naznačeni time da – W’-X’-Y’-Z’ jest halo, C1-6 alkil, C2-6 alkenil, C2-6 alkinil, C1-6 haloalkil, halosulfanil, CN, NO2, N3, ORa2, SRa2, C(O)Rb2, C(O)NRc2Rd2, C(O)ORa2, OC(O)Rb2, OC(O)NRc2Rd2, NRc2Rd2, NRc2C(O)Rb2, NRc2C(O)NRc2Rd2, NRc2C(O)ORa2, C(=NRg)NRc2Rd2, NRc2C(=NRg)NRc2Rd2, P(Rf2)2, P(ORe2)2, P(O)Re2Rf2, P(O)ORe2ORf2, S(O)Rb2, S(O)NRc2Rd2, S(O)2Rb2, NRc2S(O)2Rb2, S(O)2NRc2Rd2, aril, cikloalkil, heteroaril i heterocikloalkil, pri čemu je navedeni C1-6 alkil, C2-6 alkenil, C2-6 alkinil, aril, cikloalkil, heteroaril i heterocikloalkil izborno zamijenjen sa 1, 2, 3, 4 ili 5 supstituenta nezavisno odabrana od halo, C1-6 alkila, C2-6 alkenila, C2-6 alkinila, C1-6 haloalkila, halosulfanila, CN, NO2, N3, ORa2, SRa2, C(O)Rb2, C(O)NRc2Rd2, C(O)ORa2, OC(O)Rb2, OC(O)NRc2Rd2, NRc2Rd2, NRc2C(O)Rb2, NRc2C(O)NRc2Rd2, NRc2C(O)ORa2, C(=NRg)NRc2Rd2, NRc2C(=NRg)NRc2Rd2, P(Rf2)2, P(ORe2)2, P(O)Re2Rf2, P(O)ORe2ORf2, S(O)Rb2, S(O)NRc2Rd2, S(O)2Rb2, NRc2S(O)2Rb2 i S(O)2NRc2Rd2.
43.Spoj prema zahtjevu 1 ili njegova farmaceutski prihvatljiva sol, naznačeni time da –W’-X’-Y’-Z’ jest halo, C1-6 alkil, C2-6 alkenil, C2-6 alkinil, C1-6 haloalkil, halosulfanil, CN, NO2, N3, ORa2, SRa2, C(O)Rb2, C(O)NRc2Rd2, C(O)ORa2, OC(O)Rb2, OC(O)NRc2Rd2, NRc2Rd2, NRc2C(O)Rb2, NRc2C(O)NRc2Rd2, NRc2C(O)ORa2, C(=NRg)NRc2Rd2, NRc2C(=NRg)NRc2Rd2, P(Rf2)2, P(ORe2)2, P(O)Re2Rf2, P(O)ORe2ORf2, S(O)Rb2, S(O)NRc2Rd2, S(O)2Rb2, NRc2S(O)2Rb2 ili S(O)2NRc2Rd2.
44. Spoj prema zahtjevu 1 ili njegova farmaceutski prihvatljiva sol, naznačeni time da –W’-X’-Y’-Z’jest halo, C1-6 alkil, C1-6 haloalkil, CN, NO2, N3, ORa2 ili C(O)NRc2Rd2
45.Spoj prema zahtjevu 1 ili njegova farmaceutski prihvatljiva sol, naznačeni time da -W’-X’-Y’-Z’ jest halo, C1-6 alkil, C1-6 haloalkil, CN, NO2, N3 ili ORa2.
46.Spoj prema zahtjevu 1 ili njegova farmaceutski prihvatljiva sol, naznačeni time da -W’-X’-Y’-Z’ jest halo ili C(O)NRc2Rd2.
47.Spoj prema zahtjevu 1 ili njegova farmaceutski prihvatljiva sol, naznačeni time da imaju formulu IIa ili IIb:
48.Spoj prema zahtjevu 1 ili njegova farmaceutski prihvatljiva sol, naznačeni time da imaju formulu III:
49.Spoj prema zahtjevu 1 ili njegova farmaceutski prihvatljiva sol, naznačeni time da imaju formulu VIII:
50.Spoj prema zahtjevu 1, naznačen time da je odabran od: 2-(4-fluorofenil)-7-(4-metoksibenzil)imidazo[1,2-b] [1,2,4]triazina; 2-(4-fluorofenil)-7-[1-(4-metoksifenil)ciklopropil]imidazo[1,2-b]-[1,2,4]-triazina; 6-(1-(2-(4-fluorofenil)imidazo[1,2-b][1,2,4]triazin-7-il)ciklopropil)kinolina; 6-(4-fluorofenil)-3-(4-metoksibenzil)imidazo[1,2-a]pirimidina; 6-(4-fluorofenil)-3-(1-(4-metoksifenil)ciklopropil)imidazo[1,2-a]pirimidina; 6-(1-(6-(4-fluorofenil)imidazo[1,2-a]pirimidin-3-il)ciklopropil)kinolina; 2-fluoro-N-metil-4-[7-(kinolin-6-ilmetil)imidazo[1,2-b][1,2,4]triazin-2-il]benzamida; 2-(4-bromo-3-fluorofenil)-7-[(4-metoksifenil)tio]imidazo[1,2-b][1,2,4]triazina; 2-fluoro-4-(3-[(4-metoksifenil)tio]imidazo[1,2-a]pirimidin-6-il)-N-metilbenzamida; 2-kloro-4-3-[(4-metoksifenil)tio]imidazo[1,2-a]pirimidin-6-il-N-metilbenzamida; 2-fluoro-N-metil-4-[3-(kinolin-6-ltio)imidazo[1,2-a]pirimidin-6-il]benzamida; 2-kloro-N-metil-4-[3-(kinolin-6-iltio)imidazo[1,2-a]pirimidin-6-il]benzamida; metil-2-fluoro-4-[7-(kinolin-6-iltio)imidazo[1,2-b][1,2,4]triazin-2-il]benzoata; 2-(4-bromo-3-fluorofenil)-7-(4-metoksifenoksi)imidazo[1,2-b][1,2,4]triazina; 3-(4-metoksifenoksi)-6-(4-metil-1H-pirazol-1-il)imidazo[1,2-a]pirimidina; 6-(4-bromofenil)-3-(4-metoksifenoksi)imidazo[1,2-a]pirimidina; 2-kloro-N-metil-4-[3-(kinolin-6-iloksi)imidazo[1,2-a]pirimidin-6-il]benzamida; 2-fluoro-N-metil-4-[3-(1-kinolin-6-ilciklopropil)imidazo[1,2-a]pirimidin-6-il]benzamida; 6-(4-bromofenil)-3-[(4-metoksifenil)tio]imidazo[1,2-a]pirimidina; 2-(4-fluorofenil)-7-[(4-metoksifenil)tio]imidazo[1,2-b][1,2,4]triazina; 6-(1-{6-[3-fluoro-4-(1-metil-2-okso-2-pirolidin-1-iletoksi)fenil]imidazo[1,2-a]pirimidin-3-il}ciklopropil)kinolina; 6-{1-[6-(1H-pirazol-1-il)imidazo[1,2-a]pirimidin-3-il]ciklopropil}kinolina; 6-1-[6-(4-metil-1H-pirazol-1-il)imidazo[1,2-a]pirimidin-3-il]ciklopropil}kinolina; N,N-dimetil-1-[3-(1-kinolin-6-ilciklopropil)imidazo[1,2-a]pirimidin-6-il]-1H-pirazol-4-karboksamida; N-[1-(4-metil-1,3-tiazol-2-il)etil]-1-[3-(1-kinolin-6-ilciklopropil)imidazo[1,2-a]pirimidin-6-il]-1H-pirazol-4-karboksamida; N-cikloheksil-3-(1-kinolin-6-ilciklopropil)imidazo[1,2-a]pirimidin-6-karboksamida; 3-(1-kinolin-6-ilciklopropil)-N-(tetrahidrofuran-2-ilmetil)imidazo[1,2-a]pirimidin-6-karboksamida; N-ciklobutil-4-[3-(1-kinolin-6-ilciklopropil)imidazo[1,2-a]pirimidin-6-il]benzamida; 6-(1-{16-[4-(azetidin-1-ilkarbonil)fenil]imidazo[1,2-a]pirimidin-3-il}ciklopropil)kinolina; N,N-dimetil-4-[3-(1-kinolin-6-ilciklopropil)imidazo[1,2-a]pirimidin-6-il]benzamida; 4-[3-(1-kinolin-6-ilciklopropil)imidazo[1,2-a]pirimidin-6-il]-N-(tetrahidrofuran-2-ilmetil)benzamida; N-(1-benzilpirolidin-3-il)-N-metil-4-[3-(1-kinolin-6-ilciklopropil)imidazo[1,2-a]pirimidin-6-il]benzamida; N-(1-piridin-2-ilpiperidin-4-il)-4-[3-(1-kinolin-6-ilciklopropil)imidazo[1,2-a]pirimidin-6-il]benzamida; N-(1-piridin-2-iletil)-4-[3-(1-kinolin-6-ilcilopropil)imidazo[1,2-a]pirimidin-6-il]benzamida; 6-{1-[6-(4-[(3S)-3-fluoropirolidin-1-il]karbonilfenil)imidazo[1,2-a]pirimidin-3-il]ciklopropil}kinolina; N-[1-(metoksimetil)ciklobutil]-4-[3-(1-kinolin-6-ilciklopropil)imidazo[1,2-a]pirimidin-6-il]benzamida; N-(1-piridin-2-ilpirolidin-3-il)-4-[3-(1-kinolin-6-ilciklopropil)imidazo[1,2-a]pirimidin-6-il]benzamida; 6-[1-(6-{4-[(3-piridin-2-ilpirolidin-1-il)karbonil]fenil}imidazo[1,2-a]pirimidin-3-il)ciklopropil]kinolina; 6-{1-[6-(4-[(3S)-3-(piridin-2-iloksi)pirolidin-1-il]karbonilfenil)imidazo[1,2-a]pirimidin-3-il]ciklopropil}kinolina; N-[2-(piridin-2-iloksi)etil]-4-[3-(1-kinolin-6-ilciklopropil)imidazo[1,2-a]pirimidin-6-il]benzamida; N-[1-metil-2-(piridin-2-iloksi)etil]-4-[3-(1-kinolin-6-ilciklopropil)imidazo[1,2-a]pirimidin-6-il]benzamida; N-(2-fenoksietil)-4-[3-(1-kinolin-6-ilciklopropil)imidazo[1,2-a]pirimidin-6-il]benzamid; N-(1S)-2,2-dimetil-1-[(metilamino)karbonil]propil-4-[3-(1-kinolin-6-ilciklopropil)imidazo[1,2-a]pirimidin-6-il]benzamida; N-(1S)-1-[(dimetilamino)karbonil]-2,2-dimetilpropil-4-[3-(1-kinolin-6-ilciklopropil)imidazo[1,2-a]pirimidin-6-il]benzamida; N-[(1S)-1-(azetidin-1-ilkarbonil)-2,2-dimetilpropil]-4-[3-(1-kinolin-6-ilciklopropil)imidazo[1,2-a]pirimidin-6-il]benzamida; N-ciklopropil-3-[3-(1-kinolin-6-ilciklopropil)imidazo[1,2-a]pirimidin-6-il]benzamida; N-(piridin-2-ilmetil)-3-[3-(1-kinolin-6-ilciklopropil)imidazo[1,2-a]pirimidin-6-il]benzamida; N,N-dimetil-3-[3-(1-kinolin-6-ilciklopropil)imidazo[1,2-a]pirimidin-6-il]benzamida; N-metil-3-[3-(1-kinolin-6-ilciklopropil)imidazo[1,2-a]pirimidin-6-il]benzamida; N-[(1S)-1-metil-2-(metilamino)-2-oksoetil]-4-[3-(1-kinolin-6-ilciklopropil)imidazo[1,2-a]pirimidin-6-il]benzamida; N-[(1R)-1-metil-2-(metilamino)-2-oksoetil]-4-[3-(1-kinolin-6-ilciklopropil)imidazo[1,2-a]pirimidin-6-il]benzamida; (3R)-1-{4-[3-(1-kinolin-6-ilciklopropil)imidazo[1,2-a]pirimidin-6-il]benzoil}pirolidin-3-karbonitrila; metil-4-{5-[3-(1-kinolin-6-ilciklopropil)imidazo[1,2-a]pirimidin-6-il]piridin-2-il}-piperazin-1-karboksilata; 6-[1-(6-{6-[4-(metilsulfonil)piperazin-1-il]piridin-3-il}imidazo[1,2-a]pirimidin-3-il)ciklopropil]kinolina; N,N-dimetil-4-{5-[3-(1-kinolin-6-ilciklopropil)imidazo[1,2-a]pirimidin-6-il]piridin-2-il}piperazin-1-karboksamida; N-(1S)-1-[(dimetilamino)karbonil]-2-metilpropil-4-[3-(1-kinolin-6-ilciklopropil)imidazo[1,2-a]pirimidin-6-il]benzamida; N-1-[(dimetilamino)karbonil]ciklobutil-4-[3-(1-kinolin-6-ilciklopropil)imidazo[1,2-a]pirimidin-6-il]benzamida; N-[(1S)-1-(azetidin-1-ilkarbonil)-2,2-dimetilpropil]-5-[3-(1-kinolin-6-ilciklopropil)imidazo[1,2-a]pirimidin-6-il]piridin-2-karboksamida; N-(1S)-2,2-dimetil-1-[(metilamino)karbonil]propil-5-[3-(1-kinolin-6-ilciklopropil)imidazo[1,2-a]pirimidin-6-il]piridin-2-karboksamida; N-(1S)-1-[(ciklopropilamino)karbonil]-2,2-dimetilpropil-5-[3-(1-kinolin-6-ilciklopropil)imidazo[1,2-a]pirimidin-6-il]piridin-2-karboksamida; N-[(1S)-2-(dimetilamino)-1-metil-2-oksoetil]-5-[3-(1-kinolin-6-ilciklopropil)imidazo[1,2-a]pirimidin-6-il]piridin-2-karboksamida; N-[(1R)-2-(dimetilamino)-1-metil-2-oksoetil]-5-[3-(1-kinolin-6-ilciklopropil)imidazo[1,2-a]pirimidin-6-il]piridin-2-karboksamida; 6-(1-{6-[4-(2-okso-2-pirolidin-1-iletoksi)fenil]imidazo[1,2-a]pirimidin-3-il}ciklopropil)kinolina; 1-{4-[3-(1-kinolin-6-ilciklopropil)imidazo[1,2-a]pirimidin-6-il]fenil}ciklopropankarbonitrila; N,N-dimetil-4-[3-(1-kinolin-6-ilciklopropil)imidazo[1,2-a]pirimidin-6-il]benzensulfonamida; metil-2-fluoro-4-[3-(1-kinolin-6-ilciklopropil)imidazo[1,2-a]pirimidin-6-il]benzilkarbamata; N’-2-fluoro-4[3-(1-kinolin-6-ilciklopropil)imidazo[1,2-a]pirimidin-6-il]benzil-N,N-dimetiluree; (3R)-1-{2-fluoro-4-[3-(1-kinolin-6-ilciklopropil)imidazo[1,2-a]pirimidin-6-il]benzil}pirolidin-3-ola; 6-(1-{6-[3-fluoro-4-(1H-pirazol-1-ilmetil)fenil]imidazo[1,2-a]pirimidin-3-il}ciklopropil)kinolina; 3-{2-fluoro-4-[3-(1-kinolin-6-ilciklopropil)imidazo[1,2-a]pirimidin-6-il]benzil}-1,3-oksazolidin-2-ona; 2-fluoro-N-metil-4-[7-(kinoksalin-6-ilmetil)imidazo[1,2-b][1,2,4]triazin-2-il]benzamida; 6-{1-[6-(4-kloro-1H-pirazol-1-il)imidazo[1,2-a]pirimidin-3-il]ciklopropil}kinolina; 6-{1-[6-(2-metil-1,3-tiazol-4-il)imidazo[1,2-a]pirimidin-3-il]ciklopropil} kinolina; 6-{1-[6-(1,3-tiazol-4-il)imidazo[1,2-a]pirimidin-3-il]ciklopropil}kinolina; 3-fluoro-N-metil-4-[3-(1-kinolin-6-ilciklopropil)imidazo[1,2-a]pirimidin-6-il]benzamida; (3S)-1-{3-fluoro-4-[3-(1-kinolin-6-ilciklopropil)imidazo[1,2-a]pirimidin-6-il]benzoil}pirolidin-3-ola; 2,5-difluoro-N-metil-4-[3-(1-kinolin-6-ilciklopropil)imidazo[1,2-a]pirimidin-6-il]benzamida; 2,5-difluoro-4-[3-(1-kinolin-6-ilciklopropil)imidazo[1,2-a]pirimidin-6-il]benzamida; N-ciklopropil-2,5-difluoro-4-[3-(1-kinolin-6-ilciklopropil)imidazo[1,2-a]pirimidin-6-il]benzamida; 2,5-difluoro-N-(trans-4-hidroksicikloheksil)-4-[3-(1-kinolin-6-ilciklopropil)imidazo[1,2-a]pirimidin-6-il]benzamida; 1-{2-fluoro-4-[3-(1-kinolin-6-ilciklopropil)imidazo[1,2-a]pirimidin-6-il]fenil}pirolidin-2-ona; 3-{2-fluoro-4-[3-(1-kinolin-6-ilciklopropil)imidazo[1,2-a]pirimidin-6-il]fenil}-1,3-oksazolidin-2-ona; etil-4-{4-[3-(1-kinolin-6-ilciklopropil)imidazo[1,2-a]pirimidin-6-il]-1H-pirazol-1-il}piperidin-1-karboksilata; 2-(4-{2-fluoro-4-[3-(1-kinolin-6-ilciklopropil)imidazo[1,2-a]pirimidin-6-il]fenil}-1H-pirazol-1-il)-N,N-dimetilacetamida; 5-{2-fluoro-4-[3-(1-kinolin-6-ilciklopropil)imidazo[1,2-a]pirimidin-6-il]fenil}-N-metilpiridin-2-karboksamida; 5-{2-fluoro-4-[3-(1-kinolin-6-ilciklopropil)imidazo[1,2-a]pirimidin-6-il]fenil}-N,N-dimetilpiridin-2-karboksamida; 6-(1-{6-[3-fluoro-4-(1-metil-1H-pirazol-4-il)fenil]imidazo[1,2-a]pirimidin-3-il}ciklopropil)kinolina; 6-(1-{6-[1-(fetrahidrofuran-3-il)-1H-pirazol-4-il]imidazo[1,2-a]pirimidin-3-il}ciklopropil)kinolina; 6-(1-{6-[1-(1-benzilpirolidin-3-il)-1H-pirazol-4-il]imidazo[1,2-a]pirimidin-3-il}ciklopropil)kinolina; 6-{1-[6-(1-metil-1H-pirazol-4-il)imidazo[1,2-a]pirimidin-3-il]ciklopropil}kinolina; N,N-dimetil-4-{4-[3-(1-kinolin-6-ilciklopropil)imidazo[1,2-a]pirimidin-6-il]-1H-pirazol-1-il}piperidin1-karboksamida; 4-{4-[3-(1-kinolin-6-ilciklopropil)imidazo[1,2-a]pirimidin-6-il]-1H-pirazol-1-il}cikloheksanola; {4-[3-(1-kinolin-6-ilciklopropil)imidazo[1,2-a]pirimidin-6-il]-1H-pirazol-1-il} acetonitrila; N-metil-5-{4-[7-(1-kinolin-6-ilciklopropil)imidazo[1,2-b][1,2,4]triazin-2-il]fenil}piridin-2-karboksamida; 6-{1-[2-(4-pirimidin-5-il-fenil)imidazo[1,2-b][1,2,4]triazin-7-il]ciklopropil}kinolina; 6-(1-{2-[4-(1-acetil-1,2,3,6-tetrahidropiridin-4-il)fenil]imidazo[1,2-b][1,2,4]triazin-7-il}ciklopropil)kinolina; 6-[1-(2-(4-[1-(metilsulfonil)-1,2,3,6-tetrahidropiridin-4-il]fenil}imidazo[1,2-b][1,2,4]triazin-7-il)ciklopropil]kinolina; N,N-dimetil-5-{4-[7-(1-kinolin-6-ilciklopropil)imidazo[1,2-b][1,2,4]triazin-2-il]fenil}piridin-2-karboksamida; 6-(1-{2-[4-(1H-imidazol-1-il)fenil]imidazo[1,2-b][1,2,4]triazin-7-il}ciklopropil)-kinolina; 2-fluoro-N-(trans-4-hidroksicikloheksil)-4-[7-(1-kinolin-6-ilciklopropil)imidazo[1,2-b][1,2,4]triazin-2-il]benzamida; N-ciklopropil-2-fluoro-4-[7-(1-kinolin-6-ilciklopropil)imidazo[1,2-b][1,2,4]triazin-2-il]benzamida; 2-fluoro-N-metil-4-[7-(1-kinolin-6-ilciklopropil)imidazo[1,2-b][1,2,4]triazin-2-il]benzamida; 2-fluoro-N-[1-(metoksimetil)ciklopropil]-4-[7-(1-kinolin-6-ilciklopropil)imidazo[1,2-b][1,2,4]triazin-2-il]benzamida; 2-fluoro-4-(7-(1-(kinolin-6-il)ciklopropil)imidazo[1,2-b][1,2,4]triazin-2-il)benzamida; 4-[7-(1-kinolin-6-ilciklopropil)imidazo[1,2-b][1,2,4]triazin-2-il]-N-(tetrahidrofuran-2-ilmetil)benzamida; N-(piridin-2-ilmetil)-4-[7-(1-kinolin-6-ilciklopropil)imidazo[1,2-b][1,2,4]triazin-2-il]benzamida; N-ciklopropil-4-[7-(1-kinolin-6-ilciklopropil)imidazo[1,2-b][1,2,4]triazin-2-il]benzamida; N-ciklobutil-4-[7-(1-kinolin-6-ilciklopropil)imidazo[1,2-b][1,2,4]triazin-2-il]benzamida; N-(1-piridin-2-ilciklopropil)-4-[7-(1-kinolin-6-ilciklopropil)imidazo[1,2-b][1,2,4]triazin-2-il]benzamida; N-(2-hidroksi-1,1-dimetiletil)-4-[7-(1-kinolin-6-ilciklopropil)imidazo[1,2-b][1,2,4]triazin-2-il]benzamida; N-[(1S)-1-benzil-2-hidroksietil]-4-[7-(1-kinolin-6-ilciklopropil)imidazo[1,2-b][1,2,4]triazin-2-il]benzamida; (3R)-1-{4-[7-(1-kinolin-6-ilciklopropil)imidazo[1,2-b][1,2,4]triazin-2-il]benzoil}pirolidin-3-ola; 4-(7-(1-(kinolin-6-il)ciklopropil)imidazo[1,2-b][1,2,4]triazin-2-il)-N-(tetrahidro-2H-piran-4-il)benzamida; N-ciklopropil-N-metil-4-[7-(1-kinolin-6-ilciklopropil)imidazo[1,2-b][1,2,4]triazin-2-il]benzamida; N-[1-(metoksimetil)ciklopropil]-4-[7-(1-kinolin-6-ilciklopropil)imidazo[1,2-b][1,2,4]triazin-2-il]benzamida; N-[1-(metoksimetil)ciklobutil]-4-[7-(1-kinolin-6-ilciklopropil)imidazo[1,2-b][1,2,4]triazin-2-il]benzamida; N-[(1S)-1-(metoksimetil)-2-metilpropil]-4-[7-(1-kinolin-6-ilciklopropil)imidazo[1,2-b][1,2,4]triazin-2-il]benzamida; N-[4-(metoksimetil)tetrahidro-2H-piran-4-il]-4-[7-(1-kinolin-6-ilciklopropil)imidazo[1,2-b][1,2,4]triazin-2-il]benzamida; 4-[7-(1-kinolin-6-ilciklopropil)imidazo[1,2-b][1,2,4]triazin-2-il]-N-1,3-tiazol-2-ilbenzamida; N-pirimidin-4-il-4-[7-(1-kinolin-6-ilciklopropil)imidazo[1,2-b][1,2,4]triazin-2-il]benzamida; N-[4-(metoksimetil)tetrahidro-2H-piran-4-il]-4-[7-(1-kinolin-6-ilciklopropil)imidazo[1,2-b][1,2,4]triazin-2-il]benzamida; N-ciklopropil-2-fluoro-4-[7-(kinolin-6-ilmetil)imidazo[1,2-b][1,2,4]triazin-2-il]benzamida; 2-fluoro-N-[1-(metoksimetil)ciklopropil]-4-[7-(kinolin-6-ilmetil)imidazo[1,2-b][1,2,4]triazin-2-il]benzamida; 2-fluoro-4-[7-(kinolin-6-ilmetil)imidazo[1,2-b][1,2,4]triazin-2-il]-N-(tetrahidro-2H-piran-4-il)benzamida; (3R)-1-{2-fluoro-4-[7-(kinolin-6-ilmetil)imidazo[1,2-b][1,2,4]triazin-2-il]benzoil}pirolidin-3-ola; 2-fluoro-4-[7-(kinolin-6-ilmetil)imidazo[1,2-b][1,2,4]triazin-2-il]benzamida; 2-fluoro-N-(trans-4-hidroksicikloheksil)-4-[7-(kinolin-6-ilmetil)imidazo[1,2-b][1,2,4]triazin-2-il]benzamida; 6-{2-[3-fluoro-4-(1H-imidazol-1-il)fenil]imidazo[1,2-b][1,2,4]triazin-7-ilmetil}kinolina; 3-{2-fluoro-4-[7-(kinolin-6-ilmetil)imidazo[1,2-b][1,2,4]triazin-2-il]fenil}-1,3-oksazolidin-2-ona; N-(1S)-2,2-dimetil-1-[(metilamino)karbonil]propil-2-fluoro-4-[7-(kinolin-6-ilmetil)imidazo[1,2-b][1,2,4]triazin-2-il]benzamida; N-(1S)-1-[(dimetilamino)karbonil]-2,2-dimetilpropil-2-fluoro-4-[7-(kinolin-6-ilmetil)imidazo[1,2-b] [1,2,4]triazin-2-il]benzamida; N-[(1S)-1-(azetidin-1-ilkarbonil)-2,2-dimetilpropil]-2-fluoro-4-[7-(kinolin-6-ilmetil)imidazo[1,2-b][1,2,4]triazin-2-il]benzamida; N-{(1S)-1-[(dimetilamino)karbonil]-3-metilbutil-2-fluoro-4-[7-(kinolin-6-ilmetil)imidazo[1,2-b][1,2,4]triazin-2-il]benzamida; 2-fluoro-N-{(1R)-3-metil-1-[(metilamino)karbonil]butil}-4-[7-(kinolin-6-ilmetil)imidazo[1,2-b][1,2,4]triazin-2-il]benzamida; N-{(1R)-1-[(dimetilamino)karbonil]-3-metilbutil}-2-fluoro-4-[7-(kinolin-6-ilmetil)imidazo[1,2-b][1,2,4]triazin-2-il]benzamida; N-[(1R)-1-(azetidin-1-ilkarbonil)-3-metilbutil]-2-fluoro-4-[7-(kinolin-6-ilmetil)imidazo[1,2-b][1,2,4] triazin-2-il]benzamida; 3-{4-[7-(kinolin-6-ilmetil)imidazo[1,2-b][1,2,4]triazin-2-il]-1H-pirazol-1-il} propanenitrila; 4-[7-(kinolin-6-ilmetil)imidazo[1,2-b][1,2,4]triazin-2-il]-1H-pirazol-1-ilacetonitrila; 2-{4-[7-(kinolin-6-ilmetil)imidazo[1,2-b][1,2,4]triazin-2-il]-1H-pirazol-1-il}acetamida; metil-4-{4-[7-(kinolin-6-ilmetil)imidazo[1,2-b][1,2,4]triazin-2-il]-1H-pirazol-1-il}piperidin-1-karboksilata; 2-fluoro-N-[(1S,2S)-2-hidroksiciklopentil]-4-[7-(kinolin-6-ilmetil)imidazo[1,2-b][1,2,4]triazin-2-il]benzamida; 2-fluoro-N-(2-hidroksietil)-4-[7-(kinolin-6-ilmetil)imidazo[1,2-b][1,2,4]triazin-2-il]benzamida; 2-fluoro-N-[1-(metoksimetil)ciklobutil]-4-[7-(kinolin-6-ilmetil)imidazo[1,2-b][1,2,4]triazin-2-il]benzamida; 2-fluoro-N-[4-(metoksimetil)tetrahidro-2H-piran-4-il]-4-[7-(kinolin-6-ilmetil)imidazo[1,2-b][1,2,4]triazin-2-il]benzamida; N-(ciklopropilmetil)-2-fluoro-4-[7-(kinolin-6-ilmetil)imidazo[1,2-b][1,2,4]triazin-2-il]benzamida; 2-fluoro-4-[7-(kinolin-6-ilmetil)imidazo[1,2-b][1,2,4]triazin-2-il]-N-(tetrahidro-2H-piran-4-ilmetil)benzamida; N-[2-(dimetilamino)etil]-2-fluoro-4-[7-(kinolin-6-ilmetil)imidazo[1,2-b][1,2,4]triazin-2-il]benzamida; 2-fluoro-N-(2-piperidin-1-iletil)-4-[7-(kinolin-6-ilmetil)imidazo[1,2-b][1,2,4]triazin-2-il]benzamida; 2-fluoro-N-[2-(1-metilpirolidin-2-il)etil]-4-[7-(kinolin-6-ilmetil)imidazo[1,2-b][1,2,4]triazin-2-il]benzamida; 2-fluoro-N-(piridin-2-ilmetil)-4-[7-(kinolin-6-ilmetil)imidazo[1,2-b][1,2,4]triazin-2-il]benzamida; 2-fluoro-N-(piridin-3-ilmetil)-4-[7-(kinolin-6-ilmetil)imidazo[1,2-b][1,2,4]triazin-2-il]benzamida; 2-fluoro-N-(piridin-4-ilmetil)-4-[7-(kinolin-6-ilmetil)imidazo[1,2-b][1,2,4]triazin-2-il]benzamida; 2-fluoro-N-(2-piridin-2-iletil)-4-[7-(kinolin-6-ilmetil)imidazo[1,2-b] [1,2,4]triazin-2-il]benzamida; 2-fluoro-N-(1-piridin-3-iletil)-4-[7-(kinolin-6-ilmetil)imidazo[1,2-b][1,2,4]triazin-2-il]benzamida; 2-fluoro-N-(1-piridin-4-iletil)-4-[7-(kinolin-6-ilmetil)imidazo[1,2-b][1,2,4]triazin-2-il]benzamida; 2-fluoro-N-[(1S)-1-(hidroksimetil)-2,2-dimetilpropil]-4-[7-(kinolin-6-ilmetil)imidazo[1,2-b][1,2,4]triazin-2-il]benzamida; 2-fluoro-N-[1-(hidroksimetil)ciklopentil]-4-[7-(kinolin-6-ilmetil)imidazo[1,2-b][1,2,4]triazin-2-il]benzamida; 2-fluoro-N-(2-metoksi-1-metiletil)-4-[3-(1-kinolin-6-ilciklopropil)imidazo[1,2-a]pirimidin-6-il]benzamida; 6-{1-[6-(3-fluoro-4-[(3S)-3-fluoropirolidin-1-il]karbonilfenil)imidazo[1,2-a]pirimidin-3-il]ciklopropil} kinolina; 2-fluoro-N-(piridin-2-ilmetil)-4-[3-(1-kinolin-6-ilciklopropil)imidazo[1,2-a]pirimidin-6-il]benzamida; 2-fluoro-N-(1-piridin-2-ilciklopropil)-4-[3-(1-kinolin-6-ilciklopropil)imidazo[1,2-a]pirimidin-6-il]benzamida; 2-fluoro-N-(1-piridin-2-ilpirolidin-3-il)-4-[3-(1-kinolin-6-ilciklopropil)imidazo[1,2-a]pirimidin-6-il]benzamida; 2-fluoro-4-[3-(1-kinolin-6-ilciklopropil)imidazo[1,2-a]pirimidin-6-il]-N-[(3R)-tetrahidrofuran-3-il]benzamida; 2-fluoro-4-[3-(1-kinolin-6-ilciklopropil)imidazo[1,2-a]pirimidin-6-il]-N-(tetrahidrofuran-2-ilmetil)benzamida; N-ciklopropil-2-fluoro-4-[3-(1-kinolin-6-ilciklopropil)imidazo[1,2-a]pirimidin-6-il]benzamida; 2-fluoro-N-[(1S)-1-(metoksimetil)-2-metilpropil]-4-[3-(1-kinolin-6-ilcklopropil)imidazo[1,2-a]pirimidin-6-il]benzamida; 2-fluoro-4-[3-(1-kinolin-6-ilciklopropil)imidazo[1,2-a]pirimidin-6-il]benzamida; 2-fluoro-N-metil-N-2-[metil(piridin-2-il)amino]etil-4-[3-(1-kinolin-6-ilciklopropil)imidazo[1,2-a]pirimidin-6-il]benzamida; 2-kloro-N-metil-4-[3-(1-kinolin-6-ilciklopropil)imidazo[1,2-a]pirimidin-6-il]benzamida; 2-kloro-N-ciklopropil-4[3-(1-kinolin-6-ilciklopropil)imidazo[1,2-a]pirimidin-6-il]benzamida; 2-kloro-4-[3-(1-kinolin-6-ilciklopropil)imidazo[1,2-a]pirimidin-6-il]-N-(tetrahidrofuran-3-il)benzamida; 2-kloro-N-(1-piridin-2-iletil)-4-[3-(1-kinolin-6-ilciklopropil)imidazo[1,2-a]pirimidin-6-il]benzamida; 6-(1-{6-[4-(Azetidin-1-ilkarbonil)-3-klorofenil]imidazo[1,2-a]pirimidin-3-il}ciklopropil)kinolina; 2-kloro-N-(1-piridin-2-ilpirolidin-3-il)-4-[3-(1-kinolin-6-ilciklopropil)imidazo[1,2-a]pirimidin-6-il]benzamida; 2-kloro-N-[1-metil-2-(piridin-2-iloksi)etil]-4-[3-(1-kinolin-6-ilciklopropil)imidazo[1,2-a]pirimidin-6-il]benzamida; 2-kloro-N-(1S)-1-[(dimetilamino)karbonil]-2-metilpropil-4-[3-(1-kinolin-6-ilciklopropil)imidazo[1,2-a]pirimidin-6-il]benzamida; 2-ciklopropil-5-[3-(1-kinolin-6-ilciklopropil)imidazo[1,2-a]pirimidin-6-il]izoindolin-1-ona; 2-etil-5-[3-(1-kinolin-6-ilciklopropil)imidazo[1,2-a]pirimidin-6-il]izoindolin-1-ona; 2-(2-metoksi-1-metiletil)-S-[3-(1-kinolin-6-ilciklopropil)imidazo[1,2-a]pirimidin-6-il]izoindolin-1 -ona; 2-(piridin-2-ilmetil)-5-[3-(1-kinolin-6-ilciklopropil)imidazo[1,2-a]pirimidin-6-il]izoindolin-1-ona; 2-metil-5-[3-(1-kinolin-6-ilciklopropil)imidazo[1,2-a]pirimidin-6-il]izoindolin-1-ona; N-etil-1-{4-[3-(1-kinolin-6-ilciklopropil)imidazo[1,2-a]pirimidin-6-il]fenil}ciklopropankarboksamida; N-(1-piridin-2-iletil)-1-{4-[3-(1-kinolin-6-ilciklopropil)imidazo[1,2-a]pirimidin-6-il]fenil}ciklopropankarboksamida; N-[1-metil-2-(piridin-2-iloksi)etil]-1-{4-[3-(1-kinolin-6-ilciklopropil)imidazo[1,2-a]pirimidin-6-il]fenil}ciklopropankarboksamida; 2-{2-fluoro-4-[3-(1-kinolin-6-ilciklopropil)imidazo[1,2-a]pirimidin-6-il]fenil}-2-hidroksi-N-metilacetamida; 2-{2-fluoro-4-[3-(1-kinolin-6-ilciklopropil)imidazo[1,2-a]pirimidin-6-il]fenil}-2-hidroksi-N,N-dimetilacetamida; N-(3-[2-(4-bromo-3-fluorofenil)imidazo[1,2-b][1,2,4]triazin-7-il]metilfenil)-N’-etiluree; 2-(2,3-dihlorofenil)-7-(1-kinolin-6-ilciklopropil)imidazo[1,2-b][1,2,4]triazin-3-amina; 2,3-difluoro-N-metil-4-[3-(1-kinolin-6-ilciklopropil)imidazo[1,2-a]pirimidin-6-il]benzamida; 6-difluoro-N-metil-4-[3-(1-kinolin-6-ilciklopropil)imidazo[1,2-a]pirimidin-6-il]benzamida; 2-fluoro-N-metil-4-[3-(1-kinolin-6-ilciklopropil)imidazo[1,2-a]pirimidin-6-il]benzensulfonamida; N,N-dimetil-2-{3-[3-(1-kinolin-6-ilciklopropil)imidazo[1,2-a]pirimidin-6-il]-1H-pirazol-1-il}acetamida; N-[(1S)-1-(azetidin-1-ilkarbonil)-2,2-dimetilpropil]-2-fluoro-4-[3-(1-kinolin-6-ilciklopropil)imidazo[1,2-a]pirimidin-6-il]benzamida; N-[2-(dimetilamino)-1-metil-2-oksoetil]-2-fluoro-4-[3-(1-kinolin-6-ilciklopropil)imidazo[1,2-a]pirimidin-6-il]benzamida; N-(2-azetidin-1-il-1-metil-2-oksoetil)-2-fluoro-4-[3-(1-kinolin-6-ilciklopropil)imidazo[1,2-a]pirimidin-6-il]benzamida; 2-fluoro-N-2-[(3R)-3-metoksipirolidin-1-il]-1-metil-2-oksoetil-4-[3-(1-kinolin-6-ilciklopropil)imidazo[1,2-a]pirimidin-6-il]benzamida; 2-fluoro-N-[(1-hidroksiciklopropil)metil]-4-[7-(kinolin-6-ilmetil)imidazo[1,2-b][1,2,4]triazin-2-il]benzamida; metil-4-(cijanometil)-4-{4-[7-(kinolin-6-ilmetil)imidazo[1,2-b][1,2,4]triazin-2-il]-1H-pirazol-1-il}piperidin-1-karboksilata; etil-4-(cijanometil)-4-{4-[7-(kinolin-6-ilmetil)imidazo[1,2-b][1,2,4]triazin-2-il]-1H-pirazol-1-il}piperidin-1-karboksilata; (1-acetil-4-{4-[7-(kinolin-6-ilmetil)imidazo[1,2-b] [1,2,4]triazin-2-il]-1H-pirazol-1-il}piperidin-4-il)acetonitrila, ili njihovih farmaceutski prihvatljivih soli.
51.Spoj prema zahtjevu 1, naznačen time da je 2-fluoro-N-metil-4-[7-(kinolin-6-ilmetil)imidazo[1,2-b][1,2,4]triazin-2-il]benzamid ili njegova farmaceutski prihvatljiva sol.
52.Sastav, naznačen time da sadrži spoj bilo kojeg zahtjeva od 1 do 51 ili njegovu farmaceutski prihvatljivu sol i najmanje jedan farmaceutski prihvatljivi nosač.
53.Sastav, naznačen time da sadrži spoj prema zahtjevu 51 ili njegovu farmaceutski prihvatljivu sol i najmanje jedan farmaceutski prihvatljivi nosač.
54.Metoda inhibiranja aktivnosti receptorske ili nereceptorske tirozin-kinaze ex vivo, naznačena time da uključuje dovođenje navedene kinaze u kontakt sa spojem iz bilo kojeg zahtjeva od 1 do 51 ili njegovom farmaceutski prihvatljivom soli.
55.Metoda prema zahtjevu 54, naznačena time da navedena kinaza pripada podfamiliji Met, PDGFR, HER, FLK, Src, Abl ili Jak.
56.Metoda prema zahtjevu 54, naznačena time da je navedena kinaza c-Met, Ron, PDGFR beta, c-kit, EGFR, HER2, KDR, flt-3, Src, Abl, Jak1, Jak2 ili Jak 3 kinaza.
57.Metoda prema zahtjevu 54, naznačena time da je navedena kinaza c-Met.
58.Metoda inhibiranja signalnog puta HGF/c-Met kinaze u stanici ex vivo, naznačena time da uključuje dovođenje navedene stanice u kontakt sa spojem iz bilo kojeg zahtjeva od 1 do 51 ili njegovom farmaceutski prihvatljivom soli.
59.Metoda inhibiranja proliferativne aktivnosti stanice ex vivo, naznačena time da uključuje dovođenje navedene stanice u kontakt sa spojem iz bilo kojeg zahtjeva od 1 do 51 ili njegovom farmaceutski prihvatljivom soli.
60.Spoj prema bilo kojem zahtjevu od 1 do 51 ili njegova farmaceutski prihvatljiva sol, naznačeni time da se upotrebljavaju u inhibiciji rasta tumora kod pacijenata.
61.Spoj prema bilo kojem zahtjevu od 1 do 51 ili njegova farmaceutski prihvatljiva sol, naznačeni time da se upotrebljavaju u inhibiciji metastaze tumora kod pacijenata.
62.Spoj prema bilo kojem zahtjevu od 1 do 51 ili njegova farmaceutski prihvatljiva sol, naznačeni time da se upotrebljavaju u liječenju bolesti kod pacijenta, gdje je navedena bolest povezana s nepravilnom regulacijom signalnog puta HGF/c-MET.
63.Spoj ili njegova farmaceutski prihvatljiva sol prema zahtjevu 62, naznačeni time da se upotrebljavaju u liječenju bolesti pri čemu je navedena bolest rak, ateroskleroza, plućna fibroza, renalna fibroza i regeneracija, bolest jetre, alergijski poremećaj, upalna bolest, autoimuni poremećaj, cerebrovaskularna bolest, kardiovaskularna bolest ili stanje povezano sa transplantacijom organa.
64.Spoj prema bilo kojem zahtjevu od 1 do 51 ili njegova farmaceutski prihvatljiva sol, naznačeni time da se upotrebljavaju u liječenju raka kod pacijenta.
65.Spoj ili njegova farmaceutski prihvatljiva sol prema zahtjevu 64, naznačeni time da se upotrebljavaju u liječenju raka pri čemu je navedeni rak karcinom, mišićnokoštani sarkom, sarkom mekog tkiva ili hematopoetski malignitet.
66.Spoj ili njegova farmaceutski prihvatljiva sol prema zahtjevu 64, naznačeni time da se upotrebljavaju u liječenju raka pri čemu je navedeni rak rak mokraćnog mjehura, rak dojke, rak grlića materice, kolangiokarcinom, rak debelog crijeva, rak jednjaka, rak želuca, rak glave i vrata, rak bubrega, rak jetre, rak pluća, nazofaringealni rak, rak jajnika, rak pankreasa, rak prostate, rak štitne žlijezde, osteosarkom, sinovijalni sarkom, rabdomiosarkom, MFH/fibrosarkom, leiomiosarkom, Kaposijev sarkom, multipli mijelom, limfom, leukemija odraslih T stanica, akutna mijelogena leukemija, kronična mijeloična leukemija, glioblastom, astrocitom, melanom, mezoteliom ili Wilmsov tumor. 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US86084006P | 2006-11-22 | 2006-11-22 | |
| US86145906P | 2006-11-29 | 2006-11-29 | |
| US95723607P | 2007-08-22 | 2007-08-22 | |
| EP07864592A EP2099447B1 (en) | 2006-11-22 | 2007-11-19 | Imidazotriazines and imidazopyrimidines as kinase inhibitors |
| PCT/US2007/085100 WO2008064157A1 (en) | 2006-11-22 | 2007-11-19 | Imidazotriazines and imidazopyrimidines as kinase inhibitors |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ME01507B true ME01507B (me) | 2014-04-20 |
Family
ID=39166437
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| MEP-2016-13A ME02372B (me) | 2006-11-22 | 2007-11-19 | Imidazotriazini i imidazopiramidini kao inhibitori kinaze |
| MEP-2013-35A ME01507B (me) | 2006-11-22 | 2007-11-19 | Imidazotriazini i imidazopirimidini kao inhibitori kinaze |
Family Applications Before (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| MEP-2016-13A ME02372B (me) | 2006-11-22 | 2007-11-19 | Imidazotriazini i imidazopiramidini kao inhibitori kinaze |
Country Status (35)
| Country | Link |
|---|---|
| US (8) | US7767675B2 (me) |
| EP (4) | EP2497470B8 (me) |
| JP (1) | JP5572388B2 (me) |
| KR (2) | KR101532256B1 (me) |
| CN (2) | CN101641093B (me) |
| AR (1) | AR066142A1 (me) |
| AU (1) | AU2007323725B2 (me) |
| CA (1) | CA2669991C (me) |
| CL (1) | CL2007003341A1 (me) |
| CO (1) | CO6210810A2 (me) |
| CR (1) | CR10841A (me) |
| CY (4) | CY1116763T1 (me) |
| DK (3) | DK2099447T3 (me) |
| EA (2) | EA026126B1 (me) |
| EC (1) | ECSP099400A (me) |
| ES (3) | ES2398843T3 (me) |
| FR (1) | FR22C1060I2 (me) |
| GE (1) | GEP20125658B (me) |
| HR (3) | HRP20130106T1 (me) |
| HU (2) | HUE026659T2 (me) |
| IL (4) | IL198716A (me) |
| LT (2) | LT3034075T (me) |
| LU (1) | LUC00293I2 (me) |
| ME (2) | ME02372B (me) |
| MX (1) | MX2009005144A (me) |
| MY (2) | MY188338A (me) |
| NL (1) | NL301209I2 (me) |
| NO (4) | NO346024B1 (me) |
| NZ (1) | NZ577127A (me) |
| PL (3) | PL2099447T3 (me) |
| PT (3) | PT2099447E (me) |
| RS (3) | RS54510B1 (me) |
| SI (3) | SI3034075T1 (me) |
| TW (1) | TWI429432B (me) |
| WO (1) | WO2008064157A1 (me) |
Families Citing this family (146)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TWI630207B (zh) | 2005-12-13 | 2018-07-21 | 英塞特控股公司 | 作為傑納斯激酶(JANUS KINASE)抑制劑之經雜芳基取代之吡咯并〔2,3-b〕吡啶及吡咯并〔2,3-b〕嘧啶 |
| KR20080108539A (ko) | 2006-04-12 | 2008-12-15 | 머크 앤드 캄파니 인코포레이티드 | 피리딜 아미드 t-형 칼슘 채널 길항제 |
| US7683060B2 (en) * | 2006-08-07 | 2010-03-23 | Incyte Corporation | Triazolotriazines as kinase inhibitors |
| KR101532256B1 (ko) | 2006-11-22 | 2015-06-29 | 인사이트 코포레이션 | 키나제 억제제로서의 이미다조트리아진 및 이미다조피리미딘 |
| EP3070090B1 (en) | 2007-06-13 | 2018-12-12 | Incyte Holdings Corporation | Use of salts of the janus kinase inhibitor (r)-3-(4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)-1h- pyrazol-1-yl)-3- cyclopentylpropanenitrile |
| WO2009054984A1 (en) * | 2007-10-24 | 2009-04-30 | Merck & Co., Inc. | Heterocycle phenyl amide t-type calcium channel antagonists |
| UY31676A1 (es) | 2008-02-28 | 2009-09-30 | "derivados de 3-metil-imidiazo-[1,2-b]-piridazina" | |
| WO2009143211A2 (en) | 2008-05-21 | 2009-11-26 | Incyte Corporation | Salts of 2-fluoro-n-methyl-4-[7-(quinolin-6-yl-methyl)- imidazo[1,2-b][1,2,4]triazin-2-yl]benzamide and processes related to preparing the same |
| US20110269740A1 (en) * | 2008-07-02 | 2011-11-03 | Ambit Biosciences Corporation | Jak kinase modulating compounds and methods of use thereof |
| FR2933982A1 (fr) * | 2008-07-18 | 2010-01-22 | Sanofi Aventis | Nouveaux derives imidazo°1,2-a!pyrimidine, leur procede de preparation, leur application a titre de medicaments, compositions pharmaceutiques et nouvelle utilisation notamment comme inhibiteurs de met |
| UY32049A (es) | 2008-08-14 | 2010-03-26 | Takeda Pharmaceutical | Inhibidores de cmet |
| TWI665200B (zh) | 2009-01-15 | 2019-07-11 | 英塞特公司 | 製造jak抑制劑之方法及相關中間化合物 |
| AU2010213192A1 (en) * | 2009-02-13 | 2011-08-04 | Bayer Intellectual Property Gmbh | Fused pyrimidines |
| AR076794A1 (es) | 2009-05-22 | 2011-07-06 | Incyte Corp | Derivados de n-(hetero)aril-pirrolidina de pirazol-4-il-pirrolo [2,3-d]pirimidinas y pirrol-3-il-pirrolo [2,3-d ]pirimidinas como inhibidores de la quinasa janus y composiciones farmaceuticas que los contienen |
| EP3643312A1 (en) | 2009-05-22 | 2020-04-29 | Incyte Holdings Corporation | 3-[4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)-1h-pyrazol-1-yl]octane- or heptane-nitrile as jak inhibitors |
| EP2448938B9 (en) | 2009-06-29 | 2015-06-10 | Incyte Corporation | Pyrimidinones as pi3k inhibitors |
| CA2770873A1 (en) | 2009-08-12 | 2011-02-17 | Novartis Ag | Heterocyclic hydrazone compounds and their uses to treat cancer and inflammation |
| CA2771432A1 (en) * | 2009-08-20 | 2011-02-24 | Novartis Ag | Heterocyclic oxime compounds |
| AR078012A1 (es) | 2009-09-01 | 2011-10-05 | Incyte Corp | Derivados heterociclicos de las pirazol-4-il- pirrolo (2,3-d) pirimidinas como inhibidores de la quinasa janus |
| WO2011075643A1 (en) | 2009-12-18 | 2011-06-23 | Incyte Corporation | Substituted heteroaryl fused derivatives as pi3k inhibitors |
| HUE025504T2 (en) | 2009-12-31 | 2016-02-29 | Hutchison Medipharma Ltd | Certain triazolopyrazines, compositions thereof and methods of use therefor |
| EA025304B1 (ru) * | 2010-02-03 | 2016-12-30 | Инсайт Холдингс Корпорейшн | ИМИДАЗО[1,2-b][1,2,4]ТРИАЗИНЫ В КАЧЕСТВЕ c-Met ИНГИБИТОРОВ |
| EP3050882B1 (en) | 2010-03-10 | 2018-01-31 | Incyte Holdings Corporation | Piperidin-4-yl azetidine derivatives as jak1 inhibitors |
| US8518945B2 (en) * | 2010-03-22 | 2013-08-27 | Hoffmann-La Roche Inc. | Pyrrolopyrazine kinase inhibitors |
| US8410117B2 (en) * | 2010-03-26 | 2013-04-02 | Hoffmann-La Roche Inc. | Imidazopyrimidine derivatives |
| EP2558463A1 (en) * | 2010-04-14 | 2013-02-20 | Incyte Corporation | Fused derivatives as i3 inhibitors |
| PH12012502046A1 (en) * | 2010-04-14 | 2017-07-26 | Array Biopharma Inc | 5,7-substituted~imidazo[1,2-c]pyrimidines as inhibitors of jak kinases |
| ES2715611T3 (es) | 2010-05-17 | 2019-06-05 | Incozen Therapeutics Pvt Ltd | Compuestos novedosos de 3H-imidazo[4,5-b]piridina-3,5-disustituida y 3H-[1,2,3]triazolo[4,5-b]piridina 3,5-disustituida como moduladores de proteína cinasas |
| SG10201503983QA (en) | 2010-05-21 | 2015-06-29 | Incyte Corp | Topical Formulation for a JAK Inhibitor |
| CN103415515B (zh) | 2010-11-19 | 2015-08-26 | 因塞特公司 | 作为jak抑制剂的环丁基取代的吡咯并吡啶和吡咯并嘧啶衍生物 |
| US9034884B2 (en) | 2010-11-19 | 2015-05-19 | Incyte Corporation | Heterocyclic-substituted pyrrolopyridines and pyrrolopyrimidines as JAK inhibitors |
| TW201249844A (en) | 2010-12-20 | 2012-12-16 | Incyte Corp | N-(1-(substituted-phenyl)ethyl)-9H-purin-6-amines as PI3K inhibitors |
| CN103298468A (zh) | 2011-02-01 | 2013-09-11 | 协和发酵麒麟株式会社 | 稠环杂环衍生物 |
| WO2012125629A1 (en) | 2011-03-14 | 2012-09-20 | Incyte Corporation | Substituted diamino-pyrimidine and diamino-pyridine derivatives as pi3k inhibitors |
| US9126948B2 (en) | 2011-03-25 | 2015-09-08 | Incyte Holdings Corporation | Pyrimidine-4,6-diamine derivatives as PI3K inhibitors |
| PE20140832A1 (es) | 2011-06-20 | 2014-07-14 | Incyte Corp | Derivados de azetidinil fenil, piridil o pirazinil carboxamida como inhibidores de jak |
| TW201313721A (zh) | 2011-08-18 | 2013-04-01 | Incyte Corp | 作為jak抑制劑之環己基氮雜環丁烷衍生物 |
| US8883819B2 (en) | 2011-09-01 | 2014-11-11 | Irm Llc | Bicyclic heterocycle derivatives for the treatment of pulmonary arterial hypertension |
| KR102030609B1 (ko) | 2011-09-02 | 2019-10-11 | 인사이트 홀딩스 코포레이션 | Pi3k 억제제로서 헤테로시클릴아민 |
| UA111854C2 (uk) | 2011-09-07 | 2016-06-24 | Інсайт Холдінгс Корпорейшн | Способи і проміжні сполуки для отримання інгібіторів jak |
| AU2012310168B2 (en) | 2011-09-15 | 2015-07-16 | Novartis Ag | 6 - substituted 3 - (quinolin- 6 - ylthio) - [1,2,4] triazolo [4, 3 -a] pyradines as tyrosine kinase |
| CN103030654A (zh) * | 2011-10-09 | 2013-04-10 | 济南赛文医药技术有限公司 | 一种小分子c-Met蛋白激酶抑制剂 |
| AU2012323399A1 (en) * | 2011-10-12 | 2014-05-29 | Array Biopharma Inc. | 5,7-substituted-imidazo[1,2-c]pyrimidines |
| CN104185420B (zh) | 2011-11-30 | 2017-06-09 | 埃默里大学 | 用于治疗或预防逆转录病毒和其它病毒感染的抗病毒jak抑制剂 |
| AR090548A1 (es) | 2012-04-02 | 2014-11-19 | Incyte Corp | Azaheterociclobencilaminas biciclicas como inhibidores de pi3k |
| MX2014011987A (es) * | 2012-04-03 | 2014-11-10 | Novartis Ag | Combinaciones de inhibidores de cinasa de tirosina y su uso. |
| EP3964513A1 (en) | 2012-04-03 | 2022-03-09 | Novartis AG | Combination products with tyrosine kinase inhibitors and their use |
| TW201406761A (zh) | 2012-05-18 | 2014-02-16 | Incyte Corp | 做爲jak抑制劑之哌啶基環丁基取代之吡咯并吡啶及吡咯并嘧啶衍生物 |
| US9611267B2 (en) | 2012-06-13 | 2017-04-04 | Incyte Holdings Corporation | Substituted tricyclic compounds as FGFR inhibitors |
| HK1211476A1 (en) * | 2012-08-16 | 2016-05-27 | Novartis Ag | Combination of pi3k inhibitor and c-met inhibitor |
| PL2919766T3 (pl) | 2012-11-15 | 2021-10-04 | Incyte Holdings Corporation | Postacie dawkowania ruksolitynibu o przedłużonym uwalnianiu |
| US9073921B2 (en) | 2013-03-01 | 2015-07-07 | Novartis Ag | Salt forms of bicyclic heterocyclic derivatives |
| CN105189509B (zh) | 2013-03-06 | 2017-12-19 | 因赛特公司 | 用于制备jak抑制剂的方法及中间体 |
| CN105968115B (zh) * | 2013-04-17 | 2018-11-09 | 上海医药集团股份有限公司 | 喹啉类化合物、其制备方法、中间体、药物组合物和应用 |
| WO2014174478A1 (en) | 2013-04-26 | 2014-10-30 | Novartis Ag | Pharmaceutical combinations of a pkc inhibitor and a c-met receptor tyrosine kinase inhibitor |
| SG10201912203XA (en) | 2013-08-07 | 2020-02-27 | Incyte Corp | Sustained release dosage forms for a jak1 inhibitor |
| US10570204B2 (en) | 2013-09-26 | 2020-02-25 | The Medical College Of Wisconsin, Inc. | Methods for treating hematologic cancers |
| GB201321736D0 (en) * | 2013-12-09 | 2014-01-22 | Ucb Pharma Sa | Therapeutic agents |
| GB201321732D0 (en) | 2013-12-09 | 2014-01-22 | Ucb Pharma Sa | Therapeutic agents |
| ES2716685T3 (es) | 2014-01-24 | 2019-06-14 | Dana Farber Cancer Inst Inc | Moléculas de anticuerpo para PD-1 y usos de las mismas |
| DK3099717T3 (da) | 2014-01-31 | 2019-07-01 | Novartis Ag | Antistofmolekyler med tim-3 og anvendelser deraf |
| PE20161573A1 (es) | 2014-02-13 | 2017-01-19 | Incyte Corp | Ciclopropilamina como inhibidor de la lsd1 |
| WO2015123437A1 (en) | 2014-02-13 | 2015-08-20 | Incyte Corporation | Cyclopropylamines as lsd1 inhibitors |
| EP3392244A1 (en) | 2014-02-13 | 2018-10-24 | Incyte Corporation | Cyclopropylamines as lsd1 inhibitors |
| US9493450B2 (en) | 2014-02-13 | 2016-11-15 | Incyte Corporation | Cyclopropylamines as LSD1 inhibitors |
| TWI777174B (zh) | 2014-03-14 | 2022-09-11 | 瑞士商諾華公司 | 針對lag-3之抗體分子及其用途 |
| HUE053654T2 (hu) | 2014-03-26 | 2021-07-28 | Astex Therapeutics Ltd | FGFR- és CMET-inhibitorok kombinációi a rák kezelésére |
| WO2015184305A1 (en) | 2014-05-30 | 2015-12-03 | Incyte Corporation | TREATMENT OF CHRONIC NEUTROPHILIC LEUKEMIA (CNL) AND ATYPICAL CHRONIC MYELOID LEUKEMIA (aCML) BY INHIBITORS OF JAK1 |
| WO2015191677A1 (en) | 2014-06-11 | 2015-12-17 | Incyte Corporation | Bicyclic heteroarylaminoalkyl phenyl derivatives as pi3k inhibitors |
| TWI687419B (zh) | 2014-07-10 | 2020-03-11 | 美商英塞特公司 | 作為lsd1抑制劑之咪唑并吡啶及咪唑并吡嗪 |
| WO2016007727A1 (en) | 2014-07-10 | 2016-01-14 | Incyte Corporation | Triazolopyridines and triazolopyrazines as lsd1 inhibitors |
| US9695180B2 (en) | 2014-07-10 | 2017-07-04 | Incyte Corporation | Substituted imidazo[1,2-a]pyrazines as LSD1 inhibitors |
| WO2016007722A1 (en) | 2014-07-10 | 2016-01-14 | Incyte Corporation | Triazolopyridines and triazolopyrazines as lsd1 inhibitors |
| EA039220B1 (ru) * | 2014-07-25 | 2021-12-20 | Новартис Аг | СОСТАВ ТАБЛЕТКИ 2-ФТОР-N-МЕТИЛ-4-[7-(ХИНОЛИН-6-ИЛМЕТИЛ)ИМИДАЗО[1,2-b][1,2,4]ТРИАЗИН-2-ИЛ]БЕНЗАМИДА |
| WO2016011658A1 (en) | 2014-07-25 | 2016-01-28 | Novartis Ag | Combination therapy |
| BR112017001695A2 (pt) * | 2014-07-31 | 2017-11-21 | Novartis Ag | terapia de combinação |
| EP3191126B1 (en) | 2014-09-13 | 2020-05-13 | Novartis AG | Combination therapies of alk inhibitors |
| EP3662903A3 (en) | 2014-10-03 | 2020-10-14 | Novartis AG | Combination therapies |
| MA41044A (fr) | 2014-10-08 | 2017-08-15 | Novartis Ag | Compositions et procédés d'utilisation pour une réponse immunitaire accrue et traitement contre le cancer |
| UY36351A (es) | 2014-10-14 | 2016-06-01 | Novartis Ag | Moléculas de anticuerpo que se unen a pd-l1 y usos de las mismas |
| AU2016219822B2 (en) * | 2015-02-20 | 2020-07-09 | Incyte Holdings Corporation | Bicyclic heterocycles as FGFR inhibitors |
| TWI713497B (zh) * | 2015-02-26 | 2020-12-21 | 南韓商愛思開生物製藥股份有限公司 | 咪唑并嘧啶及咪唑并三衍生物及包含該衍生物之醫藥組成物 |
| DK3831833T3 (da) | 2015-02-27 | 2022-11-14 | Incyte Holdings Corp | Fremgangsmåder til fremstillingen af en pi3k-inhibitor |
| CA2979215A1 (en) | 2015-03-10 | 2016-09-15 | Aduro Biotech, Inc. | Compositions and methods for activating "stimulator of interferon gene"-dependent signalling |
| PE20180455A1 (es) | 2015-04-03 | 2018-03-05 | Incyte Corp | Compuestos heterociclicos como inhibidores de lsd1 |
| AU2016250976B2 (en) | 2015-04-21 | 2020-02-27 | Jiangsu Hengrui Medicine Co., Ltd. | Imidazo isoindole derivative, preparation method therefor and medical use thereof |
| US9732097B2 (en) | 2015-05-11 | 2017-08-15 | Incyte Corporation | Process for the synthesis of a phosphoinositide 3-kinase inhibitor |
| WO2016183063A1 (en) | 2015-05-11 | 2016-11-17 | Incyte Corporation | Crystalline forms of a pi3k inhibitor |
| JP6507267B2 (ja) | 2015-05-22 | 2019-04-24 | チョン クン ダン ファーマシューティカル コーポレーション | 選択的ヒストンデアセチラーゼ阻害剤としてのヘテロ環状アルキル誘導体化合物及びこれを含有する薬剤学的組成物 |
| CN108025051B (zh) | 2015-07-29 | 2021-12-24 | 诺华股份有限公司 | 包含抗pd-1抗体分子的联合疗法 |
| LT3317301T (lt) | 2015-07-29 | 2021-07-26 | Novartis Ag | Kombinuotos terapijos, apimančios antikūno molekules prieš lag-3 |
| EP3316902A1 (en) | 2015-07-29 | 2018-05-09 | Novartis AG | Combination therapies comprising antibody molecules to tim-3 |
| SG10202001219UA (en) | 2015-08-12 | 2020-03-30 | Incyte Corp | Salts of an lsd1 inhibitor |
| KR20180094977A (ko) * | 2015-12-17 | 2018-08-24 | 노파르티스 아게 | c-Met 억제제와 PD-1에 대한 항체 분자의 조합물 및 그의 용도 |
| ES2986067T3 (es) | 2015-12-17 | 2024-11-08 | Novartis Ag | Moléculas de anticuerpos frente a PD-1 y usos de las mismas |
| AU2017213154B2 (en) | 2016-01-27 | 2023-02-02 | Universität Zürich | Use of GABAA receptor modulators for treatment of itch |
| AU2017241524B2 (en) | 2016-03-28 | 2021-07-08 | Incyte Corporation | Pyrrolotriazine compounds as TAM inhibitors |
| CN109414410B (zh) | 2016-04-22 | 2022-08-12 | 因赛特公司 | Lsd1抑制剂的制剂 |
| EP3464267B1 (en) * | 2016-05-23 | 2020-09-23 | Boehringer Ingelheim International GmbH | New phenylpyrazolylacetamide compounds and derivatives as cdk8/cdk19 inhibitors |
| WO2018009466A1 (en) | 2016-07-05 | 2018-01-11 | Aduro Biotech, Inc. | Locked nucleic acid cyclic dinucleotide compounds and uses thereof |
| CN106496000A (zh) * | 2016-10-19 | 2017-03-15 | 蚌埠学院 | 一种3‑氟‑4‑溴‑苯乙酮的合成方法 |
| NZ754364A (en) | 2016-12-22 | 2023-04-28 | Calithera Biosciences Inc | Compositions and methods for inhibiting arginase activity |
| UY37695A (es) | 2017-04-28 | 2018-11-30 | Novartis Ag | Compuesto dinucleótido cíclico bis 2’-5’-rr-(3’f-a)(3’f-a) y usos del mismo |
| CN110785187B (zh) | 2017-06-22 | 2024-04-05 | 诺华股份有限公司 | 针对cd73的抗体分子及其用途 |
| WO2018237173A1 (en) | 2017-06-22 | 2018-12-27 | Novartis Ag | Antibody molecules to cd73 and uses thereof |
| TWI821200B (zh) | 2017-09-27 | 2023-11-11 | 美商英塞特公司 | Tam抑制劑之鹽 |
| US11730810B2 (en) | 2017-11-14 | 2023-08-22 | Children's Medical Center Corporation | Composition comprising an antigen and a substituted imidazo[1,2-a]pyrimidine for enhancing human immune response |
| CN111936136B (zh) | 2017-11-14 | 2024-07-05 | 儿童医学中心公司 | 新咪唑并嘧啶化合物及其用途 |
| MX2020004756A (es) | 2017-11-16 | 2020-08-20 | Novartis Ag | Terapias de combinacion. |
| WO2019113487A1 (en) | 2017-12-08 | 2019-06-13 | Incyte Corporation | Low dose combination therapy for treatment of myeloproliferative neoplasms |
| EP3746429B1 (en) | 2018-01-30 | 2022-03-09 | Incyte Corporation | Processes for preparing (1-(3-fluoro-2-(trifluoromethyl)isonicotinyl)piperidine-4-one) |
| US12528810B2 (en) | 2018-03-01 | 2026-01-20 | Arizona Board Of Regents On Behalf Of The University Of Arizona | Small molecule inhibitors of DYRK/CLK and uses thereof |
| PT3773593T (pt) | 2018-03-30 | 2024-06-25 | Incyte Corp | Tratamento da hidradenite supurativa com inibidores de jak |
| TW201946630A (zh) | 2018-05-04 | 2019-12-16 | 美商英塞特公司 | Fgfr抑制劑之鹽 |
| ES2991427T3 (es) | 2018-05-04 | 2024-12-03 | Incyte Corp | Formas sólidas de un inhibidor de FGFR y procedimientos para preparar las mismas |
| CN110526916B (zh) * | 2018-05-23 | 2021-07-13 | 海创药业股份有限公司 | 氘代Capmatinib化合物及其用途 |
| TWI869346B (zh) | 2018-05-30 | 2025-01-11 | 瑞士商諾華公司 | Entpd2抗體、組合療法、及使用該等抗體和組合療法之方法 |
| WO2019232244A2 (en) | 2018-05-31 | 2019-12-05 | Novartis Ag | Antibody molecules to cd73 and uses thereof |
| CN119258070A (zh) | 2018-06-01 | 2025-01-07 | 因赛特公司 | 治疗pi3k相关病症的给药方案 |
| CN108530337B (zh) * | 2018-06-25 | 2020-11-03 | 南华大学 | 一种可选择性抑制胃癌细胞的吲哚酰胺类化合物 |
| US11241438B2 (en) | 2018-06-29 | 2022-02-08 | Incyte Corporation | Formulations of an AXL/MER inhibitor |
| AR116109A1 (es) | 2018-07-10 | 2021-03-31 | Novartis Ag | Derivados de 3-(5-amino-1-oxoisoindolin-2-il)piperidina-2,6-diona y usos de los mismos |
| WO2020047198A1 (en) | 2018-08-31 | 2020-03-05 | Incyte Corporation | Salts of an lsd1 inhibitor and processes for preparing the same |
| CN113164476A (zh) * | 2018-09-28 | 2021-07-23 | 代表亚利桑那大学的亚利桑那校董会 | Dyrk1/clk的小分子抑制剂及其用途 |
| MX2021007392A (es) | 2018-12-20 | 2021-08-24 | Novartis Ag | Regimen de dosificacion y combinacion farmaceutica que comprende derivados de 3-(1-oxoisoindolin-2-il)piperidina-2,6-diona. |
| KR20210116488A (ko) * | 2018-12-20 | 2021-09-27 | 인사이트 코포레이션 | 액티빈 수용체-유사 키나제-2의 억제제로서의 이미다조피리다진 및 이미다조피리딘 화합물 |
| US20220040324A1 (en) | 2018-12-21 | 2022-02-10 | Daiichi Sankyo Company, Limited | Combination of antibody-drug conjugate and kinase inhibitor |
| BR112021015783A2 (pt) | 2019-02-15 | 2021-10-05 | Novartis Ag | Derivados de 3-(1-oxo-5-(piperidin-4-il)isoindolin-2-il)piperidina-2,6-diona e usos dos mesmos |
| WO2020165834A1 (en) | 2019-02-15 | 2020-08-20 | Novartis Ag | Substituted 3-(1-oxoisoindolin-2-yl)piperidine-2,6-dione derivatives and uses thereof |
| WO2021053559A1 (en) | 2019-09-18 | 2021-03-25 | Novartis Ag | Entpd2 antibodies, combination therapies, and methods of using the antibodies and combination therapies |
| AU2020395185A1 (en) | 2019-12-04 | 2022-06-02 | Incyte Corporation | Derivatives of an FGFR inhibitor |
| TW202135859A (zh) | 2019-12-20 | 2021-10-01 | 瑞士商諾華公司 | 組合療法 |
| WO2021173476A1 (en) | 2020-02-24 | 2021-09-02 | The Trustees Of Columbia University In The City Of New York | Compounds, pharmaceutical formulations, and methods for treatment of cancer |
| EP4114401A1 (en) | 2020-03-06 | 2023-01-11 | Incyte Corporation | Combination therapy comprising axl/mer and pd-1/pd-l1 inhibitors |
| US11833155B2 (en) | 2020-06-03 | 2023-12-05 | Incyte Corporation | Combination therapy for treatment of myeloproliferative neoplasms |
| CN111825678A (zh) * | 2020-06-05 | 2020-10-27 | 连庆泉 | 一种卡马替尼的制备方法 |
| WO2021260528A1 (en) | 2020-06-23 | 2021-12-30 | Novartis Ag | Dosing regimen comprising 3-(1-oxoisoindolin-2-yl)piperidine-2,6-dione derivatives |
| WO2022007752A1 (zh) * | 2020-07-06 | 2022-01-13 | 苏州晶云药物科技股份有限公司 | 苯甲酰胺类化合物及其二盐酸盐的新晶型及其制备方法 |
| TW202304979A (zh) | 2021-04-07 | 2023-02-01 | 瑞士商諾華公司 | 抗TGFβ抗體及其他治療劑用於治療增殖性疾病之用途 |
| EP4323405A1 (en) | 2021-04-12 | 2024-02-21 | Incyte Corporation | Combination therapy comprising an fgfr inhibitor and a nectin-4 targeting agent |
| AR125874A1 (es) | 2021-05-18 | 2023-08-23 | Novartis Ag | Terapias de combinación |
| TW202327569A (zh) | 2021-09-01 | 2023-07-16 | 瑞士商諾華公司 | 包含tead抑制劑的藥物組合及其用於癌症治療之用途 |
| CN113896732B (zh) * | 2021-10-13 | 2023-09-12 | 沈阳红旗制药有限公司 | 抗癌药物卡马替尼的制备方法及其应用 |
| WO2023249994A1 (en) * | 2022-06-22 | 2023-12-28 | Mayo Foundation For Medical Education And Research | Methods and materials for treating cancer |
| JP2025522965A (ja) | 2022-07-08 | 2025-07-17 | アストラゼネカ・アクチエボラーグ | 癌の治療のためのhgf受容体阻害剤と組み合わせた上皮成長因子受容体チロシンキナーゼ阻害剤 |
| CN116903627B (zh) | 2023-05-15 | 2024-01-16 | 云白药征武科技(上海)有限公司 | 一种咪唑并三嗪硫代苯甲酰胺衍生物及其制备方法和应用 |
Family Cites Families (96)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US1411859A (en) | 1920-12-08 | 1922-04-04 | Marchand Robert | Process for preparing hydrate of terpin |
| US2837520A (en) * | 1955-05-26 | 1958-06-03 | Ind Chimica Profarmaco S R L | Fluorescent materials on the basis of tetrazoindenes |
| US4209621A (en) | 1979-04-27 | 1980-06-24 | American Cyanamid Company | (Substituted-phenyl)-1,2,4-triazolo[4,3-a]-pyrimidines and (substituted-phenyl)-1,2,4-triazolo[1,5-a]pyrimidines |
| US4405619A (en) | 1981-09-02 | 1983-09-20 | Diamond Shamrock Corporation | Antiinflammatory substituted-1,2,4-triazolo[4,3-b]-1,2,4-triazines |
| DE3311753A1 (de) | 1983-03-31 | 1984-10-04 | Hoechst Ag, 6230 Frankfurt | Substituierte 6-aryl-1,2,4-triazolo(4,3-b)pyridazine - ihre herstellung und verwendung - |
| JPS6337347A (ja) | 1986-08-01 | 1988-02-18 | Fuji Photo Film Co Ltd | 直接ポジカラ−画像形成方法 |
| JPS63199347A (ja) | 1987-02-14 | 1988-08-17 | Konica Corp | 鮮鋭性の向上した高感度ハロゲン化銀写真感光材料 |
| JPS63310891A (ja) | 1987-06-12 | 1988-12-19 | Yoshitomi Pharmaceut Ind Ltd | 縮合ピリダジン化合物 |
| US5236917A (en) | 1989-05-04 | 1993-08-17 | Sterling Winthrop Inc. | Saccharin derivatives useful as proteolytic enzyme inhibitors and compositions and method of use thereof |
| JPH0313934A (ja) | 1989-06-12 | 1991-01-22 | Konica Corp | ハロゲン化銀写真感光材料 |
| IL96432A0 (en) | 1989-11-30 | 1991-08-16 | Schering Ag | Pesticidal compositions containing pyridine derivatives and novel pyridine derivatives |
| JP2664264B2 (ja) | 1990-02-15 | 1997-10-15 | 富士写真フイルム株式会社 | ハロゲン化銀写真乳剤及びこれを用いた写真感光材料 |
| FR2662163A1 (fr) | 1990-05-16 | 1991-11-22 | Lipha | Nouvelles 8-amino-1,2,4-triazolo(4,3-a) pyrazines, procedes de preparation et medicaments les contenant. |
| JPH04251243A (ja) | 1991-01-09 | 1992-09-07 | Konica Corp | ハロゲン化銀写真感光材料 |
| FR2671551B1 (fr) | 1991-01-15 | 1993-03-12 | Adir | Nouveaux composes de structure aryl triazinique, leur procede de preparation et les compositions pharmaceutiques qui les contiennent. |
| US5232618A (en) | 1991-09-30 | 1993-08-03 | E. I. Du Pont De Nemours And Company | Substantially constant boiling compositions of difluoromethane and trifluoroethane or perfluoroethane |
| JPH05232618A (ja) | 1992-02-21 | 1993-09-10 | Konica Corp | ハロゲン化銀写真感光材料 |
| DE4309285A1 (de) | 1993-03-23 | 1994-09-29 | Boehringer Ingelheim Kg | Heterocyclen enthaltende Amidinderivate, ihre Herstellung und Verwendung |
| CN1268137A (zh) | 1997-07-03 | 2000-09-27 | 杜邦药品公司 | 治疗神经失调的咪唑并嘧啶和咪唑并吡啶 |
| ES2137113B1 (es) | 1997-07-29 | 2000-09-16 | Almirall Prodesfarma Sa | Nuevos derivados de triazolo-piridazinas heterociclicos. |
| DE19734311A1 (de) | 1997-08-08 | 1999-02-11 | Bosch Gmbh Robert | Anordnung zur Übertragung optischer Signale mit Ersatzschaltungswirkung |
| JP4251243B2 (ja) | 1998-11-26 | 2009-04-08 | 株式会社日立メディコ | 領域拡張装置 |
| JP4025468B2 (ja) | 1999-07-29 | 2007-12-19 | 三井化学株式会社 | 有機電界発光素子 |
| MXPA01007019A (es) | 1999-11-10 | 2002-09-18 | Johnson & Johnson | 2-aril-3-(heteroaril)-imidazo[1,2-a]pirimidinas, sustituidas y composiciones farmaceuticas relacionados y metodos. |
| ES2195943T3 (es) | 1999-11-12 | 2003-12-16 | Neurogen Corp | Compuestos heteroaromaticos biciclicos y triciclicos. |
| DE10010067A1 (de) * | 2000-03-02 | 2001-09-06 | Bayer Ag | Neue Imidazotriazinone und ihre Verwendung |
| AU2000240570A1 (en) * | 2000-03-29 | 2001-10-08 | Knoll Gesellschaft Mit Beschraenkter Haftung | Pyrrolopyrimidines as tyrosine kinase inhibitors |
| JP2001302667A (ja) * | 2000-04-28 | 2001-10-31 | Bayer Ag | イミダゾピリミジン誘導体およびトリアゾロピリミジン誘導体 |
| CA2427779A1 (en) | 2000-11-10 | 2002-05-16 | Merck Sharp & Dohme Limited | Imidazo-triazine derivatives as ligands for gaba receptors |
| GB0103926D0 (en) | 2001-02-17 | 2001-04-04 | Astrazeneca Ab | Chemical compounds |
| DE60210755T2 (de) | 2001-03-09 | 2006-11-16 | Pfizer Products Inc., Groton | Triazolopyridine als entzündungshemmende mittel |
| GB0107751D0 (en) | 2001-03-28 | 2001-05-16 | Pfizer Ltd | Pharmaceutically active compounds |
| US20050090498A1 (en) | 2001-05-24 | 2005-04-28 | Kiyohiro Samizu | 3-Quinolin-2(1h)-ylideneindolin-2-one derivative |
| DE10130167A1 (de) * | 2001-06-22 | 2003-01-02 | Bayer Ag | Imidazotriazine |
| EP1481977A4 (en) | 2002-03-01 | 2006-02-01 | Astellas Pharma Inc | NITROGENIC HETEROCYCLIC COMPOUND |
| AU2003223295A1 (en) | 2002-03-19 | 2003-10-08 | Merck And Co., Inc. | Process and intermediates to substituted imidazopyrimidines |
| US6790852B2 (en) | 2002-04-18 | 2004-09-14 | Hoffmann-La Roche Inc. | 2-(2,6-dichlorophenyl)-diarylimidazoles |
| GB0210127D0 (en) | 2002-05-02 | 2002-06-12 | Merck Sharp & Dohme | Therapeutic agents |
| GB0210124D0 (en) | 2002-05-02 | 2002-06-12 | Merck Sharp & Dohme | Therapeutic agents |
| GB0211649D0 (en) | 2002-05-21 | 2002-07-03 | Novartis Ag | Organic compounds |
| DE10230604A1 (de) | 2002-07-08 | 2004-01-29 | Bayer Ag | Heterocyclisch substituierte Imidazotriazine |
| DE10230605A1 (de) | 2002-07-08 | 2004-01-29 | Bayer Ag | Substituierte Imidazotriazine |
| MXPA05002123A (es) | 2002-08-30 | 2005-06-06 | Pfizer Prod Inc | Nuevos procedimientos e intermedios para preparar triazolo-piridinas. |
| US6784297B2 (en) | 2002-09-04 | 2004-08-31 | Kopran Limited | Process for the preparation of anti-ischemic and anti-hypertensive drug amlodipine besylate |
| ATE473980T1 (de) | 2002-12-18 | 2010-07-15 | Vertex Pharma | Triazolopyridazine als proteinkinase-inhibitoren |
| UA80171C2 (en) * | 2002-12-19 | 2007-08-27 | Pfizer Prod Inc | Pyrrolopyrimidine derivatives |
| GB0303910D0 (en) * | 2003-02-20 | 2003-03-26 | Merck Sharp & Dohme | Therapeutic agents |
| GEP20084341B (en) | 2003-02-26 | 2008-03-25 | Sugen Inc | Aminoheteroaryl compounds as protein kinase inhibitors |
| PA8595001A1 (es) | 2003-03-04 | 2004-09-28 | Pfizer Prod Inc | Nuevos compuestos heteroaromaticos condensados que son inhibidores del factor de crecimiento transforante (tgf) |
| JPWO2005002590A1 (ja) | 2003-07-01 | 2006-08-10 | アステラス製薬株式会社 | 骨量増加誘導剤 |
| US7250417B2 (en) | 2003-07-02 | 2007-07-31 | Sugen Inc. | Arylmethyl triazolo- and imidazopyrazines as c-Met inhibitors |
| CA2529622A1 (en) | 2003-07-02 | 2005-01-20 | Sugen, Inc. | Indolinone hydrazides as c-met inhibitors |
| US7122548B2 (en) | 2003-07-02 | 2006-10-17 | Sugen, Inc. | Triazolotriazine compounds and uses thereof |
| US7037909B2 (en) | 2003-07-02 | 2006-05-02 | Sugen, Inc. | Tetracyclic compounds as c-Met inhibitors |
| CA2534292A1 (en) | 2003-07-30 | 2005-02-17 | Laboratorios S.A.L.V.A.T., S.A. | Substituted imidazopyrimidines for the prevention and treatment of cancer |
| AR045595A1 (es) | 2003-09-04 | 2005-11-02 | Vertex Pharma | Composiciones utiles como inhibidores de proteinas quinasas |
| EP1697352B1 (en) | 2003-09-24 | 2012-06-27 | Vertex Pharmceuticals Incorporated | 4-azole substituted imidazole compositions useful as inhibitors or c-met receptor tyrosine kinase |
| EP2392565B1 (en) | 2003-09-26 | 2014-03-19 | Exelixis, Inc. | c-Met modulators and methods of use |
| US7144889B2 (en) | 2003-10-16 | 2006-12-05 | Hoffman-La Roche Inc. | Triarylimidazoles |
| US7169781B2 (en) | 2003-10-17 | 2007-01-30 | Hoffmann-La Roche Inc. | Imidazole derivatives and their use as pharmaceutical agents |
| US7419978B2 (en) | 2003-10-22 | 2008-09-02 | Bristol-Myers Squibb Company | Phenyl-aniline substituted bicyclic compounds useful as kinase inhibitors |
| GB0325031D0 (en) | 2003-10-27 | 2003-12-03 | Novartis Ag | Organic compounds |
| WO2005073224A2 (en) | 2004-01-23 | 2005-08-11 | Amgen Inc | Quinoline quinazoline pyridine and pyrimidine counds and their use in the treatment of inflammation angiogenesis and cancer |
| WO2005070891A2 (en) | 2004-01-23 | 2005-08-04 | Amgen Inc | Compounds and methods of use |
| CA2556404A1 (en) | 2004-02-18 | 2005-08-25 | Banyu Pharmaceutical Co., Ltd. | Nitrogenous fused heteroaromatic ring derivative |
| DE602005014964D1 (de) | 2004-04-02 | 2009-07-30 | Osi Pharm Inc | Mit einem 6,6-bicyclischen ring substituierte heterobicyclische proteinkinaseinhibitoren |
| US20050277650A1 (en) | 2004-04-20 | 2005-12-15 | Sundaram Venkataraman | Process for preparing aripirazole hydrate |
| MXPA06012613A (es) | 2004-05-07 | 2007-01-31 | Amgen Inc | Derivados heterociclicos nitrogenados como moduladores de proteina cinasa y uso para el tratamiento de angiogenesis y cancer. |
| WO2005121125A1 (en) | 2004-06-09 | 2005-12-22 | Pfizer Inc. | Ether-linked heteroaryl compounds |
| JP5368701B2 (ja) | 2004-07-02 | 2013-12-18 | エクセリクシス、インコーポレイテッド | c−Metモジュレーター及び使用方法 |
| AR053090A1 (es) * | 2004-07-20 | 2007-04-25 | Osi Pharm Inc | Imidazotriazinas como inhibidores de proteina quinasas y su uso para la preparacion de medicamentos |
| US7361763B2 (en) * | 2004-07-27 | 2008-04-22 | Sgx Pharmaceuticals, Inc. | Pyrrolo-pyridine kinase modulators |
| BRPI0513915A (pt) | 2004-08-26 | 2008-05-20 | Pfizer | compostos aminoeteroarila enantiomericamente puros como inibidores de proteìna quinase |
| AU2005295734A1 (en) | 2004-10-15 | 2006-04-27 | Biogen Idec Ma Inc. | Methods of treating vascular injuries |
| JP4935357B2 (ja) * | 2004-11-08 | 2012-05-23 | Msd株式会社 | 新規縮環イミダゾール誘導体 |
| US7456289B2 (en) | 2004-12-31 | 2008-11-25 | National Health Research Institutes | Anti-tumor compounds |
| CN101137412B (zh) | 2005-01-13 | 2012-11-07 | 布里斯托尔-迈尔斯·斯奎布公司 | 用作凝血因子XIa抑制剂的取代的二芳基化合物 |
| AU2006247833A1 (en) | 2005-05-12 | 2006-11-23 | Merck & Co., Inc. | Tyrosine kinase inhibitors |
| JP2009500451A (ja) | 2005-07-11 | 2009-01-08 | スミスクライン ビーチャム コーポレーション | ピラノピリジン化合物 |
| WO2007015866A2 (en) * | 2005-07-20 | 2007-02-08 | Kalypsys, Inc. | Inhibitors of p38 kinase and methods of treating inflammatory disorders |
| EP1910369A1 (en) | 2005-07-29 | 2008-04-16 | Astellas Pharma Inc. | Fused heterocycles as lck inhibitors |
| WO2007025090A2 (en) | 2005-08-25 | 2007-03-01 | Kalypsys, Inc. | Heterobicyclic and - tricyclic inhibitors of mapk/erk kinase |
| WO2007064797A2 (en) | 2005-11-30 | 2007-06-07 | Vertex Pharmaceuticals Incorporated | Inhibitors of c-met and uses thereof |
| PT1966214T (pt) | 2005-12-21 | 2017-02-03 | Janssen Pharmaceutica Nv | Triazolpiridazinas como moduladores de tirosina quinase |
| JP5200939B2 (ja) | 2005-12-23 | 2013-06-05 | アリアド・ファーマシューティカルズ・インコーポレイテッド | 二環式ヘテロアリール化合物 |
| WO2007096764A2 (en) * | 2006-02-27 | 2007-08-30 | Glenmark Pharmaceuticals S.A. | Bicyclic heteroaryl derivatives as cannabinoid receptor modulators |
| PE20080403A1 (es) | 2006-07-14 | 2008-04-25 | Amgen Inc | Derivados heterociclicos fusionados y metodos de uso |
| US8217177B2 (en) | 2006-07-14 | 2012-07-10 | Amgen Inc. | Fused heterocyclic derivatives and methods of use |
| US7683060B2 (en) | 2006-08-07 | 2010-03-23 | Incyte Corporation | Triazolotriazines as kinase inhibitors |
| PL2081937T3 (pl) | 2006-10-23 | 2013-01-31 | Sgx Pharmaceuticals Inc | Triazolopirydazynowe modulatory kinaz białkowych |
| WO2008058126A2 (en) | 2006-11-06 | 2008-05-15 | Supergen, Inc. | Imidazo[1,2-b]pyridazine and pyrazolo[1,5-a]pyrimidine derivatives and their use as protein kinase inhibitors |
| KR101532256B1 (ko) | 2006-11-22 | 2015-06-29 | 인사이트 코포레이션 | 키나제 억제제로서의 이미다조트리아진 및 이미다조피리미딘 |
| CN101678014B (zh) | 2007-05-21 | 2012-12-12 | Sgx药品公司 | 杂环激酶调节剂 |
| WO2009143211A2 (en) | 2008-05-21 | 2009-11-26 | Incyte Corporation | Salts of 2-fluoro-n-methyl-4-[7-(quinolin-6-yl-methyl)- imidazo[1,2-b][1,2,4]triazin-2-yl]benzamide and processes related to preparing the same |
| EA025304B1 (ru) | 2010-02-03 | 2016-12-30 | Инсайт Холдингс Корпорейшн | ИМИДАЗО[1,2-b][1,2,4]ТРИАЗИНЫ В КАЧЕСТВЕ c-Met ИНГИБИТОРОВ |
| US8901323B2 (en) | 2011-05-06 | 2014-12-02 | Takasago International Corporation | Ruthenium-diamine complex and method for producing optically active compound |
-
2007
- 2007-11-19 KR KR1020097013022A patent/KR101532256B1/ko active Active
- 2007-11-19 ES ES07864592T patent/ES2398843T3/es active Active
- 2007-11-19 CN CN2007800503102A patent/CN101641093B/zh active Active
- 2007-11-19 EA EA200970501A patent/EA026126B1/ru unknown
- 2007-11-19 MY MYPI2013000862A patent/MY188338A/en unknown
- 2007-11-19 HR HRP20130106TT patent/HRP20130106T1/hr unknown
- 2007-11-19 NZ NZ577127A patent/NZ577127A/en unknown
- 2007-11-19 CN CN201310141352.4A patent/CN103288833B/zh active Active
- 2007-11-19 PT PT78645926T patent/PT2099447E/pt unknown
- 2007-11-19 SI SI200732055T patent/SI3034075T1/sl unknown
- 2007-11-19 DK DK07864592.6T patent/DK2099447T3/da active
- 2007-11-19 DK DK12158715.8T patent/DK2497470T3/en active
- 2007-11-19 PL PL07864592T patent/PL2099447T3/pl unknown
- 2007-11-19 PL PL15191241T patent/PL3034075T3/pl unknown
- 2007-11-19 DK DK15191241.7T patent/DK3034075T3/en active
- 2007-11-19 PT PT15191241T patent/PT3034075T/pt unknown
- 2007-11-19 CA CA2669991A patent/CA2669991C/en active Active
- 2007-11-19 HU HUE12158715A patent/HUE026659T2/en unknown
- 2007-11-19 GE GEAP200711325A patent/GEP20125658B/en unknown
- 2007-11-19 ES ES15191241.7T patent/ES2689444T3/es active Active
- 2007-11-19 RS RS20160017A patent/RS54510B1/sr unknown
- 2007-11-19 SI SI200731149T patent/SI2099447T1/sl unknown
- 2007-11-19 WO PCT/US2007/085100 patent/WO2008064157A1/en not_active Ceased
- 2007-11-19 JP JP2009538473A patent/JP5572388B2/ja active Active
- 2007-11-19 MY MYPI20092064A patent/MY188335A/en unknown
- 2007-11-19 EA EA201691862A patent/EA032254B1/ru active IP Right Revival
- 2007-11-19 EP EP12158715.8A patent/EP2497470B8/en active Active
- 2007-11-19 ME MEP-2016-13A patent/ME02372B/me unknown
- 2007-11-19 KR KR1020147033803A patent/KR101588583B1/ko active Active
- 2007-11-19 MX MX2009005144A patent/MX2009005144A/es active IP Right Grant
- 2007-11-19 EP EP07864592A patent/EP2099447B1/en active Active
- 2007-11-19 US US11/942,130 patent/US7767675B2/en active Active
- 2007-11-19 ME MEP-2013-35A patent/ME01507B/me unknown
- 2007-11-19 RS RS20130041A patent/RS52677B/sr unknown
- 2007-11-19 ES ES12158715.8T patent/ES2560435T3/es active Active
- 2007-11-19 PT PT121587158T patent/PT2497470E/pt unknown
- 2007-11-19 EP EP15191241.7A patent/EP3034075B1/en active Active
- 2007-11-19 NO NO20200077A patent/NO346024B1/no unknown
- 2007-11-19 EP EP18182215.6A patent/EP3443958A1/en active Pending
- 2007-11-19 PL PL12158715T patent/PL2497470T3/pl unknown
- 2007-11-19 RS RS20181200A patent/RS57741B1/sr unknown
- 2007-11-19 SI SI200731739T patent/SI2497470T1/sl unknown
- 2007-11-19 LT LTEP15191241.7T patent/LT3034075T/lt unknown
- 2007-11-19 AU AU2007323725A patent/AU2007323725B2/en active Active
- 2007-11-21 AR ARP070105176A patent/AR066142A1/es active IP Right Grant
- 2007-11-22 TW TW096144319A patent/TWI429432B/zh active
- 2007-11-22 CL CL200703341A patent/CL2007003341A1/es unknown
-
2009
- 2009-05-12 IL IL198716A patent/IL198716A/en active IP Right Grant
- 2009-05-18 NO NO20091924A patent/NO344399B1/no active Protection Beyond IP Right Term
- 2009-06-08 CR CR10841A patent/CR10841A/es unknown
- 2009-06-10 CO CO09060491A patent/CO6210810A2/es active IP Right Grant
- 2009-06-11 EC EC2009009400A patent/ECSP099400A/es unknown
-
2010
- 2010-06-10 US US12/813,148 patent/US8461330B2/en active Active
-
2013
- 2013-02-04 CY CY20131100098T patent/CY1116763T1/el unknown
- 2013-05-16 US US13/895,799 patent/US20130324515A1/en not_active Abandoned
-
2016
- 2016-01-12 CY CY20161100026T patent/CY1117108T1/el unknown
- 2016-01-25 HR HRP20160077TT patent/HRP20160077T1/hr unknown
- 2016-02-05 US US15/016,841 patent/US9944645B2/en active Active
- 2016-02-23 IL IL244244A patent/IL244244B/en active IP Right Grant
-
2018
- 2018-03-20 US US15/925,996 patent/US10738052B2/en active Active
- 2018-10-05 HR HRP20181622TT patent/HRP20181622T1/hr unknown
- 2018-10-22 CY CY20181101082T patent/CY1121021T1/el unknown
-
2019
- 2019-06-07 NO NO20190709A patent/NO344864B1/no unknown
-
2020
- 2020-06-23 US US16/909,686 patent/US11261191B2/en active Active
- 2020-08-25 IL IL276928A patent/IL276928B/en unknown
-
2021
- 2021-07-15 IL IL284889A patent/IL284889B2/en unknown
-
2022
- 2022-01-13 US US17/575,371 patent/US12084449B2/en active Active
- 2022-12-12 LU LU00293C patent/LUC00293I2/en unknown
- 2022-12-13 NO NO2022057C patent/NO2022057I1/no unknown
- 2022-12-13 LT LTPA2022527C patent/LTC2099447I2/lt unknown
- 2022-12-14 HU HUS2200052C patent/HUS2200052I1/hu unknown
- 2022-12-15 FR FR22C1060C patent/FR22C1060I2/fr active Active
- 2022-12-16 CY CY2022037C patent/CY2022037I2/el unknown
- 2022-12-16 NL NL301209C patent/NL301209I2/nl unknown
-
2024
- 2024-08-08 US US18/798,506 patent/US20250223291A1/en active Pending
Also Published As
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| ME01507B (me) | Imidazotriazini i imidazopirimidini kao inhibitori kinaze | |
| JP2010510319A5 (me) | ||
| HRP20231614T1 (hr) | Spojevi pirolotriazina kao tam inhibitori | |
| JP2013523889A5 (me) | ||
| RU2012132426A (ru) | ПРОИЗВОДНЫЕ ТИЕНО[3,2-d]ПИРИМИДИНА, ОБЛАДАЮЩИЕ ИНГИБИРУЮЩЕЙ АКТИВНОСТЬЮ В ОТНОШЕНИИ ПРОТЕИНКИНАЗЫ | |
| RU2011101901A (ru) | Триазолопиридиновые соединения-ингибиторы jak и способы | |
| JP2016510035A5 (me) | ||
| JP2017530185A5 (me) | ||
| JP2016522246A5 (me) | ||
| JP2017505794A5 (me) | ||
| JP2019535664A5 (me) | ||
| SI2797918T1 (en) | Bromodomain inhibitors | |
| JP2019504901A5 (me) | ||
| RU2009101911A (ru) | Производные пиридина и пиразина в качестве ингибиторов mnk-киназы | |
| ME02856B (me) | Aminopirimidinilni spojevi kao inhibitori jak | |
| HRP20201469T1 (hr) | Derivati tetrahidroizokinolina | |
| RU2017121044A (ru) | Производные амидотиадиазола в качестве ингибиторов надфн-оксидазы | |
| US11529350B2 (en) | Tyrosine kinase non-receptor 1 (TNK1) inhibitors and uses thereof | |
| JP2013510876A5 (me) | ||
| RU2014120374A (ru) | Имидазопиридазины | |
| JP2016528298A5 (me) | ||
| HRP20192151T1 (hr) | Derivati izokromena kao inhibitori fosfoinozitid 3-kinaza | |
| RU2014119254A (ru) | Средства, вызывающие апоптоз, для лечения злокачественных новообразований и иммунных и аутоиммунных заболеваний | |
| JP2009513575A5 (me) | ||
| JP2014530237A5 (me) |