ME02461B - Modulatori indoleamina 2,3-dioksigenaze i metode za upotrebu istih - Google Patents

Modulatori indoleamina 2,3-dioksigenaze i metode za upotrebu istih

Info

Publication number
ME02461B
ME02461B MEP-2016-96A MEP9616A ME02461B ME 02461 B ME02461 B ME 02461B ME P9616 A MEP9616 A ME P9616A ME 02461 B ME02461 B ME 02461B
Authority
ME
Montenegro
Prior art keywords
amino
methyl
fluorophenyl
oxadiazol
bromo
Prior art date
Application number
MEP-2016-96A
Other languages
English (en)
Inventor
Andrew P Combs
Eddy W Yue
Original Assignee
Incyte Holdings Corp
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=37396891&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=ME02461(B) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Incyte Holdings Corp filed Critical Incyte Holdings Corp
Publication of ME02461B publication Critical patent/ME02461B/me

Links

Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4245—Oxadiazoles
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D271/00—Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms
    • C07D271/02—Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms not condensed with other rings
    • C07D271/08—1,2,5-Oxadiazoles; Hydrogenated 1,2,5-oxadiazoles
    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/433—Thidiazoles
    • 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
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • 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
    • A61K31/54—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame
    • A61K31/541—Non-condensed thiazines containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/24—Antidepressants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A61P27/12—Ophthalmic agents for cataracts
    • 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
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A61P31/18—Antivirals for RNA viruses for HIV
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • 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
    • A61P37/04—Immunostimulants
    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D285/00—Heterocyclic compounds containing rings having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by groups C07D275/00 - C07D283/00
    • C07D285/01—Five-membered rings
    • C07D285/02—Thiadiazoles; Hydrogenated thiadiazoles
    • C07D285/04—Thiadiazoles; Hydrogenated thiadiazoles not condensed with other rings
    • C07D285/10—1,2,5-Thiadiazoles; Hydrogenated 1,2,5-thiadiazoles
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Immunology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Oncology (AREA)
  • Virology (AREA)
  • Pulmonology (AREA)
  • Rheumatology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Dermatology (AREA)
  • Psychiatry (AREA)
  • Communicable Diseases (AREA)
  • Pain & Pain Management (AREA)
  • Psychology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Molecular Biology (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • AIDS & HIV (AREA)
  • Transplantation (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Hospice & Palliative Care (AREA)
  • Hematology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)

Claims (14)

1. Jedinjenje formuleili njegova farmaceutski prihvatljiva so, za upotrebu u tretmanu kancera u kombinaciji sa anti-PD-1 antitelom gde su: W, X1, i X2 nezavisno izabrani od (CRaRb)t, (CRaRb)uO(CRaRb)v, (CRaRb)uC(O)(CRaRb)v, (CRaRb)uC(O)NRc(CRaRb)v, (CRaRb)uC(O)O(CRaRb)v, (CRaRb)uC(S)(CRaRb)u, (CRaRb)uC(S)NRc(CRaRb)v, (CRaRb)uS(O)(CRaRb)v, (CRaRb)uS(O)NRc(CRaRb)v, (CRaRb)uS(O)2(CRaRb)v, (CRaRb)uS(O)2NRc(CRaRb)v, (CRaRb)uNRc(CRaRb)v i (CRaRb)uC(=NRd)NRc(CRaRb)v;R2 je H, C1-6 alkil ili C3-7 cikloalkil;R3a i R5a su nezavisno izabrani od C1-8 alkila, C2-8 alkenila, C2-8 alkinila, arila, cikloalkila, heteroarila i heterocikloalkila, svaki opciono supstituisan sa 1, 2, 3, 4 ili 5 supstituenata nezavisno izabranih od halo, C1-6 alkila, C2-6 alkenila, C2-6 alkinila, C1-4 haloalkila, Cy1, CN, NO2, ORe1, SRe1, C(O)Rf1, C(O)NRg1Rh1, C(O)ORe1, OC(O)Rf1, OC(O)NRg1Rh1, NRg1C(O)NRg1Rh1, NRg1Rh1, NRg1C(O)Rf1, NRg1C(O)ORe1, C(=NRi)NRg1Rh1, NRg1C(=NRi)NRg1Rh1, P(Rf1)2, P(ORe1)2, P(O)Re1Rf1, P(O)ORe1ORf1, S(O)Rf1, S(O)NRg1Rh1, S(O)2Rf1 i S(O)2NRg1Rh1;R3b je aril ili heteroaril svaki opciono supstituisan sa 1, 2, 3, 4 ili 5 supstituenata nezavisno izabranih od halo, C1-6 alkila, C2-6 alkenila, C2-6 alkinila, C1-4 haloalkila, C1-4 hidroksialkila, Cy2, CN, NO2, ORe1, SRe1, C(O)Rf1, C(O)NRg1Rh1, C(O)ORe1, OC(O)Rf1, OC(O)NRg1Rh1, NRg1C(O)NRg1Rh1, NRg1Rh1, NRg1C(O)Rf1, NRg1C(O)ORe1, C(=NRi)NRg1Rh1, NRg1C(=NRi)NRg1Rh1, P(Rf1)2, P(ORe1)2, P(O)Re1Rf1, P(O)ORe1ORf1, S(O)Rf1, S(O)NRg1Rh1, S(O)2Rf1 i S(O)2NRg1Rh1;R5b je H, C1-8 alkil, C2-8 alkenil, C2-8 alkinil, aril, cikloalkil, heteroaril ili heterocikloalkil gde su spomenuti C1-8 alkil, C2-8 alkenil, C2-5 alkinil, aril, cikloalkil, heteroaril ili heterocikloalkil opciono supstituisani sa 1, 2, 3, 4 ili 5 supstituenata nezavisno izabranih od halo, C1-6 alkila, C2-6 alkenilaC2-6 alkinila, C1-4 haloalkila, C1-4 hidroksialkila, Cy2, CN, NO2, ORe1, SRe1, C(O)Rf1, C(O)NRg1Rh1, C(O)ORe1, OC(O)Rf1, OC(O)NRg1Rh1, NRg1C(O)NRg1Rh1, NRg1Rh1, NRg1C(O)Rf1, NRg1C(O)ORe1, C(=NRi)NRg1Rh1, NRg1C(=NRi)NRh1R, P(Rf1)2, P(ORe1)2, P(O)Re1Rf1, P(O)ORe1ORf1, S(O)Rf1, S(O)NRg1Rh1, S(O)2Rf1 i S(O)2NRg1Rh1;Cy1 i Cy2 su opciono izabrani od arila, heteroarila, cikloalkila i heterocikloalkila, svaki supstituisan sa 1, 2, 3, 4 ili 5 supstituenata nezavisno izabranih od halo, C1-4 alkila, C2-4 alkenila, C2-4 alkinila, C1-4 haloalkila, CN, NO2, ORe3, SRe3, C(O)Rf3, C(O)NRg3Rh3, C(O)ORe3, OC(O)Rf3, OC(O)NRg3Rh3, NRg3Rh3, NRg3C(O)Rh3, NRg3C(O)ORe3, C(=NRi)NRg1Rh1, NRg1C(=NRi)NRg1Rh1, P(Rf3)2, P(ORe3)2, P(O)Re3Rf3, P(O)ORe3ORf3, S(O)Rf3, S(O)NRg3Rh3, S(O)2Rf3 i S(O)2NRg3Rh3;Ra i Rb su nezavisno izabrani od H, halo, C1-6 alkila, C2-6 alkenila, C2-6 alkinila, C1-4 haloalkila, arila, cikloalkila, heteroarila, heterocikloalkila, arilalkila, cikloalkilalkila, heteroarilalkila, heterocikloalkilalkila, CN, NO2, ORe4, SRe4, C(O)Rf4, C(O)NRg4Rh4, C(O)ORe4, OC(O)Rf4, OC(O)NRg4Rh4, NRg4Rh4, NRg4C(O)Rh4, NRg4C(O)ORe4, C(=NRi)NRg1Rh1, NRg1C(=NRi)NRg1Rh1, P(Rf4)2, P(ORe4)2, P(O)Re4Rf4, P(O)ORe4ORf4, S(O)Rf4, S(O)NRg4Rh4, S(O)2Rf4 i S(O)2NRg4Rh4;Rc je H, C1-6 alkila, C1-6 haloalkila, C2-6 alkenila, C2-6 alkinila, arila, cikloalkila, arilalkila ili cikloalkilalkila;Rd je H, ORd1, CN ili NO2;Rd1 je H, C1-6 alkil, C1-6 haloalkil, C2-6 alkenil, C2-6 alkinil, aril, cikloalkil, arilalkil ili cikloalkilalkil;Rel, Re3 i R64 su nezavisno izabrani 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;Rf1, Rf3 i Rf4 su nezavisno izabrani od H, C1-6 alkila, C1-6 haloalkila, C2-6 alkenila, C2-6 alkinila, arila, cikloalkila, heteroarila i heterocikloalkila;Rg1, Rg3 i Rg4 nezavisno su izabrani od H, C1-6 alkil, C1-6 haloalkila, C2-6 alkenila, C2-6 alkinila, arila, cikloalkila, arilalkila i cikloalkilalkila;Rh1, Rh3 i Rh4 su nezavisno izabrani od H, C1-6 alkila, C1-6 haloalkila, C2-6 alkenila, C2-6 alkinila, arila, cikloalkila, arilalkila i cikloalkilalkila;ili Rg1 i Rh1 zajedno sa N atomom za koji su vezani formiraju 4-, 5-, 6- ili 7-očlanu heterocikloalkil grupu;ili Rg3 i Rh3 zajedno sa N atomom za koji su vezani formiraju 4-, 5-, 6- ili 7-očlanu heterocikloalkil grupu;ili Rg4 i Rh4 zajedno sa N atomom za koji su vezani formiraju 4-, 5-, 6- ili 7-očlanu heterocikloalkil grupu;Ri je H, CN ili NO2;a je 0 ili 1;b je 0 ili 1;n je 0 ili 1;p je 0 ili 1;t je 1, 2, 3, 4, 5 ili 6;u je 0, 1, 2, 3, 4, 5 ili 6; iv je 0, 1, 2, 3, 4, 5 ili 6.
2. Jedinjenje ili so za upotrebu prema zahtevu 1, pri čemu R2 jeste H.
3. Jedinjenje ili so za upotrebu prema zahtevu 2, pri čemu n jeste 0.
4. Jedinjenje ili so za upotrebu prema zahtevu 3, pri čemu p jeste 1.
5. Jedinjenje ili so za upotrebu prema zahtevu 4, pri čemu R5b jeste H.
6. Jedinjenje ili so za upotrebu prema zahtevu 5, pri čemu a jeste 0.
7. Jedinjenje ili so za upotrebu prema zahtevu 6, pri čemu b jeste 0.
8. Jedinjenje ili so za upotrebu prema zahtevu 7, pri čemu R3b jeste fenil opciono supstituisan sa 1, 2, 3, 4 ili 5 supstituenata nezavisno izabranih od halo, C1-6 alkila, C2-6 alkenila, C1-6 alkinila, C1-4 haloalkila, Cy2, CN, NO2, ORe1, SRe1, C(O)Rf1, C(O)NRg1Rh1, C(O)ORe1, OC(O)Rf1, OC(O)NRg1Rh1, NRg1(O)NRg1Rh1, NRg1Rh1, NRg1C(O)Rf1, NRg1C(O)ORe1, P(Rf1)2, P(ORe1)2, P(O)Re1Rt1, P(O)ORe1ORf1, S(O)Rf1, S(O)NRg1Rh1, S(O)1Rf1 i S(O)2NRg1Rh1.
9. Jedinjenja ili so za upotrebu prema zahtevu 6, pri čemu b jeste 1.
10. Jedinjenja ili so za upotrebu prema zahtevu 9, pri čemu W jeste (CRaRb)t ili (CRaRb)uO(CRaRb)v.
11. Jedinjenje ili so za upotrebu prema zahtevu 10, pri čemu R3b je heteroaril, opciono supstituisan sa 1, 2, 3, 4 ili 5 supstituenata nezavisno izabranih od halo, C1-6 alkila, C2-6 alkenila, C2-6 alkinila, C1-4 haloalkila, Cy2, CN, NO2, ORe1, SRe1, C(O)Rf1, C(O)NRg1Rh1, C(O)ORe1, OC(O)Rf1, OC(O)NRg1Rh1, NRg1C(O)NRg1Rh1, Ng1Rh1, NRg1C(O)Rf1, NRg1C(O)ORe1 P(Rf1)2, P(ORe1)2, P(O)Re1Rf1, P(O)ORe1ORf1, S(O)Rf1, S(O)NRg1Rh1, S(O)2Rf1 i S(O)2NRg1Rh1.
12. Jedinjenje ili so za upotrebu prema zahtevu 1, pri čemu jedinjenje ima formulu: gde je: X1 (CRaRb)t ili (CRaRb)uC(O)(CRaRb)v; R3a je C1-8 alkil, C2-8 alkenil, C2-8 alkinil, aril, cikloalkil, heteroaril ili heterocikloalkil, svaki opciono supstituisan sa 1, 2, 3, 4 ili 5 supstituenata nezavisno izabranih od halo, C1-6 alkila, C2-6 alkenila, C2-6 alkinila, C1-4 haloalkila, C1-4 hidroksialkila, Cy1, CN, NO2, ORe1, SRe1, C(O)Rf1, C(O)NRg1Rh1, C(O)ORe1, OC(O)Rf1, OC(O)NRg1Rh1, NRg1C(O)NRg1Rh1, NRg1Rh1, NRg1C(O)Rf1, NRg1C(O)ORe1, C(=NRi)NRg1Rh1, NRg1C(=NRi)NRg1Rh1, P(Rf1)2, P(ORe1)2, P(O)Re1Rf1, P(O)ORe1Rf1, S(O)Rf1, S(O)NRg1Rh1, S(O)2Rf1 i S(O)2NRg1Rh1; R3b je aril ili heteroaril, svaki opciono supstituisan sa 1, 2, 3, 4 ili 5 supstituenata nezavisno izabranih od halo, C1-6 alkila, C2-6 alkenila, C2-6 alkinila, C1-4 haloalkila, C1-4 hidroksialkila, Cy2, CN, NO2, ORe1, SRe1, C(O)Rf1, C(O)NRg1Rh1, C(O)ORe1, OC(O)Rf1, OC(O)NRg1Rh1, NRg1C(O)NRg1Rh1, NRg1Rh1, NRg1C(O)Rf1, NRg1C(O)ORe1, C(=NRi)NRg1Rh1, NRg1C(=NRi)NRg1Rh1, P(Rf1)2, P(ORe1)2, P(O)Re1Rf1, P(O)ORe1ORf1, S(O)Rf1, S(O)NRg1Rh1, S(O)2Rf1 i S(O)2NRg1Rh1; R5b je H, C1-8 alkil, C2-8 alkenil, C2-8 alkinil, aril, cikloalkil, heteroaril ili heterocikloalkil; gde su spomenuti C1-8 alkil, C2-8 alkenil, C2-8 alkinil, aril, cikloalkil, heteroaril ili heterocikloalkil svaki opciono supstituisan sa 1, 2, 3, 4 ili 5 supstituenata nezavisno izabranih od halo, C1-6 alkila, C2-6 alkenila, C2-6 alkinila, C1-4 haloalkila, C1-4 hidroksialkila, Cy2, CN, NO2, ORe1, SRe1, C(O)Rf1, C(O)NRg1Rh1, C(O)ORe1, OC(O)Rf1, OC(O)NRg1Rh1, NRg1C(O)NRg1Rh1, NRg1R , NRg1C(O)Rf1, NRg1C(O)ORe1, C(=NRi)NRg1Rh1, NRg1C(=NRi)NRg1Rh1, P(Rf1)2, P(ORe1)2, P(O)Re1Rf1, P(O)ORe10Rf1, S(O)Rf1, S(O)NRg1Rh1, S(O)2Rf1 i S(O)2NRg1Rh1; Cy1 i Cy2 su nezavisno izabrani kao aril, heteroaril, cikloalkil i heterocikloalkil, svaki opciono supstituisan sa 1, 2, 3,4 ili 5 supstituenata nezavisno izabranih od halo, C1-4 alkila, C2-4 alkenila, C2-4 alkinila, C1-4 haloalkila, CN, NO2, ORe3, SRe3, C(O)Rf3, C(O)NRg3Rh3, C(O)ORe3, OC(O)Rf3, OC(O)NRg3Rh3, NRg3Rh3, NRg3C(O)Rh3, NRg3C(O)ORe3, C(=NRi)NRg1Rh1, NRg1C(=NRi)NRg1Rh1, P(Rf3)2, P(ORe3)2, P(O)Re3Rf3, P(O)ORe3ORf3, S(O)Rf3, S(O)NRg3Rh3, S(O)zRf3 i S(O)2NRg3Rh3; Ra i Rb su nezavisno izabrani od H, halo, C1-6 alkila, C2-6 alkenila, C2-6 alkinila, C1-4 haloalkila, arila, cikloalkila, heteroarila, heterocikloalkila, arilalkila, cikloalkilalkila, heteroarilalkila, heterocikloalkilalkila, CN, NO2, ORe4, SRe4, C(O)Rf4, C(O)NRg4Rh4, C(O)ORe4, OC(O)Rf4, OC(O)NRg4Rh4, NRg4Rh4, NRg4C(O)Rh4, NRg4C(O)ORe4, C(=NRi)NRg1Rh1, NRg1C(=NRi)NRg1Rh1, P(Rf4)2, P(ORe4)2 P(O)Re4Rf4, P(O)ORe4ORf4, S(O)Rf4, S(O)NRg4Rh4, S(O)2Rf4 i S(O)2NRg4Rh4; Re1, Re3 i Re4 su nezavisno izabrani 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; Rf1, Rf3 i Rf4 su nezavisno izabrani od H, C1-6 alkila, C1-6 haloalkila, C2-6 alkenila, C2-6 alkinila, arila, cikloalkila, heteroarila i heterocikloalkila; Rg1, Rg3 i Rg4 su nezavisno izabrani od H, C1-6 alkila, C1-6 haloalkila, C2-6 alkenila, C2-6 alkinila, arila, cikloalkila, arilalkila i cikloalkilalkila; Rh1, Rh3 i Rh4 su nezavisno izabrani od H, C1-6 alkila, C1-6 haloalkila, C2-6 alkenila, C2-6 alkinila, arila, cikloalkila, arilalkila i cikloalkilalkila; ili Rg1 i Rh1 zajedno sa N atomom za koji su vezani, formiraju 4-, 5-, 6- ili 7-očlanu heterocikloalkil grupu; ili Rg3 i Rh3 zajedno sa N atomom za koji su vezani, formiraju 4-, 5-, 6- ili 7-očlanu heterocikloalkil grupu; ili Rg4 i Rh4 zajedno sa N atomom za koji su vezani, formiraju 4-, 5-, 6- ili 7-očlanu heterocikloalkil grupu; Ri je H, CN ili NO2; a je 0 ili 1; t je 1, 2, 3, 4, 5 ili 6; u je 0, 1, 2, 3, 4, 5 ili 6; i v je 0, 1, 2, 3, 4, 5 ili 6.
13. Jedinjenje ili so za upotrebu prema zahtevu 1, pri čemu je jedinjenje izabrano od: N-benzil-4-(benzilamino)-N’-hidroksi-1,2,5-oksadiazol-3-karboksimidamid; 4-[(anilinokarbonil)amino]-N-(3-hlorofenil)-N’-hidroksi-1,2,5-oksadiazol-3-karboksimidamid; Terc-butil{4-[({4-[(E,Z)-[(3-hlorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}amino)karbonil]benzil} karbamat; 4-(aminometil)-N-{4-[(E,Z)-[(3-hlorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}benzamid; 4-{[(benzilamino)karbonil]amino}-N-(3-bromo-4-fluorofenil)-N’-hidroksi-1,2,5-oksadiazol-3-karboksimidamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}morfolin-4-karboksamid; N-(3-bromo-4-fluorofenil)-N’-hidroksi-4-(metilamino)-1,2,5-oksadiazol-3-karboksimidamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}piperidin-4-karboksamid; Terc-butil4-{4-[({4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}amino) karbonil]benzil}piperazin-1-karboksilat; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-4-(piperazin-1-ilmetil) benzamid; 1-benzoil-N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}piperidin- 4-karboksamid; N(4)-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-N(1)-fenilpiperidin- 1,4-dikarboksamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-1-etilpiperidin-4- karboksamid; 4-[(benzoilamino)metil]-N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol- 3-il}benzamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-2-(2-cijanofenoksi) acetamid; N-{4-[(E,Z-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-4-fenilpiperidin-4-karboksamid; N-(3-bromo-4-fluorofenil)-4-({4-[(1,1-dioksidotiomorfolin-4-il)metil]benzil}amino)-N’-hidroksi-1,2,5-oksadiazol-3-karboksimidamid; N-(3-bromo-4-fluorofenil)-N’-hidroksi-4-{[4-(morfolin-4-ilmetil)benzil]amino}-1,2,5-oksadiazol-3-karboksimidamid; N-(3-cijano-4-fluorofenil)-4-({4-[(1,1-dioksidotiomorfolin-4-il)metil]benzil}amino)-N’-hidroksi-1,2,5-oksadiazol-3-karboksimidamid; N-(3-bromo-4-fluorofenil)-N’-hidroksi-4-[(piridin-3-ilmetil)amino]-1,2,5-oksadiazol-3-karboksimidamid; N-(3-cijano-4-fluorofenil)-N’-hidroksi-4-[(piridin-4-ilmetil)amino]-1,2,5-oksadiazol-3-karboksimidamid; 4-[(3-cijanobenzil)amino]-N-(3-cijano-4-fluorofenil)-N’-hidroksi-1,2,5-oksadiazol-3-karboksimidamid; N-(3-bromo-4-fluorofenil)-N’-hidroksi-4-[(1H-tetrazol-5-ilmetil)amino]-1,2,5-oksadiazol-3-karboksimidamid; N-{4-[(E,Z)-[(3-hlorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}ciklopentankarboksamid; N-{4-[(E,Z)-[(3-hlorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}nikotinamid; N-{4-[(E,Z)-[(3-hlorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il} izonikotinamid; N-{4-[(E,Z-[(3-hlorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-2-metoksibenzamid; N-{4-[(E,Z)-[(3-hlorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-3-metoksibenzamid; N-{4-[(E,Z)-[(3-hlorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-4-metoksibenzamid; 2-hloro-N-{4-[(E,Z)-[(3-hlorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}benzamid; 3-hloro-N-{4-[(E,Z)-[(3-hlorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}benzamid; 4-hloro-N-{4-[(E,Z)-[(3-hlorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}benzamid; N-{4-[(E,Z)-[(3-hlorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-3,3-dimetilbutanamid; N-{4-[(E,Z)-[(3-hlorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-4-jodobenzamid; N-{4-[(E,Z)-[(3-hlorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-4-cijanobenzamid; N-{4-[(E,Z)-{[4-fluoro-3-(trifluorometil)fenil]amino}(hidroksiimino)metil]-1,2,5-oksadiazol-3-il}nikotinamid; N-{4-[(E,Z-{[4-fluoro-3-(trifluorometil)fenil]amino}(hidroksiimino)metil]-1,2,5-oksadiazol-3-il}izonikotinamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}benzamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}nikotinamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il} izonikotinamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-4-cijanobenzamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-3-cijanobenzamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-2-naftamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-1-naftamid; 1-acetil-N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}piperidin-4-karboksamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-2-furamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}tiofen-2-karboksamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-1-fenil-5-(trifluorometil)- 1H-pirazol-4-karboksamid; 4-(acetilamino)-N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}benzamid Terc-butil {4-[({4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}amino)karbonil] benzil}karbamat N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-1-benzotiofen-2-karboksamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-1,3-tiazol-4-karboksamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-1-benzotiofen-3-karboksamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}tiofen-3-karboksamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-1H-imidazol-2-karboksamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-4-metil-1,2,3-tiadiazol-5-karboksamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-1,2,3-tiadiazol-4-karboksamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-2,1-benzizoksazol-3-karboksamid; 4-(aminometil)-N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}benzamid; N-(3-bromo-4-fluorofenil)-N’-hidroksi-4-({[(2-feniletil)amino]karbonil}amino)-1,2,5-oksadiazol-3-karboksimidamid; N-(3-bromo-4-fluorofenil)-4-{[(ciklopentilamino)karbonil]amino}-N’-hidroksi-1,2,5-oksadiazol-3-karboksimidamid; N-(3-bromo-4-fluorofenil)-4-({[(3-cijanofenil)amino]karbonil}amino)-N’-hidroksi-1,2,5-oksadiazol-3 -karboksimidamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-3-terc-butil-1-metil-1H-pirazol-5 -karboksamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-2-metoksiacetamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}ciklopentankarboksamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}butanamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-2-metilpropanamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}propanamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}cikloheksankarboksamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-1H-benzimidazol-5-karboksamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-2-fenoksiacetamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}ciklobutankarboksamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-3-metilbutanamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-3-piridin-3-ilpropanamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}kinolin-6-karboksamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-2-(4-hlorofenoksi)acetamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-2-(4-bromofenoksi)acetamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-2-(4-fluorofenoksi)acetamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-2-(4-terc-butilfenoksi) acetamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-2-(3-hlorofenoksi)acetamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-2-(3,4-dihlorofenoksi) acetamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-2-(2-naftiloksi)acetamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-2-(2,3-dihlorofenoksi) acetamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-2-(4-hlorofenoksi)-2-metilpropanamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-2-(2-hlorofenoksi)acetamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-2-(3-metoksifenoksi)acetamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-2-(4-metoksifenoksi)acetamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-2-(2-metoksifenoksi)acetamid; Benzil {4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}karbamat; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}acetamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}piperidin-1-karboksamid; N-(3-bromo-4-fluorofenil)-4-({[(3-cijanofenil)(metil)amino]karbonil}amino)-N’-hidroksi-1,2,5-oksadiazol-3-karboksimidamid; 4-({[benzil(metil)amino]karbonil}amino)-N-(3-bromo-4-fluorofenil)-N’-hidroksi-1,2,5-oksadiazol-3-karboksimidamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-2-fenilacetamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-2-(3-metoksifenil)acetamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-2-(4-metoksifenil)acetamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-2-(2-metoksifenil)acetamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-2-cijanobenzamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-3-(3-bromofenil)propanamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-3-(4-bromofenil)propanamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-3-(4-hlorofenil)propanamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-3-(3-hlorofenil)propanamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-3-(2-fluorofenil)propanamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-3-(3-fluorofenil)propanamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-3-(2-hlorofenil)propanamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-3-(3-metilfenil)propanamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-3-(3-(trifluorometil)fenil) propanamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-3-(4-fluorofenil)propanamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-3-(2-metoksifenil)propanamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-3-(3-metoksifenil)propanamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-3-(4-metoksifenil)propanamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-3-(4-metilfenil)propanamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-3-[4-(trifluorometil)fenil] propanamid; 3-[2,5-bis(trifluorometil)fenil]-N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}propanamid; 3-[3,5-bis(trifluorometil)fenil]-N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}propanamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-2-metil-3-fenilpropanamid; 2-benzil-N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-3,3-dimetilbutanamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-1-[4-(trifluorometil) pirimidin-2-il]piperidin-4-karboksamid; 1-benzil-N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-3-terc-butil-1H-pirazol-5-karboksamid; 2-(benziloksi)-N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}acetamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-1-(4-hlorofenil)ciklopentan karboksamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-3-fenoksibenzamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-2,4,6-trihlorobenzamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-2-metoksibenzamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-3-metoksibenzamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-2,2-difenilacetamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-4-(trifluorometoksi)benzamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-4-metoksibenzamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-3,4-dimetoksibenzamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-2-(2-nitrofenoksi)acetamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}bifenil-4-karboksamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-2-(2,6-dihlorobenzil)-1,3-tiazol-4-karboksamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-2,6-dimetoksibenzamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-4-nitrobenzamid; 5-bromo-N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}nikotinamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-3,3-dimetilbutanamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-2-(2-tienil)acetamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-4-fenilbutanamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-2,2-dimetilpropanamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-4-(morfolin-4-ilmetil)benzamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-4-[(1,1-dioksidotiomorfolin- 4-il)metil]benzamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-1-(fenilacetil)piperidin-4-karboksamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-1-(metilsulfonil)piperidin-4-karboksamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-2-piridin-4-il-1,3-tiazol-4-karboksamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-2-nitrobenzamid; N-(4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-3-nitrobenzamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-1-izopropilpiperidin-4-karboks amid; Terc-butil 4-{4-[({4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}amino)karbonil]-1,3-tiazol-2-il}piperidin-1-karboksilat; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-2-fenil-1,3-tiazol-4-karboks amid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-2-metil-1,3-tiazol-4-karboks amid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-2-piperidin-4-il-1,3-tiazol-4-karboksamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-2-(4-cijanofenoksi)acetamid; Terc-butil 3-[({4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}amino)karbonil] piperidin-1-karboksilat; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-3-(3-nitrofenil)propanamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-2-(3-nitrofenoksi)acetamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-2-(4-nitrofenoksi)acetamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}piperidin-3-karboksamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-4-metil-2-piridin-3-il-1,3-tiazol-5-karboksamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-4-metil-1,3-tiazol-5-karboks amid; 2-amino-N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-1,3-tiazol-4-karboks amid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-4-metil-2-pirazin-2-il-1,3-tiazol-5-karboksamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-4-metil-2-[4-(trifluorometil) fenil]-1,3-tiazol-5-karboksamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-2,4-dimetil-1,3-tiazol-5-karboksamid; 1-acetil-N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}pirolidin-2-karboks amid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-1,5-dimetil-1H-pirazol-3-karboksamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-5-hloro-1-metil-1H-pirazol-4-karboksamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-1,3-dimetil-1H-pirazol-5-karboksamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-1-metil-1H-imidazol-2-karboksamid; 4-[(acetilamino)metil]-N-{4-[(E,Z-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3- il}benzamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-4-metilpiperidin-4-karboks amid; 1-acetil-N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}piperidin-3-karboks amid; 1-acetil-N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-4-metilpiperidin- 4-karboksamid; 1-acetil-N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-4-fenilpiperidin- 4-karboksamid; 4-(benzilamino)-N-(3-bromo-4-fluorofenil)-N’-hidroksi-1,2,5-oksadiazol-3-karboksimidamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-1-etilpiperidin-3-karboksamid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-4-etilpiperazin-1-karboksamid; 4-acetil-N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}piperazin-1-karboks amid; N-{4-[(E,Z)-[(3-bromo-4-fluorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-2-(1-etilpiperidin- 4-il)-1,3-tiazol-4-karboksamid; N-(3-bromo-4-fluorofenil)-N’-hidroksi-4-[(1,3-tiazol-4-ilmetil)amino]-1,2,5-oksadiazol-3-karboksimidamid; N-(3-bromo-4-fluorofenil)-4-[(4-cijanobenzil)amino]-N’-hidroksi-1,2,5-oksadiazol-3-karboksimidamid; N-(3-bromo-4-fluorofenil)-N’-hidroksi-4-{[(1-metilpiperidin-4-il)metil]amino}-1,2,5-oksadiazol-3 -karboksimidamid; N-(3-bromo-4-fluorofenil)-N’-hidroksi-4-{[4-(piperazin-1-ilmetil)benzil]amino}-1,2,5-oksadiazol-3-karboksimidamid; N-(3-bromo-4-fluorofenil)-4-({4-[(4-etilpiperazin-1-il)metil]benzil}amino)-N’-hidroksi-1,2,5-oksadiazol-3-karboksimid amid; N-(3-bromo-4-fluorofenil)-N’-hidroksi-4-[(piridin-4-ilmetil)amino]-1,2,5-oksadiazol-3-karboksimidamid; i N-(3-bromo-4-fluorofenil)-4-[(3-cijanobenzil)amino]-N’-hidroksi-1,2,5-oksadiazol-3-karboksimidamid; N-{4-[[(3-hlorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}-2-fenilacetamid; N-{4-[[(3-hlorofenil)amino](hidroksiimino)metil]-1,2,5-oksadiazol-3-il}benzamid; i N-{4-[(benzilamino)(hidroksiimino)metil]-1,2,5-oksadiazol-3-il}benzamid; ili njihove farmaceutski prihvatljive soli.
14. Jedinjenje ili so za upotrebu prema zahtevu 1, pri čemu je spomenuti kancer izabran od kancera debelog creva, pankreasa, kancera dojke, kancera prostate, kancera pluća, kancera mozga, kancera jajnika, cervikalnog kancera, kancera testisa, kancera bubrega, kancera glave i vrata, limfoma, leukemije i melanoma.
MEP-2016-96A 2005-05-10 2006-05-09 Modulatori indoleamina 2,3-dioksigenaze i metode za upotrebu istih ME02461B (me)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US67950705P 2005-05-10 2005-05-10
EP12178315.3A EP2559690B1 (en) 2005-05-10 2006-05-09 Modulators of indoleamine 2,3-dioxygenase and methods of using the same

Publications (1)

Publication Number Publication Date
ME02461B true ME02461B (me) 2017-02-20

Family

ID=37396891

Family Applications (1)

Application Number Title Priority Date Filing Date
MEP-2016-96A ME02461B (me) 2005-05-10 2006-05-09 Modulatori indoleamina 2,3-dioksigenaze i metode za upotrebu istih

Country Status (32)

Country Link
US (6) US8034953B2 (me)
EP (3) EP1879573B1 (me)
JP (2) JP4990270B2 (me)
KR (2) KR101562549B1 (me)
CN (2) CN101212967A (me)
AR (1) AR054271A1 (me)
AU (1) AU2006244068B9 (me)
BR (2) BRPI0608604B8 (me)
CA (1) CA2606783C (me)
CR (1) CR9485A (me)
CY (2) CY1113989T1 (me)
DK (2) DK1879573T3 (me)
EA (1) EA026785B1 (me)
ES (2) ES2401482T3 (me)
GE (1) GEP20217221B (me)
HR (2) HRP20130220T1 (me)
HU (1) HUE029214T2 (me)
IL (2) IL186957A (me)
ME (1) ME02461B (me)
MX (1) MX2007013977A (me)
MY (1) MY153424A (me)
NO (2) NO340487B1 (me)
NZ (1) NZ562919A (me)
PL (2) PL1879573T3 (me)
PT (2) PT2559690T (me)
RS (2) RS54876B1 (me)
SG (3) SG10201809390QA (me)
SI (2) SI2559690T1 (me)
TW (1) TWI377060B (me)
UA (1) UA99897C2 (me)
WO (1) WO2006122150A1 (me)
ZA (1) ZA200709698B (me)

Families Citing this family (262)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
BRPI0307077A2 (pt) * 2002-01-22 2017-06-20 Biomatera Inc método para secar polímeros biodegradáveis
DE602006001511D1 (de) * 2005-02-04 2008-07-31 Ctg Pharma S R L Neue 4-aminochinolinderivate als antimalariamittel
EP2322553A3 (en) 2005-02-14 2011-11-16 Wyeth LLC Interleukin-17F antibodies and other IL-17F signaling antagonists and uses therefor
RS54876B1 (sr) * 2005-05-10 2016-10-31 Incyte Holdings Corp Modulatori indoleamina 2,3-dioksigenaze i metode za upotrebu istih
GB0512091D0 (en) * 2005-06-14 2005-07-20 Novartis Ag Organic compounds
DE102005053947A1 (de) * 2005-11-11 2007-05-16 Univ Ernst Moritz Arndt Neue Arzneimittel
ES2540561T3 (es) 2005-12-20 2015-07-10 Incyte Corporation N-hidroxiamidinoheterociclos como moduladores de indolamina 2,3-dioxigenasa
WO2007095050A2 (en) * 2006-02-09 2007-08-23 Incyte Corporation N-hydroxyguanidines as modulators of indoleamine 2,3-dioxygenase
CA2661017A1 (en) * 2006-08-24 2008-02-28 Novartis Ag Organic compounds
WO2008036652A2 (en) * 2006-09-19 2008-03-27 Incyte Corporation Amidines as modulators of indoleamine 2,3-dioxygenase
CL2007002650A1 (es) 2006-09-19 2008-02-08 Incyte Corp Compuestos derivados de heterociclo n-hidroxiamino; composicion farmaceutica, util para tratar cancer, infecciones virales y desordenes neurodegenerativos entre otras.
JP5319532B2 (ja) * 2006-09-19 2013-10-16 インサイト・コーポレイション インドールアミン２，３−ジオキシゲナーゼのモジュレーターとしてのｎ−ヒドロキシアミジノヘテロサイクル
KR20090053923A (ko) 2006-09-22 2009-05-28 노파르티스 아게 헤테로시클릭 유기 화합물
US20080182882A1 (en) * 2006-11-08 2008-07-31 Incyte Corporation N-hydroxyamidinoheterocycles as modulators of indoleamine 2,3-dioxygenase
EP2121671A1 (en) 2006-12-20 2009-11-25 Novartis AG 2-substituted 5-membered heterocycles as scd inhibitors
WO2008115804A1 (en) * 2007-03-16 2008-09-25 Lankenau Institute For Medical Research Novel ido inhibitors and methods of use thereof
US20090170842A1 (en) 2007-11-14 2009-07-02 University Of Kansas Brca1-based breast or ovarian cancer prevention agents and methods of use
EP2227233B1 (en) * 2007-11-30 2013-02-13 Newlink Genetics Ido inhibitors
US20090253706A1 (en) * 2008-04-03 2009-10-08 Muller Alexander J Methods and Compositions for the Treatment of Rheumatoid Arthritis and Other Inflammatory Diseases
ES2657963T3 (es) 2008-04-17 2018-03-07 Io Biotech Aps Inmunoterapia basada en indolamina 2,3-dioxigenasa
SMT201800206T1 (it) * 2008-07-08 2018-05-02 Incyte Holdings Corp 1,2,5-ossadiazoli come inibitori di indoleamina 2,3-diossigenasi
ES2428104T3 (es) * 2009-09-25 2013-11-05 Bayer Cropscience Ag N-(1,2,5-oxadiazol-3-il)benzamidas y su uso como herbicidas
JP2012041325A (ja) * 2010-08-23 2012-03-01 Bayer Cropscience Ag オキサジアゾリノン誘導体およびその有害生物の防除用途
PL2654758T3 (pl) 2010-12-22 2017-10-31 Idogen Ab Kompozycja zawierająca co najmniej dwa związki, która indukuje 2,3-dioksygenazę indolaminy (IDO) do leczenia zaburzenia autoimmunologicznego lub immunologicznego odrzucenia narządów
NO2694640T3 (me) 2011-04-15 2018-03-17
AU2012338879A1 (en) 2011-11-16 2014-06-05 Basf Se Substituted 1,2,5-oxadiazole compounds and their use as herbicides II
KR20140107280A (ko) * 2011-11-18 2014-09-04 바스프 에스이 치환된 1,2,5-옥사디아졸 화합물 및 이의 제초제 ｉｉｉ 로서의 용도
KR101229365B1 (ko) * 2012-07-02 2013-02-18 대한민국 〔ｚ〕­ｎ­〔３­〔２，４­디플루오로페닐아미노〕­１­〔４­나이트로페닐〕­３­옥소프로프­１­엔­２­일〕­２­메톡시벤즈아마이드를 유효성분으로 함유하는 신경퇴행성 질환 예방 및 치료용 약학적 조성물
EP2911669B1 (en) 2012-10-26 2024-04-10 The University of Chicago Synergistic combination of immunologic inhibitors for the treatment of cancer
CN105377812B (zh) 2013-06-21 2018-09-18 组合化学工业株式会社 2-氨基-2-肟基-n-烷氧基亚氨代乙酰基氰化物的制备方法及其制备中间体
GB201311891D0 (en) 2013-07-03 2013-08-14 Glaxosmithkline Ip Dev Ltd Novel compound
GB201311888D0 (en) 2013-07-03 2013-08-14 Glaxosmithkline Ip Dev Ltd Novel compounds
RU2536041C1 (ru) * 2013-10-11 2014-12-20 ФЕДЕРАЛЬНОЕ ГОСУДАРСТВЕННОЕ БЮДЖЕТНОЕ УЧРЕЖДЕНИЕ НАУКИ ИНСТИТУТ ОРГАНИЧЕСКОЙ ХИМИИ им. Н.Д. ЗЕЛИНСКОГО РОССИЙСКОЙ АКАДЕМИИ НАУК (ИОХ РАН) 3,3'-бис(фтординитрометил-onn-азокси)-4,4'-дифуразаниловый эфир и способ его получения
KR102370067B1 (ko) 2013-11-08 2022-03-04 인사이트 홀딩스 코포레이션 인돌아민 2,3-디옥시게나제 억제제의 합성 방법
CN103570727B (zh) 2013-11-12 2015-08-19 复旦大学 一种n-苄基色胺酮衍生物及其制备方法和应用
AU2014369982B2 (en) 2013-12-24 2019-04-18 Bristol-Myers Squibb Company Tricyclic compounds as anticancer agents
US20180228907A1 (en) 2014-04-14 2018-08-16 Arvinas, Inc. Cereblon ligands and bifunctional compounds comprising the same
CN106535884A (zh) * 2014-06-06 2017-03-22 弗雷克萨斯生物科学公司 免疫调节剂
PT3151921T (pt) 2014-06-06 2019-11-21 Bristol Myers Squibb Co Anticorpos contra recetor do fator de necrose tumoral induzido por glicocorticoide e utilizações dos mesmos
KR20250007032A (ko) * 2014-08-13 2025-01-13 오클랜드 유니서비시즈 리미티드 트립토판 디옥시게나제 (ido1 및 tdo)의 억제제 및 치료에서 이들의 용도
GB201414730D0 (en) 2014-08-19 2014-10-01 Tpp Global Dev Ltd Pharmaceutical compound
US10183082B2 (en) * 2014-09-09 2019-01-22 H. Lee Moffitt Cancer Center And Research Institute, Inc. PET probes of radiofluorinated carboximidamides for IDO-targeted imaging
CN105481789B (zh) 2014-09-15 2020-05-19 中国科学院上海有机化学研究所 一种吲哚胺-2,3-双加氧酶抑制剂及其制备方法
UY36390A (es) 2014-11-05 2016-06-01 Flexus Biosciences Inc Compuestos moduladores de la enzima indolamina 2,3-dioxigenasa (ido), sus métodos de síntesis y composiciones farmacéuticas que los contienen
UY36391A (es) 2014-11-05 2016-06-01 Flexus Biosciences Inc Compuestos moduladores de la enzima indolamina 2,3-dioxigenasa (ido1), sus métodos de síntesis y composiciones farmacèuticas que las contienen
MX2017005462A (es) 2014-11-05 2017-07-28 Flexus Biosciences Inc Agentes inmunorreguladores.
UY36404A (es) 2014-11-21 2016-06-01 Bristol Myers Squibb Company Una Corporación Del Estado De Delaware ANTICUERPOS MONOCLONALES (Ab) COMO DETECTORES DE CD73 E INHIBIDORES DE SU ACTIVIDAD ENZIMÁTICA, Y COMPOSICIONES QUE LOS CONTIENEN
US10525035B2 (en) 2014-12-18 2020-01-07 Lankenau Institute For Medical Research Methods and compositions for the treatment of retinopathy and other ocular diseases
TW201630907A (zh) 2014-12-22 2016-09-01 必治妥美雅史谷比公司 ＴＧＦβＲ拮抗劑
US10189902B2 (en) 2014-12-23 2019-01-29 Bristol-Myers Squibb Company Antibodies to TIGIT
WO2016127052A1 (en) 2015-02-05 2016-08-11 Bristol-Myers Squibb Company Cxcl11 and smica as predictive biomarkers for efficacy of anti-ctla4 immunotherapy
ES2789331T3 (es) 2015-03-02 2020-10-26 Rigel Pharmaceuticals Inc Inhibidores de TGF-beta
EA201792186A1 (ru) 2015-04-03 2018-03-30 Бристол-Майерс Сквибб Компани Ингибиторы индоламин-2,3-диоксигеназы и способы их применения
WO2016162505A1 (en) 2015-04-08 2016-10-13 F-Star Biotechnology Limited Her2 binding agent therapies
PL3283527T3 (pl) 2015-04-13 2021-06-14 Five Prime Therapeutics, Inc. Leczenie skojarzone nowotworów
US10899764B2 (en) 2015-04-21 2021-01-26 Jiangsu Hengrui Medicine Co., Ltd. Imidazo isoindole derivative, preparation method therefor and medical use thereof
US10683290B2 (en) 2015-05-11 2020-06-16 Bristol-Myers Squibb Company Tricyclic compounds as anticancer agents
WO2016183115A1 (en) 2015-05-12 2016-11-17 Bristol-Myers Squibb Company 5h-pyrido[3,2-b]indole compounds as anticancer agents
US9725449B2 (en) 2015-05-12 2017-08-08 Bristol-Myers Squibb Company Tricyclic compounds as anticancer agents
IL293135A (en) 2015-05-13 2022-07-01 Agenus Inc Composition comprising at least two different complexes of a purified stress protein bound to an antigenic peptide
WO2016196228A1 (en) 2015-05-29 2016-12-08 Bristol-Myers Squibb Company Antibodies against ox40 and uses thereof
UY36757A (es) 2015-06-29 2016-12-30 Bristol Myers Squibb Company Una Corporación Del Estado De Delaware Anticuerpos monoclonales murinos contra cd40 con actividad agonista mejorada
RU2018101431A (ru) * 2015-07-02 2019-08-05 Глаксосмитклайн Интеллекчуал Проперти Дивелопмент Лимитед Ингибиторы индоламин-2,3-диоксигеназы
GB201511790D0 (en) 2015-07-06 2015-08-19 Iomet Pharma Ltd Pharmaceutical compound
EP3322444A4 (en) 2015-07-14 2019-06-12 Kyowa Hakko Kirin Co., Ltd. THERAPEUTIC FOR A TUMOR WITH AN IDO INHIBITOR IN COMBINATION WITH AN ANTIBODY
US10682390B2 (en) 2015-07-16 2020-06-16 Biokine Therapeutics Ltd. Compositions and methods for treating cancer
AU2016298471C1 (en) 2015-07-24 2020-03-05 Newlink Genetics Corporation Salts and prodrugs of 1-methyl-D-tryptophan
KR20180034548A (ko) 2015-07-28 2018-04-04 브리스톨-마이어스 스큅 컴퍼니 Tgf 베타 수용체 길항제
JP2018525415A (ja) 2015-08-25 2018-09-06 ブリストル−マイヤーズ スクイブ カンパニーＢｒｉｓｔｏｌ−Ｍｙｅｒｓ Ｓｑｕｉｂｂ Ｃｏｍｐａｎｙ Ｔｇｆベータ受容体アンタゴニスト
CN106565696B (zh) * 2015-10-09 2020-07-28 江苏恒瑞医药股份有限公司 噁二唑类衍生物、其制备方法及其在医药上的应用
EP3371208B8 (en) 2015-11-02 2024-10-23 Five Prime Therapeutics, Inc. Cd80 extracellular domain polypeptides and their use in cancer treatment
JP2019500893A (ja) 2015-11-03 2019-01-17 ヤンセン バイオテツク，インコーポレーテツド Ｐｄ−１及びｔｉｍ−３に特異的に結合する抗体及びそれらの使用
JP2018532756A (ja) 2015-11-04 2018-11-08 インサイト・コーポレイションＩｎｃｙｔｅ Ｃｏｒｐｏｒａｔｉｏｎ インドールアミン２，３−ジオキシゲナーゼを阻害するための医薬組成物と方法、及びその適応
AU2016356780A1 (en) 2015-11-19 2018-06-28 Bristol-Myers Squibb Company Antibodies against glucocorticoid-induced tumor necrosis factor receptor (GITR) and uses thereof
AU2016359609B2 (en) 2015-11-23 2023-12-07 Five Prime Therapeutics, Inc. FGFR2 inhibitors alone or in combination with immune stimulating agents in cancer treatment
RU2020113165A (ru) 2015-12-03 2020-06-09 Глэксосмитклайн Интеллекчуал Проперти Дивелопмент Лимитед Циклические пуриновые динуклеотиды в качестве модуляторов sting
CN108602829A (zh) 2015-12-15 2018-09-28 百时美施贵宝公司 Cxcr4受体拮抗剂
WO2017106062A1 (en) 2015-12-15 2017-06-22 Merck Sharp & Dohme Corp. Novel compounds as indoleamine 2,3-dioxygenase inhibitors
CN106883193B (zh) * 2015-12-15 2021-10-15 上海翰森生物医药科技有限公司 吲哚胺2,3-双加氧酶抑制剂及其制备方法与应用
CN106883194A (zh) * 2015-12-16 2017-06-23 江苏恒瑞医药股份有限公司 噁二唑类衍生物、其制备方法及其在医药上的应用
US9624185B1 (en) * 2016-01-20 2017-04-18 Yong Xu Method for preparing IDO inhibitor epacadostat
CN105646389B (zh) * 2016-01-28 2019-06-28 中国科学院上海有机化学研究所 一种作为吲哚胺-2,3-双加氧酶抑制剂的氨基磺酸脂及其制备方法和用途
AU2017215424A1 (en) 2016-02-02 2018-08-09 Emcure Pharmaceuticals Limited Derivatives of pyrroloimidazole or analogues thereof which are useful for the treatment of inter alia cancer
CN107033097B (zh) * 2016-02-04 2022-02-08 江苏恒瑞医药股份有限公司 噁二唑类衍生物、其制备方法及其在医药上的应用
EP3416725A1 (en) * 2016-02-19 2018-12-26 INSERM (Institut National de la Santé et de la Recherche Médicale) Methods and pharmaceutical compositions for the treatment of obesity
TW201736373A (zh) * 2016-02-19 2017-10-16 Chia Tai Tianqing Pharmaceutical Group Co Ltd 作為免疫調節劑的三並環化合物
WO2017149469A1 (en) 2016-03-03 2017-09-08 Emcure Pharmaceuticals Limited Heterocyclic compounds useful as ido and/or tdo modulators
CA3016187A1 (en) 2016-03-04 2017-09-08 Bristol-Myers Squibb Company Combination therapy with anti-cd73 antibodies
CN107176933B (zh) * 2016-03-09 2020-10-09 中国科学院上海有机化学研究所 一种含氮烷基化和芳基化亚砜亚胺的吲哚胺-2,3-双加氧酶抑制剂
IL295649B2 (en) 2016-04-07 2025-12-01 Glaxosmithkline Ip Dev Ltd Heterocyclic amides useful as protein modulators
WO2017175156A1 (en) 2016-04-07 2017-10-12 Glaxosmithkline Intellectual Property Development Limited Heterocyclic amides useful as protein modulators
EP3445783A2 (en) 2016-04-18 2019-02-27 Celldex Therapeutics, Inc. Agonistic antibodies that bind human cd40 and uses thereof
WO2017181849A1 (zh) * 2016-04-20 2017-10-26 江苏豪森药业集团有限公司 吲哚胺2,3-双加氧酶抑制剂及其制备方法与应用
CN107304191B (zh) * 2016-04-20 2023-09-29 上海翰森生物医药科技有限公司 吲哚胺2,3-双加氧酶抑制剂及其制备方法与应用
US10696648B2 (en) 2016-05-04 2020-06-30 Bristol-Myers Squibb Company Inhibitors of indoleamine 2,3-dioxygenase and methods of their use
JP2019516682A (ja) 2016-05-04 2019-06-20 ブリストル−マイヤーズ スクイブ カンパニーＢｒｉｓｔｏｌ−Ｍｙｅｒｓ Ｓｑｕｉｂｂ Ｃｏｍｐａｎｙ インドールアミン２，３−ジオキシゲナーゼ阻害剤およびその使用方法
EP3452451A4 (en) 2016-05-04 2019-11-13 Bristol-Myers Squibb Company INDOLEAMINE 2,3-DIOXYGENASE INHIBITORS AND METHODS OF USE
WO2017192840A1 (en) 2016-05-04 2017-11-09 Bristol-Myers Squibb Company Inhibitors of indoleamine 2,3-dioxygenase and methods of their use
KR20190004743A (ko) * 2016-05-04 2019-01-14 브리스톨-마이어스 스큅 컴퍼니 인돌아민 2,3-디옥시게나제의 억제제 및 그의 사용 방법
JOP20170131B1 (ar) * 2016-06-10 2021-08-17 Lilly Co Eli مركبات 1-تيترا هيدروبيرانييل كاربونيل -2،3-ديهيدرو -1 h- اندول لعلاج السرطان
BR112019000431A2 (pt) 2016-07-14 2019-07-09 Bristol-Myers Squibb Company anticorpos contra tim3 e usos dos mesmos
EP3487503A1 (en) 2016-07-20 2019-05-29 GlaxoSmithKline Intellectual Property Development Limited Isoquinoline derivatives as perk inhibitors
US20190292179A1 (en) 2016-07-21 2019-09-26 Bristol-Myers Squibb Company TGF Beta RECEPTOR ANTAGONISTS
WO2018024208A1 (zh) * 2016-08-02 2018-02-08 南京明德新药研发股份有限公司 Ido1抑制剂及其制备方法和应用
WO2018039430A1 (en) * 2016-08-24 2018-03-01 H. Lee Moffitt Cancer Center & Research Institute, Inc. Radiofluorinated carboximidamides as ido targeting pet tracer for cancer imaging
WO2018039518A1 (en) 2016-08-26 2018-03-01 Bristol-Myers Squibb Company Inhibitors of indoleamine 2,3-dioxygenase and methods of their use
WO2018044663A1 (en) * 2016-08-29 2018-03-08 Merck Sharp & Dohme Corp. Novel substituted n'-hydroxycarbamimidoyl-1,2,5-oxadiazole compounds as indoleamine 2,3-dioxygenase (ido) inhibitors
EP4268838A3 (en) 2016-09-19 2023-12-27 University Of South Florida Method of targeting oncolytic viruses to tumors
WO2018054365A1 (en) 2016-09-24 2018-03-29 Beigene, Ltd. NOVEL 5 or 8-SUBSTITUTED IMIDAZO [1, 5-a] PYRIDINES AS SELECTIVE INHIBITORS OF INDOLEAMINE AND/OR TRYPTOPHANE 2, 3-DIOXYGENASES
WO2018072697A1 (zh) * 2016-10-17 2018-04-26 上海医药集团股份有限公司 含噁二唑环化合物、制备方法、中间体、组合物及应用
UY37466A (es) 2016-11-03 2018-01-31 Phenex Discovery Verwaltungs Gmbh N-hidroxiamidinheterociclos sustituidos como moduladores de la indolamina 2,3-dioxigenasa
EP3544965A4 (en) 2016-11-28 2020-05-20 Shanghai Fochon Pharmaceutical Co., Ltd. Sulfoximine, sulfonimidamide, sulfondiimine and diimidosulfonamide compounds as inhibitors of indoleamine 2, 3-dioxygenase
CN106883224B (zh) * 2017-01-03 2019-10-22 中国药科大学 苯并含氮杂环类吲哚胺-2,3-双加氧酶1抑制剂及其用途
CN106866648B (zh) * 2017-01-03 2019-10-22 中国药科大学 邻苯二甲酰亚胺类吲哚胺-2,3-双加氧酶1抑制剂及其用途
US10961239B2 (en) 2017-01-05 2021-03-30 Bristol-Myers Squibb Company TGF beta receptor antagonists
CA3047002A1 (en) 2017-01-17 2018-07-26 Board Of Regents, The University Of Texas System Compounds useful as inhibitors of indoleamine 2,3-dioxygenase and/or tryptophan dioxygenase
CN106866571B (zh) * 2017-01-20 2018-06-29 中国药科大学 杂环脲类化合物及其药物组合物和应用
EP3585774B1 (en) * 2017-02-24 2021-11-10 Merck Sharp & Dohme Corp. Novel substituted sulfoximine compounds as indoleamine 2,3-dioxygenase (ido) inhibitors
CN106967004B (zh) * 2017-03-29 2019-09-17 中国药科大学 含脲基的ido1和ido2双重抑制剂、其制法及其医药用途
KR20190133171A (ko) * 2017-03-29 2019-12-02 머크 샤프 앤드 돔 코포레이션 인돌아민 2,3-디옥시게나제 (ido) 억제제로서의 신규 치환된 n'-히드록시카르밤이미도일-1,2,5-옥사디아졸 화합물
US20200031944A1 (en) 2017-03-31 2020-01-30 Five Prime Therapeutics, Inc. Combination therapy for cancer using anti-gitr antibodies
CN108689958B (zh) * 2017-04-05 2021-09-17 南京华威医药科技集团有限公司 一种含有肼基的吲哚胺2,3-双加氧化酶抑制剂
TWI788340B (zh) 2017-04-07 2023-01-01 美商必治妥美雅史谷比公司 抗icos促效劑抗體及其用途
CN110831600B (zh) 2017-04-21 2023-10-17 医肯纳肿瘤学公司 吲哚ahr抑制剂和其用途
US11046679B2 (en) 2017-04-24 2021-06-29 Nanjing Transthera Biosciences Co. Ltd. Indoleamine 2,3-dioxygenase inhibitor and application
CN108794423B (zh) * 2017-04-27 2022-07-19 鲁南制药集团股份有限公司 亚氨脲衍生物
EP3628070B1 (en) 2017-04-28 2021-09-08 Five Prime Therapeutics, Inc. Cd80 extracellular domain polypeptides for use in increasing central memory t cells
US11066392B2 (en) 2017-05-12 2021-07-20 Bristol-Myers Squibb Company Inhibitors of indoleamine 2,3-dioxygenase and methods of their use
CN109081818B (zh) * 2017-06-14 2022-04-22 南京华威医药科技集团有限公司 新型吲哚胺2,3-双加氧化酶抑制剂
CN109111438B (zh) * 2017-06-26 2021-11-02 正大天晴药业集团股份有限公司 用于ido抑制剂的脒类化合物
US11236049B2 (en) 2017-06-30 2022-02-01 Bristol-Myers Squibb Company Amorphous and crystalline forms of IDO inhibitors
CN110891942B (zh) * 2017-07-14 2022-06-07 四川科伦博泰生物医药股份有限公司 噁二唑类衍生物、其制备方法及其在医药上的应用
WO2019021208A1 (en) 2017-07-27 2019-01-31 Glaxosmithkline Intellectual Property Development Limited USEFUL INDAZOLE DERIVATIVES AS PERK INHIBITORS
ES2932354T3 (es) 2017-07-28 2023-01-18 Bristol Myers Squibb Co Dinucleótidos cíclicos como agentes anticáncer
BR112020003116A2 (pt) 2017-08-17 2020-08-04 Ikena Oncology, Inc. inibidores de ahr e usos dos mesmos
ES2904317T3 (es) 2017-08-31 2022-04-04 Bristol Myers Squibb Co Dinucleótidos cíclicos como agentes anticancerosos
EP3675877A1 (en) 2017-08-31 2020-07-08 Multimmune GmbH Hsp70 based combination therapy
KR102651946B1 (ko) 2017-08-31 2024-03-26 브리스톨-마이어스 스큅 컴퍼니 항암제로서의 시클릭 디뉴클레오티드
US11667663B2 (en) 2017-08-31 2023-06-06 Bristol-Myers Squibb Company Cyclic dinucleotides as anticancer agents
CN109422739B (zh) * 2017-09-01 2022-07-12 药捷安康(南京)科技股份有限公司 氘代的吲哚胺2，3-双加氧酶抑制剂及其应用
CN108863976B (zh) * 2017-09-11 2022-09-16 郑州泰基鸿诺医药股份有限公司 用作ido调节剂的化合物及其应用
EP4176876A1 (en) 2017-09-14 2023-05-10 Lankenau Institute for Medical Research Methods and compositions for the treatment of cancer
JP7291130B2 (ja) 2017-10-05 2023-06-14 グラクソスミスクライン、インテレクチュアル、プロパティー、ディベロップメント、リミテッド インターフェロン遺伝子の刺激物質（ｓｔｉｎｇ）の調節物質
EP3692033A1 (en) 2017-10-05 2020-08-12 GlaxoSmithKline Intellectual Property Development Limited Modulators of stimulator of interferon genes (sting) useful in treating hiv
EP3694502B1 (en) * 2017-10-09 2023-08-02 Merck Sharp & Dohme LLC Novel substituted cyclobutylbenzene compounds as indoleamine 2,3-dioxygenase (ido) inhibitors
US11111232B2 (en) 2017-10-09 2021-09-07 Merck Sharp & Dohme Corp. Substituted cyclobutylpyridine and cyclobutylpyrimidine compounds as indoleamine 2,3-dioxygenase (IDO) inhibitors
US11649212B2 (en) 2017-10-09 2023-05-16 Bristol-Myers Squibb Company Inhibitors of indoleamine 2,3-dioxygenase and methods of their use
WO2019074824A1 (en) 2017-10-09 2019-04-18 Bristol-Myers Squibb Company INDOLEAMINE 2,3-DIOXYGENASE INHIBITORS AND METHODS OF USE
WO2019075090A1 (en) 2017-10-10 2019-04-18 Tilos Therapeutics, Inc. ANTI-LAP ANTIBODIES AND USES THEREOF
KR102885797B1 (ko) 2017-10-10 2025-11-12 브리스톨-마이어스 스큅 컴퍼니 항암제로서의 시클릭 디뉴클레오티드
WO2019079261A1 (en) 2017-10-16 2019-04-25 Bristol-Myers Squibb Company CYCLIC DINUCLEOTIDES AS ANTICANCER AGENTS
CN109678813A (zh) * 2017-10-18 2019-04-26 中国科学院上海有机化学研究所 吲哚胺-2,3-双加氧酶抑制剂盐及其制备方法
KR20200074214A (ko) 2017-11-01 2020-06-24 브리스톨-마이어스 스큅 컴퍼니 암을 치료하는데 사용하기 위한 면역자극 효능작용 항체
CN109748911B (zh) * 2017-11-06 2022-03-11 中国药科大学 一种含三氮唑的ido抑制剂、其制备方法及其医药用途
ES2925450T3 (es) 2017-11-06 2022-10-18 Bristol Myers Squibb Co Compuestos de isofuranona útiles como inhibidores de HPK1
CN107987031A (zh) * 2017-12-01 2018-05-04 华东理工大学 一种靶向吲哚胺-2,3-双加氧酶1氮芥类抑制剂及其制备方法和应用
US20200352931A1 (en) 2017-12-12 2020-11-12 Phenex Discovery Verwaltungs-GmbH Oxalamides as modulators of indoleamine 2,3-dioxygenase
CN108003111A (zh) * 2017-12-14 2018-05-08 华东理工大学 一种hdac1和ido1双靶点抑制剂及其制备方法和应用
CN109942565B (zh) * 2017-12-20 2021-03-26 海创药业股份有限公司 一种吲哚胺-2,3-双加氧酶抑制剂及其制备方法和用途
EP3732198A1 (en) 2017-12-27 2020-11-04 Bristol-Myers Squibb Company Anti-cd40 antibodies and uses thereof
US11813280B2 (en) 2018-01-05 2023-11-14 Dicerna Pharmaceuticals, Inc. Reducing beta-catenin and IDO expression to potentiate immunotherapy
WO2019136112A1 (en) 2018-01-05 2019-07-11 Bristol-Myers Squibb Company Inhibitors of indoleamine 2,3-dioxygenase and methods of their use
CN111886255B (zh) 2018-01-12 2025-04-04 百时美施贵宝公司 抗tim3抗体及其用途
CN110054622B (zh) * 2018-01-18 2021-02-23 四川科伦博泰生物医药股份有限公司 噁二唑类衍生物、其制备方法及其在医药上的应用
US12398209B2 (en) 2018-01-22 2025-08-26 Janssen Biotech, Inc. Methods of treating cancers with antagonistic anti-PD-1 antibodies
CN108586378B (zh) 2018-01-22 2020-06-19 南京华威医药科技集团有限公司 吲哚胺2,3-双加氧化酶抑制剂及其制备方法和用途
CN110092750B (zh) 2018-01-29 2023-07-21 北京诺诚健华医药科技有限公司 五氟硫烷基取代的酰胺类化合物、其制备方法及其在医药学上的应用
US10519187B2 (en) 2018-02-13 2019-12-31 Bristol-Myers Squibb Company Cyclic dinucleotides as anticancer agents
CN110156674A (zh) * 2018-02-13 2019-08-23 中国科学院上海有机化学研究所 一种作为吲哚胺-2,3-双加氧酶抑制剂的螺环化合物
JP7250808B2 (ja) 2018-03-08 2023-04-03 ブリストル－マイヤーズ スクイブ カンパニー 抗がん剤としての環状ジヌクレオチド
TW201945393A (zh) 2018-03-21 2019-12-01 美商戊瑞治療有限公司 在酸性pH結合至VISTA之抗體
CA3093407A1 (en) 2018-03-23 2019-09-26 Bristol-Myers Squibb Company Antibodies against mica and/or micb and uses thereof
US20210122757A1 (en) 2018-03-29 2021-04-29 Phenex Discovery Verwaltungs-GmbH Spirocyclic compounds as modulators of indoleamine 2,3-dioxygenase
JP2021521182A (ja) 2018-04-12 2021-08-26 ブリストル−マイヤーズ スクイブ カンパニーＢｒｉｓｔｏｌ−Ｍｙｅｒｓ Ｓｑｕｉｂｂ Ｃｏｍｐａｎｙ Ｃｄ７３アンタゴニストとｐｄ−１／ｐｄ−ｌ１軸アンタゴニストの組み合わせ治療
US20190314324A1 (en) 2018-04-13 2019-10-17 The University Of Chicago Combination of micheliolide derivatives or nanoparticles with ionizing radiation and checkpoint inhibitors for cancer therapy
CA3096546A1 (en) 2018-04-16 2019-10-24 Arrys Therapeutics, Inc. Ep4 inhibitors and use thereof
WO2019206800A1 (en) 2018-04-24 2019-10-31 Phenex Discovery Verwaltungs-GmbH Spirocyclic compounds as modulators of indoleamine 2,3-dioxygenase
WO2019213340A1 (en) 2018-05-03 2019-11-07 Bristol-Myers Squibb Company Uracil derivatives as mer-axl inhibitors
GB201807924D0 (en) 2018-05-16 2018-06-27 Ctxt Pty Ltd Compounds
CN110526898A (zh) 2018-05-25 2019-12-03 北京诺诚健华医药科技有限公司 3-吲唑啉酮类化合物、其制备方法及其在医药学上的应用
GB201809050D0 (en) 2018-06-01 2018-07-18 E Therapeutics Plc Modulators of tryptophan catabolism
SI3814348T1 (sl) 2018-06-27 2023-10-30 Bristol-Myers Squibb Company Substituirane naftiridinonske spojine, uporabne kot aktivatorji t celic
HRP20230627T1 (hr) 2018-06-27 2023-09-29 Bristol-Myers Squibb Company Spojevi naftiridinona korisni kao aktivatori t ćelija
SG11202100096XA (en) 2018-07-09 2021-02-25 Five Prime Therapeutics Inc Antibodies binding to ilt4
CN121203021A (zh) 2018-07-11 2025-12-26 戊瑞治疗有限公司 在酸性pH下结合至VISTA的抗体
EP3823604A4 (en) 2018-07-17 2022-03-16 Board of Regents, The University of Texas System COMPOUNDS AS INHIBITORS OF INDOLAMINE-2,3-DIOXYGENASE AND/OR TRYPTOPHANE DIOXYGENASE
US12145927B2 (en) 2018-07-23 2024-11-19 Bristol-Myers Squibb Company Inhibitors of indoleamine 2,3-dioxygenase and methods of their use
WO2020023355A1 (en) 2018-07-23 2020-01-30 Bristol-Myers Squibb Company Inhibitors of indoleamine 2,3-dioxygenase and methods of their use
US10959986B2 (en) 2018-08-29 2021-03-30 Bristol-Myers Squibb Company Inhibitors of indoleamine 2,3-dioxygenase and methods of their use
US11253525B2 (en) 2018-08-29 2022-02-22 Bristol-Myers Squibb Company Inhibitors of indoleamine 2,3-dioxygenase and methods of their use
WO2020076969A2 (en) 2018-10-10 2020-04-16 Tilos Therapeutics, Inc. Anti-lap antibody variants and uses thereof
AU2019380307B2 (en) 2018-11-16 2026-01-29 Bristol-Myers Squibb Company Anti-NKG2A antibodies and uses thereof
AR117200A1 (es) * 2018-11-30 2021-07-21 Syngenta Participations Ag Derivados de tiazol microbiocidas
CN111689952A (zh) * 2019-03-14 2020-09-22 复旦大学 含硫代四元环结构的2,3-双加氧酶抑制剂及其制备方法和用途
CN111909107B (zh) * 2019-05-10 2023-02-03 药康众拓(江苏)医药科技有限公司 Ido/hdac双重抑制剂及其药物组合物和应用
WO2020231713A1 (en) 2019-05-13 2020-11-19 Bristol-Myers Squibb Company AGONISTS OF ROR GAMMAt
WO2020231766A1 (en) 2019-05-13 2020-11-19 Bristol-Myers Squibb Company AGONISTS OF ROR GAMMAt
CN111943906B (zh) * 2019-05-14 2023-12-15 中国医学科学院药物研究所 脒类衍生物、及其制法和药物组合物与用途
EP3969438A1 (en) 2019-05-16 2022-03-23 Stingthera, Inc. Oxoacridinyl acetic acid derivatives and methods of use
JP2022533194A (ja) 2019-05-16 2022-07-21 スティングセラ インコーポレイテッド ベンゾ［ｂ］［１，８］ナフチリジン酢酸誘導体および使用方法
CN112062732B (zh) * 2019-06-10 2023-10-24 鲁南制药集团股份有限公司 一种ido抑制剂及其组合物、制备方法和用途
GB201910304D0 (en) 2019-07-18 2019-09-04 Ctxt Pty Ltd Compounds
GB201910305D0 (en) 2019-07-18 2019-09-04 Ctxt Pty Ltd Compounds
US20220306630A1 (en) 2019-08-06 2022-09-29 Bristol-Myers Squibb Company AGONISTS OF ROR GAMMAt
AR119821A1 (es) 2019-08-28 2022-01-12 Bristol Myers Squibb Co Compuestos de piridopirimidinonilo sustituidos útiles como activadores de células t
AU2020350689A1 (en) 2019-09-19 2022-03-31 Bristol-Myers Squibb Company Antibodies binding to VISTA at acidic pH
JP7629459B2 (ja) 2019-11-19 2025-02-13 ブリストル－マイヤーズ スクイブ カンパニー Ｈｅｌｉｏｓタンパク質の阻害剤として有用な化合物
CN115151306A (zh) 2019-11-26 2022-10-04 百时美施贵宝公司 (r)-n-(4-氯苯基)-2-((1s，4s)-4-(6-氟喹啉-4-基)环己基)丙酰胺的盐/共晶
FI4065582T3 (fi) 2019-11-26 2025-05-25 Ikena Oncology Inc Polymorfisia karbatsolijohdannaisia ja niiden käyttötapoja
JP7662644B2 (ja) 2019-12-18 2025-04-15 シーティーエックスティー・ピーティーワイ・リミテッド 化合物
IL294269A (en) 2019-12-23 2022-08-01 Bristol Myers Squibb Co Substituted quinolinonyl piperazine compounds useful as t cell activators
BR112022012222A2 (pt) 2019-12-23 2022-09-13 Bristol Myers Squibb Co Derivados de piperazina substituídos úteis como ativadores de células t
US12492172B2 (en) 2019-12-23 2025-12-09 Bristol-Myers Squibb Company Substituted quinazolinyl compounds useful as T cell activators
ES3013568T3 (en) 2019-12-23 2025-04-14 Bristol Myers Squibb Co Substituted heteroaryl compounds useful as t cell activators
AR120823A1 (es) 2019-12-23 2022-03-23 Bristol Myers Squibb Co Compuestos bicíclicos sustituidos útiles como activadores de células t
BR112022013424A2 (pt) 2020-01-06 2022-12-13 Hifibio Hk Ltd Anticorpo anti-tnfr2 e seus usos
CN111138425A (zh) * 2020-01-06 2020-05-12 中国药科大学 三氮唑类衍生物及其制备方法与用途
WO2021139682A1 (en) 2020-01-07 2021-07-15 Hifibio (Hk) Limited Anti-galectin-9 antibody and uses thereof
US11534441B2 (en) 2020-01-15 2022-12-27 Blueprint Medicines Corporation MAP4K1 inhibitors
JP2023516459A (ja) 2020-03-09 2023-04-19 ブリストル－マイヤーズ スクイブ カンパニー 増強されたアゴニスト活性を有するｃｄ４０に対する抗体
TW202140441A (zh) 2020-03-23 2021-11-01 美商必治妥美雅史谷比公司 經取代之側氧基異吲哚啉化合物
EP4132971A1 (en) 2020-04-09 2023-02-15 Merck Sharp & Dohme LLC Affinity matured anti-lap antibodies and uses thereof
US20230192867A1 (en) 2020-05-15 2023-06-22 Bristol-Myers Squibb Company Antibodies to garp
WO2021258010A1 (en) 2020-06-19 2021-12-23 Gossamer Bio Services, Inc. Oxime compounds useful as t cell activators
MX2023001707A (es) 2020-08-10 2023-05-04 Shanghai Xunbaihui Biotechnology Co Ltd Composiciones y métodos para el tratamiento de enfermedades autoinmunes y cánceres por direccionamiento al miembro 8 de la superfamilia de inmunoglobulinas.
EP4228764A1 (en) 2020-10-14 2023-08-23 Five Prime Therapeutics, Inc. Anti-c-c chemokine receptor 8 (ccr8) antibodies and methods of use thereof
CA3202330A1 (en) 2020-12-16 2022-06-23 Anthony Casarez Compounds useful as t cell activators
WO2022169921A1 (en) 2021-02-04 2022-08-11 Bristol-Myers Squibb Company Benzofuran compounds as sting agonists
JP2024506339A (ja) 2021-02-12 2024-02-13 エフ・ホフマン－ラ・ロシュ・アクチェンゲゼルシャフト がんの治療のための二環式テトラヒドロアゼピン誘導体
CN113105366B (zh) * 2021-03-04 2022-05-24 中国药科大学 一类含苯基羟肟结构衍生物及其制法与用途
JP2024510176A (ja) 2021-03-08 2024-03-06 ブループリント メディシンズ コーポレイション Ｍａｐ４ｋ１阻害剤
WO2022197641A1 (en) 2021-03-15 2022-09-22 Rapt Therapeutics, Inc. 1h-pyrazolo[3,4-d]pyrimidin-6-yl-amine derivatives as hematopoietic progenitor kinase 1 (hpk1) modulators and/or inhibitors for the treatment of cancer and other diseases
EP4314068A1 (en) 2021-04-02 2024-02-07 The Regents Of The University Of California Antibodies against cleaved cdcp1 and uses thereof
JP2024515545A (ja) 2021-04-05 2024-04-10 ブリストル－マイヤーズ スクイブ カンパニー がん治療のためのピリジニル置換オキソイソインドリン化合物
FI4320112T3 (fi) 2021-04-06 2025-07-25 Bristol Myers Squibb Co Pyridinyylisubstituoituja oksoisoindoliiniyhdisteitä
MX2024000751A (es) 2021-07-14 2024-03-25 Blueprint Medicines Corp Compuestos heterociclicos como inhibidores de map4k1.
WO2023288264A1 (en) 2021-07-15 2023-01-19 Blueprint Medicines Corporation Map4k1 inhibitors
WO2023122772A1 (en) 2021-12-22 2023-06-29 Gossamer Bio Services, Inc. Oxime derivatives useful as t cell activators
WO2023122778A1 (en) 2021-12-22 2023-06-29 Gossamer Bio Services, Inc. Pyridazinone derivatives useful as t cell activators
WO2023122777A1 (en) 2021-12-22 2023-06-29 Gossamer Bio Services, Inc. Oxime derivatives useful as t cell activators
EP4472963A1 (en) 2022-02-01 2024-12-11 Arvinas Operations, Inc. Dgk targeting compounds and uses thereof
KR20250046309A (ko) 2022-08-08 2025-04-02 브리스톨-마이어스 스큅 컴퍼니 T 세포 활성화제로서 유용한 치환된 테트라졸릴 화합물
JP2025528157A (ja) 2022-08-09 2025-08-26 ブリストル－マイヤーズ スクイブ カンパニー Ｔ細胞活性化剤として有用な第三アミン置換二環式化合物
PE20250876A1 (es) 2022-08-11 2025-03-28 Hoffmann La Roche Derivados biciclicos de tetrahidrotiazepina
CR20250042A (es) 2022-08-11 2025-03-25 Hoffmann La Roche Derivados de tetrahidrotiazepina bicíclicos
EP4568746A1 (en) 2022-08-11 2025-06-18 F. Hoffmann-La Roche AG Bicyclic tetrahydrothiazepine derivatives
EP4568960A1 (en) 2022-08-11 2025-06-18 F. Hoffmann-La Roche AG Bicyclic tetrahydroazepine derivatives
WO2024137865A1 (en) 2022-12-22 2024-06-27 Gossamer Bio Services, Inc. Compounds useful as t cell activators
WO2024233900A1 (en) 2023-05-10 2024-11-14 Blueprint Medicines Corporation Gsk3a inhibitors and methods of use thereof
CN121487946A (zh) 2023-06-07 2026-02-06 百时美施贵宝公司 螺环取代的氧代异吲哚啉基哌啶-2,6-二酮化合物
AU2024314878A1 (en) 2023-06-23 2026-01-22 Bristol-Myers Squibb Company Substituted oxoisoindolinyl piperidine-2,6-dione compound as anticancer agent
WO2025030002A2 (en) 2023-08-02 2025-02-06 Arvinas Operations, Inc. Dgk targeting compounds and uses thereof
WO2025064197A1 (en) 2023-09-02 2025-03-27 Bristol-Myers Squibb Company Substituted azetidinyl oxoisoindolinyl piperidine-2,6-dione compounds
WO2025096490A1 (en) 2023-10-31 2025-05-08 Bristol-Myers Squibb Company Ubiquitin specific processing protease 1 (usp1) compounds
WO2025096494A1 (en) 2023-10-31 2025-05-08 Bristol-Myers Squibb Company Ubiquitin specific processing protease 1 (usp1) compounds
WO2025096489A1 (en) 2023-10-31 2025-05-08 Bristol-Myers Squibb Company Ubiquitin specific processing protease 1 (usp1) compounds
WO2025096488A1 (en) 2023-10-31 2025-05-08 Bristol-Myers Squibb Company Ubiquitin specific processing protease 1 (usp1) compounds
WO2025096505A1 (en) 2023-10-31 2025-05-08 Bristol-Myers Squibb Company Ubiquitin specific processing protease 1 (usp1) compounds
WO2025096487A1 (en) 2023-10-31 2025-05-08 Bristol-Myers Squibb Company Ubiquitin specific processing protease 1 (usp1) compounds
TW202535865A (zh) 2023-10-31 2025-09-16 美商必治妥美雅史谷比公司 泛素特異性加工蛋白酶1 (usp1) 化合物
WO2025226767A1 (en) 2024-04-24 2025-10-30 Bristol-Myers Squibb Company Substituted 3-(5-(6-aminopyridin-2-yl)-4-fluoro-1-oxoisoindolin-2-yl)piperidine-2,6-dione compounds for use in the treatment of cancer
CN118908989B (zh) * 2024-10-10 2024-12-17 江苏长泰药业股份有限公司 一种用于预防肺结节恶性转化的丙酮酸盐衍生物纳米雾化剂及其制备方法

Family Cites Families (129)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3236855A (en) 1964-01-17 1966-02-22 Merck & Co Inc Certain n-phenyl(thiazole-hydroxamidine) compounds and their preparation
US3354174A (en) 1964-02-19 1967-11-21 Sterling Drug Inc 1-and 2-benzimidazolyl-lower-alkylamidoximes, amidines-, and guanidines
DE1453353A1 (de) 1964-02-20 1970-01-15 Nottmeyer Maschf Heinrich Maschine zum Einpressen von Duebeln in eine vorgebohrte Platte oder dergleichen Werkstueck
US3286855A (en) 1965-06-01 1966-11-22 Standard Trailer Company Crane extension and resulting crane assembly
US3553228A (en) * 1967-09-26 1971-01-05 Colgate Palmolive Co 3-substituted-4h(1)benzopyrano(3,4-d) isoxazoles
DE2040628A1 (de) 1970-08-17 1972-02-24 Fahlberg List Veb Neue herbizide Mittel
US3948928A (en) * 1972-03-17 1976-04-06 Dainippon Pharmaceutical Co., Ltd. 3-Substituted-1,2-benzisoxazoles and pharmaceutically acceptable acid addition salts thereof
JPS5621033B2 (me) 1973-09-05 1981-05-16
IE43624B1 (en) * 1975-09-11 1981-04-22 Philagro Sa New derivatives of amidoximes
FR2323683A1 (fr) 1975-09-11 1977-04-08 Philagro Sa Nouveaux derives d'amidoximes, leur preparation et les compositions qui les contiennent
US5179017A (en) 1980-02-25 1993-01-12 The Trustees Of Columbia University In The City Of New York Processes for inserting DNA into eucaryotic cells and for producing proteinaceous materials
US4634665A (en) 1980-02-25 1987-01-06 The Trustees Of Columbia University In The City Of New York Processes for inserting DNA into eucaryotic cells and for producing proteinaceous materials
US4399216A (en) 1980-02-25 1983-08-16 The Trustees Of Columbia University Processes for inserting DNA into eucaryotic cells and for producing proteinaceous materials
US4323681A (en) * 1980-09-29 1982-04-06 American Home Products Corporation 4-Amino-2-substituted-5-pyrimidinecarboxamidoximes and carbothioamides
US5156840A (en) 1982-03-09 1992-10-20 Cytogen Corporation Amine-containing porphyrin derivatives
JPS58208275A (ja) 1982-05-20 1983-12-03 Lion Corp ５−アミノ−ピラゾ−ル誘導体及び該化合物を含有する抗腫瘍剤
ATE25250T1 (de) 1983-07-22 1987-02-15 Bayer Ag Substituierte furazane.
US4507485A (en) 1984-01-23 1985-03-26 Bristol-Myers Company 3,4-Disubstituted-1,2,5-oxadiazoles having histamine H2 -receptor antagonist activity
JPS60193968A (ja) 1984-03-13 1985-10-02 Toyo Jozo Co Ltd シクロペンテン環を有するイミダゾ−ルアミドオキシムおよびその製造法
JPS6259283A (ja) 1985-09-10 1987-03-14 Kaken Pharmaceut Co Ltd セフアロスポリン化合物
US5057313A (en) 1986-02-25 1991-10-15 The Center For Molecular Medicine And Immunology Diagnostic and therapeutic antibody conjugates
EP0307434B2 (en) 1987-03-18 1998-07-29 Scotgen Biopharmaceuticals, Inc. Altered antibodies
JP2696342B2 (ja) 1988-06-27 1998-01-14 日本曹達株式会社 アミジン誘導体、その製造方法及び殺ダニ剤・農園芸用殺菌剤
ES2051986T3 (es) 1988-07-05 1994-07-01 Akzo Nv Compuestos con actividad broncodilatadora.
US5530101A (en) 1988-12-28 1996-06-25 Protein Design Labs, Inc. Humanized immunoglobulins
IL162181A (en) 1988-12-28 2006-04-10 Pdl Biopharma Inc A method of producing humanized immunoglubulin, and polynucleotides encoding the same
DE3920358A1 (de) 1989-06-22 1991-01-17 Behringwerke Ag Bispezifische und oligospezifische, mono- und oligovalente antikoerperkonstrukte, ihre herstellung und verwendung
US5859205A (en) 1989-12-21 1999-01-12 Celltech Limited Humanised antibodies
JPH0420710A (ja) 1990-05-12 1992-01-24 Hitachi Home Tec Ltd ポットバーナの運転制御装置
JPH04297449A (ja) 1991-03-27 1992-10-21 Hokko Chem Ind Co Ltd Ｎ−ヒドロキシベンジルグアニジン誘導体および農園芸用殺菌剤
JPH05186458A (ja) 1991-04-26 1993-07-27 Japan Tobacco Inc 新規なベンゾピラン誘導体
FR2677019B1 (fr) * 1991-05-27 1994-11-25 Pf Medicament Nouvelles piperidines disubstituees-1,4, leur preparation et leur application en therapeutique.
DE69233254T2 (de) 1991-06-14 2004-09-16 Genentech, Inc., South San Francisco Humanisierter Heregulin Antikörper
WO1993011161A1 (en) 1991-11-25 1993-06-10 Enzon, Inc. Multivalent antigen-binding proteins
US5714350A (en) 1992-03-09 1998-02-03 Protein Design Labs, Inc. Increasing antibody affinity by altering glycosylation in the immunoglobulin variable region
US5521184A (en) 1992-04-03 1996-05-28 Ciba-Geigy Corporation Pyrimidine derivatives and processes for the preparation thereof
JP2709677B2 (ja) * 1992-06-19 1998-02-04 株式会社大塚製薬工場 ホスホン酸ジエステル誘導体
US5827690A (en) 1993-12-20 1998-10-27 Genzyme Transgenics Corporatiion Transgenic production of antibodies in milk
FR2720396B1 (fr) * 1994-05-27 1996-06-28 Adir Nouveaux N-pyridyl carboxamides et dérivés leur procédé de préparation et les compositions pharmaceutiques qui les contiennent.
US5731168A (en) 1995-03-01 1998-03-24 Genentech, Inc. Method for making heteromultimeric polypeptides
US5869046A (en) 1995-04-14 1999-02-09 Genentech, Inc. Altered polypeptides with increased half-life
US5731315A (en) 1995-06-07 1998-03-24 Rhone-Poulenc Rorer Pharmaceuticals Inc. Substituted sulfonic acid n- (aminoiminomethyl)phenylalkyl!-azaheterocyclamide compounds
AU725609C (en) 1995-08-18 2002-01-03 Morphosys Ag Protein/(poly)peptide libraries
BR9610988A (pt) 1995-10-17 1999-04-06 Astra Pharma Prod Composto uso do mesmo fomulação farmacêutica e processo para produção do composto
WO1997030047A1 (en) * 1996-02-17 1997-08-21 Agrevo Uk Limited Fungicidal 1,2,4-oxadiazoles and analogues
US5955495A (en) 1996-05-03 1999-09-21 Hoffmann-La Roche Inc. Method of treating diseases of the CNS
JPH11171702A (ja) 1997-09-24 1999-06-29 Takeda Chem Ind Ltd 害虫防除方法
WO1999029310A2 (en) 1997-12-05 1999-06-17 Medical College Of Georgia Research Institute, Inc. Regulation of t cell-mediated immunity by tryptophan and its analogs
BR9813536A (pt) 1997-12-10 2000-10-10 Dainippon Ink & Chemicals "derivados oxima e produtos quìmicos agrìcolas incluindo os mesmos"
AU3957399A (en) 1998-06-02 1999-12-20 Takeda Chemical Industries Ltd. Oxadiazoline derivatives and their use as insecticides
CA2339961C (en) 1998-08-11 2009-01-20 Novartis Ag Isoquinoline derivatives with angiogenesis inhibiting activity
FR2784678B1 (fr) 1998-09-23 2002-11-29 Sod Conseils Rech Applic Nouveaux derives de n-(iminomethyl)amines, leur preparation, leur application a titre de medicaments et les compositions pharmaceutiques les contenant
US6133031A (en) 1999-08-19 2000-10-17 Isis Pharmaceuticals Inc. Antisense inhibition of focal adhesion kinase expression
AU763030B2 (en) 1999-03-03 2003-07-10 Samjin Pharmaceutical Co., Ltd. Piperazine derivatives and process for the preparation thereof
GB9905075D0 (en) 1999-03-06 1999-04-28 Zeneca Ltd Chemical compounds
IL145772A0 (en) 1999-04-09 2002-07-25 Basf Ag Prodrugs of thrombin inhibitors
DK1188747T3 (da) 1999-05-24 2006-01-23 Mitsubishi Pharma Corp Phenoxypropylaminforbindelser
JP2001158785A (ja) 1999-11-30 2001-06-12 Takeda Chem Ind Ltd 農薬組成物
JP2001158786A (ja) 1999-11-30 2001-06-12 Takeda Chem Ind Ltd 哺乳動物の外部寄生虫防除剤
WO2001051456A2 (en) 2000-01-13 2001-07-19 Tularik Inc. Antibacterial agents
JP2001233861A (ja) 2000-02-22 2001-08-28 Ube Ind Ltd ピラゾールオキシム化合物、その製法及び用途
GB0004890D0 (en) 2000-03-01 2000-04-19 Astrazeneca Uk Ltd Chemical compounds
AU2002215608B2 (en) 2000-06-28 2004-12-09 Smithkline Beecham P.L.C. Wet milling process
GB0108102D0 (en) 2001-03-30 2001-05-23 Pfizer Ltd Compounds
HRP20031017A2 (en) 2001-06-18 2004-04-30 Applied Research Systems Pyrrolidine oxasidiazole- and thiadiazole derivatives
CA2466243A1 (en) 2001-09-19 2003-03-27 Aventis Pharma S.A. Indolizines as kinase protein inhibitors
EP1438059A4 (en) * 2001-10-26 2008-01-23 Angiolab Inc COMPOSITION CONTAINING EXTRACT OF BROWN FROM INDIA PREPARED FOR ANTI-ANGIOGENIC ACTIVITY AND INHIBITOR OF MATRIX METALLOPROTEINASE
PL211461B1 (pl) 2001-10-30 2012-05-31 Dana Farber Cancer Inst Inc Zastosowanie pochodnych staurosporyny do wytwarzania kompozycji farmaceutycznej do leczenia lub zapobiegania białaczkom i zespołom mielodysplastycznym, preparat farmaceutyczny do leczenia białaczek i zestaw farmaceutyczny
PL220952B1 (pl) 2002-01-22 2016-01-29 Warner Lambert Co 2-(Pirydyn-2-yloamino)pirydo[2,3-d]pirymidyn-7-ony
CA2476822A1 (en) 2002-02-19 2003-08-28 Pharmacia Italia S.P.A. Tricyclic pyrazole derivatives, process for their preparation and their use as antitumor agents
GB0208224D0 (en) 2002-04-10 2002-05-22 Celltech R&D Ltd Chemical compounds
EP1501918A4 (en) 2002-04-12 2006-03-29 Med College Georgia Res Inst ANTIGEN PRESENTING CELL POPULATIONS AND THEIR USE AS REAGENTS TO INCREASE OR REDUCE IMMUNO TOLERANCE
US7109354B2 (en) 2002-05-28 2006-09-19 3-Dimensional Pharmaceuticals, Inc. Thiophene amidines, compositions thereof, and methods of treating complement-mediated diseases and conditions
TW200406374A (en) 2002-05-29 2004-05-01 Novartis Ag Diaryl urea derivatives useful for the treatment of protein kinase dependent diseases
JP4020710B2 (ja) 2002-06-25 2007-12-12 株式会社ミツバ ドアミラーセットプレート
GB0215676D0 (en) 2002-07-05 2002-08-14 Novartis Ag Organic compounds
US7157462B2 (en) 2002-09-24 2007-01-02 Euro-Celtique S.A. Therapeutic agents useful for treating pain
US7015321B2 (en) 2002-10-12 2006-03-21 The Scripps Research Institute Synthesis of non-symmetrical sulfamides using burgess-type reagents
AR042052A1 (es) 2002-11-15 2005-06-08 Vertex Pharma Diaminotriazoles utiles como inhibidores de proteinquinasas
UA80767C2 (en) 2002-12-20 2007-10-25 Pfizer Prod Inc Pyrimidine derivatives for the treatment of abnormal cell growth
US7355008B2 (en) 2003-01-09 2008-04-08 Macrogenics, Inc. Identification and engineering of antibodies with variant Fc regions and methods of using same
WO2004065416A2 (en) 2003-01-16 2004-08-05 Genentech, Inc. Synthetic antibody phage libraries
US20050008625A1 (en) 2003-02-13 2005-01-13 Kalobios, Inc. Antibody affinity engineering by serial epitope-guided complementarity replacement
GB0305929D0 (en) 2003-03-14 2003-04-23 Novartis Ag Organic compounds
EP1613308A4 (en) 2003-03-27 2008-02-20 Lankenau Inst Medical Res NEW METHODS OF TREATING CANCER
US7598287B2 (en) 2003-04-01 2009-10-06 Medical College Of Georgia Research Institute, Inc. Use of inhibitors of indoleamine-2,3-dioxygenase in combination with other therapeutic modalities
CA2528551A1 (en) 2003-06-13 2005-01-13 Biogen Idec Ma Inc. Aglycosyl anti-cd154 (cd40 ligand) antibodies and uses thereof
JP2007512230A (ja) 2003-08-20 2007-05-17 バーテックス　ファーマシューティカルズ　インコーポレイテッド プロテインキナーゼ阻害剤として有用な（４−アミノ−１，２，５−オキサジアゾール−４−イル）−ヘテロ芳香族化合物
EP2502935B1 (en) 2003-08-22 2017-03-29 Biogen MA Inc. Improved antibodies having altered effector function and methods for making the same
PE20050952A1 (es) 2003-09-24 2005-12-19 Novartis Ag Derivados de isoquinolina como inhibidores de b-raf
DE10348022A1 (de) 2003-10-15 2005-05-25 Imtm Gmbh Neue Dipeptidylpeptidase IV-Inhibitoren zur funktionellen Beeinflussung unterschiedlicher Zellen und zur Behandlung immunologischer, entzündlicher, neuronaler und anderer Erkrankungen
DE10348023A1 (de) * 2003-10-15 2005-05-19 Imtm Gmbh Neue Alanyl-Aminopeptidasen-Inhibitoren zur funktionellen Beeinflussung unterschiedlicher Zellen und zur Behandlung immunologischer, entzündlicher, neuronaler und anderer Erkrankungen
CA2567662C (en) 2004-06-10 2012-11-27 Irm Llc Compounds and compositions as protein kinase inhibitors
EP1801108B9 (en) 2004-09-08 2013-11-20 Mitsubishi Tanabe Pharma Corporation Morpholine compounds for the treatment of inflammations
BRPI0517887A (pt) 2004-11-24 2008-10-21 Novartis Ag combinações de inibidores de jaks
WO2006067532A1 (en) 2004-12-24 2006-06-29 Prosidion Ltd G-protein coupled receptor agonists
US7429667B2 (en) * 2005-01-20 2008-09-30 Ardea Biosciences, Inc. Phenylamino isothiazole carboxamidines as MEK inhibitors
MX2007013978A (es) 2005-05-09 2008-02-22 Ono Pharmaceutical Co Anticuerpos monoclonales humanos a muerte programada 1 (pd-1) y metodos para tratamiento de cancer utilizando anticuerpos anti-pd-1 solos o en combinacion con otros inmunoterapeuticos.
RS54876B1 (sr) 2005-05-10 2016-10-31 Incyte Holdings Corp Modulatori indoleamina 2,3-dioksigenaze i metode za upotrebu istih
WO2006133417A1 (en) 2005-06-07 2006-12-14 Valeant Pharmaceuticals International Phenylamino isothiazole carboxamidines as mek inhibitors
JP2008544818A (ja) 2005-06-30 2008-12-11 アントフロゲネシス コーポレーション 胎盤由来コラーゲンバイオ線維を用いた鼓膜の修復
DE102005060466A1 (de) * 2005-12-17 2007-06-28 Bayer Cropscience Ag Carboxamide
ES2540561T3 (es) 2005-12-20 2015-07-10 Incyte Corporation N-hidroxiamidinoheterociclos como moduladores de indolamina 2,3-dioxigenasa
WO2007095050A2 (en) * 2006-02-09 2007-08-23 Incyte Corporation N-hydroxyguanidines as modulators of indoleamine 2,3-dioxygenase
JP4297449B2 (ja) 2006-05-12 2009-07-15 株式会社サクラクレパス 墨汁
CL2007002650A1 (es) 2006-09-19 2008-02-08 Incyte Corp Compuestos derivados de heterociclo n-hidroxiamino; composicion farmaceutica, util para tratar cancer, infecciones virales y desordenes neurodegenerativos entre otras.
JP5319532B2 (ja) 2006-09-19 2013-10-16 インサイト・コーポレイション インドールアミン２，３−ジオキシゲナーゼのモジュレーターとしてのｎ−ヒドロキシアミジノヘテロサイクル
WO2008036652A2 (en) 2006-09-19 2008-03-27 Incyte Corporation Amidines as modulators of indoleamine 2,3-dioxygenase
US20080119491A1 (en) * 2006-09-19 2008-05-22 Incyte Corporation Amidinoheterocycles as modulators of indoleamine 2,3-dioxygenase
US20080182882A1 (en) * 2006-11-08 2008-07-31 Incyte Corporation N-hydroxyamidinoheterocycles as modulators of indoleamine 2,3-dioxygenase
EP2121621B1 (en) 2006-12-08 2014-05-07 Exelixis Patent Company LLC Lxr and fxr modulators
CL2008000066A1 (es) * 2007-01-12 2008-08-01 Smithkline Beecham Corp Compuestos derivados de (5-hidroxi-3-oxo-2,3-dihidropiridazina-4-carbonil)glicina, inhibidores de hif prolil hidroxilasas; procedimiento de preparacion; composicion farmaceutica que comprende a dichos compuestos; y su uso en el tratamiento de la anem
NZ586069A (en) 2007-12-19 2012-05-25 Amgen Inc Fused pyridine, pyrimidine and triazine compounds as cell cycle inhibitors
CA2709784A1 (en) * 2007-12-21 2009-07-09 University Of Rochester Method for altering the lifespan of eukaryotic organisms
SMT201800206T1 (it) 2008-07-08 2018-05-02 Incyte Holdings Corp 1,2,5-ossadiazoli come inibitori di indoleamina 2,3-diossigenasi
PA8852901A1 (es) 2008-12-22 2010-07-27 Lilly Co Eli Inhibidores de proteina cinasa
UY33227A (es) 2010-02-19 2011-09-30 Novartis Ag Compuestos de pirrolopirimidina como inhibidores de la cdk4/6
CN106967074A (zh) 2010-10-25 2017-07-21 G1治疗公司 Cdk抑制剂
ES2620521T3 (es) 2011-03-23 2017-06-28 Amgen Inc. Inhibidores duales tricíclicos condensados de CDK 4/6 y FLT3
EP2911669B1 (en) 2012-10-26 2024-04-10 The University of Chicago Synergistic combination of immunologic inhibitors for the treatment of cancer
WO2015005468A1 (ja) 2013-07-12 2015-01-15 日本ケミファ株式会社 Ｐ２ｘ４受容体拮抗剤
KR102370067B1 (ko) 2013-11-08 2022-03-04 인사이트 홀딩스 코포레이션 인돌아민 2,3-디옥시게나제 억제제의 합성 방법
EP3102237B1 (en) 2014-02-04 2020-12-02 Incyte Corporation Combination of a pd-1 antagonist and an ido1 inhibitor for treating cancer
AU2015327868A1 (en) 2014-10-03 2017-04-20 Novartis Ag Combination therapies
GEAP202215554A (en) 2015-07-30 2022-06-10 Macrogenics Inc Pd-1-binding molecules and methods of use thereof
JP6955648B2 (ja) 2015-09-01 2021-10-27 ファースト ウェーブ バイオ インコーポレイテッド 異常炎症反応に関連する状態を処置するための方法および組成物
JP2018532756A (ja) 2015-11-04 2018-11-08 インサイト・コーポレイションＩｎｃｙｔｅ Ｃｏｒｐｏｒａｔｉｏｎ インドールアミン２，３−ジオキシゲナーゼを阻害するための医薬組成物と方法、及びその適応
JP2022543062A (ja) 2019-08-01 2022-10-07 インサイト・コーポレイション Ｉｄｏ阻害剤の投与レジメン
WO2021222257A1 (en) 2020-04-27 2021-11-04 Armata Pharmaceuticals, Inc. Bacteriophage compositions for treating pseudomonas infection

Also Published As

Publication number Publication date
CN103130735B (zh) 2016-08-03
EP1879573A4 (en) 2009-07-08
DK1879573T3 (da) 2013-02-25
CN103130735A (zh) 2013-06-05
EP1879573B1 (en) 2012-12-19
NZ562919A (en) 2011-04-29
EA200702455A1 (ru) 2008-04-28
JP5615308B2 (ja) 2014-10-29
SG195607A1 (en) 2013-12-30
KR101562549B1 (ko) 2015-10-23
US20110311479A1 (en) 2011-12-22
ES2578404T3 (es) 2016-07-26
EP2559690A1 (en) 2013-02-20
PL1879573T3 (pl) 2013-05-31
BR122020016659B8 (pt) 2021-07-27
US10208002B2 (en) 2019-02-19
PT1879573E (pt) 2013-03-25
AR054271A1 (es) 2007-06-13
US20180030006A1 (en) 2018-02-01
HRP20130220T1 (hr) 2013-04-30
CN101212967A (zh) 2008-07-02
BR122020016659B1 (pt) 2021-03-16
KR101386494B1 (ko) 2014-04-24
US8372870B2 (en) 2013-02-12
JP2008540548A (ja) 2008-11-20
US20190210985A1 (en) 2019-07-11
IL186957A (en) 2014-04-30
WO2006122150A1 (en) 2006-11-16
US20130123246A1 (en) 2013-05-16
ES2401482T3 (es) 2013-04-22
CY1113989T1 (el) 2016-07-27
CA2606783C (en) 2014-03-25
ZA200709698B (en) 2008-11-26
SI2559690T1 (sl) 2016-06-30
TW200719892A (en) 2007-06-01
US20140377292A1 (en) 2014-12-25
RS54876B1 (sr) 2016-10-31
AU2006244068B9 (en) 2012-10-25
BRPI0608604A2 (pt) 2010-01-26
US8034953B2 (en) 2011-10-11
NO342140B1 (no) 2018-03-26
IL232313A0 (en) 2014-06-30
HK1117392A1 (en) 2009-01-16
DK2559690T3 (en) 2016-04-25
CR9485A (es) 2008-02-20
CA2606783A1 (en) 2006-11-16
MX2007013977A (es) 2008-02-05
BRPI0608604B1 (pt) 2020-11-17
RS52711B (sr) 2013-08-30
PT2559690T (pt) 2016-07-07
BRPI0608604B8 (pt) 2021-05-25
GEP20217221B (en) 2021-02-10
JP2012140450A (ja) 2012-07-26
EP1879573A1 (en) 2008-01-23
IL232313A (en) 2016-05-31
SG161310A1 (en) 2010-05-27
EA026785B1 (ru) 2017-05-31
SI1879573T1 (sl) 2013-04-30
EP2559690B1 (en) 2016-03-30
JP4990270B2 (ja) 2012-08-01
CY1117681T1 (el) 2017-05-17
AU2006244068B2 (en) 2012-06-14
TWI377060B (en) 2012-11-21
NO20075693L (no) 2008-02-07
HK1182381A1 (en) 2013-11-29
AU2006244068A1 (en) 2006-11-16
MY153424A (en) 2015-02-13
US11192868B2 (en) 2021-12-07
US20060258719A1 (en) 2006-11-16
KR20130109263A (ko) 2013-10-07
US8846726B2 (en) 2014-09-30
PL2559690T3 (pl) 2016-09-30
NO340487B1 (no) 2017-05-02
HUE029214T2 (en) 2017-02-28
EP3085697A1 (en) 2016-10-26
KR20080005954A (ko) 2008-01-15
SG10201809390QA (en) 2018-11-29
UA99897C2 (en) 2012-10-25
IL186957A0 (en) 2008-02-09
HRP20160537T1 (hr) 2016-06-17
NO20170633A1 (no) 2008-02-07

Similar Documents

Publication Publication Date Title
ME02461B (me) Modulatori indoleamina 2,3-dioksigenaze i metode za upotrebu istih
JP2010504342A5 (me)
RU2461551C2 (ru) Азолкарбоксамидное соединение или его фармацевтически приемлемая соль
RU2006101053A (ru) Производные бензамида или соль указанного производного
JP2015517981A5 (me)
JP2007519754A5 (me)
HRP20150442T1 (hr) Sredstva za izazivanje apoptoze za lijeäśenje raka i imunih i autoimunih bolesti
JP2010501587A5 (me)
RU2008119412A (ru) N-фенил-фенилацетамидные ненуклеозидные ингибиторы обратной транскриптазы
JP2005521639A5 (me)
HRP20161085T1 (hr) Sulfonamid derivati kao bcl-2 selektivni agensi za induciranje apoptoze namijenjeni liječenju raka i imunih bolesti
RU2007107189A (ru) Производные арилпиридина
ZA200502755B (en) 1,3-Diamino-2-hydroxypropane prodrug derivatives.
JP2002532415A5 (ja) Ｍｅｋ阻害剤を含有する関節炎の治療用医薬組成物
RU2004100839A (ru) Производные пиперидина полезные в качестве модуляторов активности рецепторов хемокинов
RU2009116670A (ru) Производные 3-пиридинкарбоксамида и 2-пиразинкарбоксамида в качестве агентов, повышающих уровень лвп-холестерина
RU2007119427A (ru) Соединения, являющиеся ингибиторами гликогенфосфорилазы, и фармацевтические композиции на их основе
RU2004126936A (ru) Производные хинолина в качестве антагонистов npv
RU2012129737A (ru) Замещенные бензамидные производные
RU2009118254A (ru) Фенилацетамиды в качестве ингибиторов протеинкиназ
JP2007519619A5 (me)
JP2010506918A5 (me)
NZ603724A (en) Piperidine derivatives and their use for the treatment of metabolic disorders
JP2011529037A5 (me)
RU2006101541A (ru) Производные пиперазина и способ их применения