ME02794B - Metilen vezani hinolinil modulatori ror-gama-t - Google Patents
Metilen vezani hinolinil modulatori ror-gama-tInfo
- Publication number
- ME02794B ME02794B MEP-2017-151A MEP2017151A ME02794B ME 02794 B ME02794 B ME 02794B ME P2017151 A MEP2017151 A ME P2017151A ME 02794 B ME02794 B ME 02794B
- Authority
- ME
- Montenegro
- Prior art keywords
- alkyl
- pyridyl
- optionally substituted
- imidazolyl
- group
- Prior art date
Links
- 125000000217 alkyl group Chemical group 0.000 claims 129
- -1 pyridyl N-oxide Chemical group 0.000 claims 87
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 39
- 125000004093 cyano group Chemical group *C#N 0.000 claims 38
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 36
- 125000004076 pyridyl group Chemical group 0.000 claims 36
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims 30
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 28
- 125000002883 imidazolyl group Chemical group 0.000 claims 25
- 125000002971 oxazolyl group Chemical group 0.000 claims 22
- 101100054666 Streptomyces halstedii sch3 gene Proteins 0.000 claims 21
- 125000003226 pyrazolyl group Chemical group 0.000 claims 21
- 125000000335 thiazolyl group Chemical group 0.000 claims 21
- 125000000714 pyrimidinyl group Chemical group 0.000 claims 20
- 125000001424 substituent group Chemical group 0.000 claims 19
- 125000001425 triazolyl group Chemical group 0.000 claims 18
- 229910006074 SO2NH2 Inorganic materials 0.000 claims 16
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 claims 16
- 150000001875 compounds Chemical class 0.000 claims 16
- 125000000842 isoxazolyl group Chemical group 0.000 claims 16
- 125000003373 pyrazinyl group Chemical group 0.000 claims 16
- 125000000565 sulfonamide group Chemical group 0.000 claims 16
- 125000001544 thienyl group Chemical group 0.000 claims 13
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 12
- 125000003386 piperidinyl group Chemical group 0.000 claims 12
- 150000003839 salts Chemical class 0.000 claims 9
- 125000004541 benzoxazolyl group Chemical group O1C(=NC2=C1C=CC=C2)* 0.000 claims 8
- 125000000876 trifluoromethoxy group Chemical group FC(F)(F)O* 0.000 claims 8
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 7
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 7
- 125000005495 pyridazyl group Chemical class 0.000 claims 7
- 125000002147 dimethylamino group Chemical group [H]C([H])([H])N(*)C([H])([H])[H] 0.000 claims 6
- 229910052757 nitrogen Inorganic materials 0.000 claims 6
- 125000000168 pyrrolyl group Chemical group 0.000 claims 6
- 125000004206 2,2,2-trifluoroethyl group Chemical group [H]C([H])(*)C(F)(F)F 0.000 claims 5
- 125000004196 benzothienyl group Chemical group S1C(=CC2=C1C=CC=C2)* 0.000 claims 5
- 201000010099 disease Diseases 0.000 claims 5
- 125000002541 furyl group Chemical group 0.000 claims 5
- CBOIHMRHGLHBPB-UHFFFAOYSA-N hydroxymethyl Chemical compound O[CH2] CBOIHMRHGLHBPB-UHFFFAOYSA-N 0.000 claims 5
- 125000002943 quinolinyl group Chemical group N1=C(C=CC2=CC=CC=C12)* 0.000 claims 5
- 125000001412 tetrahydropyranyl group Chemical group 0.000 claims 5
- JNCMHMUGTWEVOZ-UHFFFAOYSA-N F[CH]F Chemical compound F[CH]F JNCMHMUGTWEVOZ-UHFFFAOYSA-N 0.000 claims 4
- 108010081348 HRT1 protein Hairy Proteins 0.000 claims 4
- 102100021881 Hairy/enhancer-of-split related with YRPW motif protein 1 Human genes 0.000 claims 4
- 125000002777 acetyl group Chemical group [H]C([H])([H])C(*)=O 0.000 claims 4
- 125000000753 cycloalkyl group Chemical group 0.000 claims 4
- 125000004786 difluoromethoxy group Chemical group [H]C(F)(F)O* 0.000 claims 4
- 125000001715 oxadiazolyl group Chemical group 0.000 claims 4
- 125000003831 tetrazolyl group Chemical group 0.000 claims 4
- 125000001113 thiadiazolyl group Chemical group 0.000 claims 4
- 125000004496 thiazol-5-yl group Chemical group S1C=NC=C1* 0.000 claims 4
- 125000003626 1,2,4-triazol-1-yl group Chemical group [*]N1N=C([H])N=C1[H] 0.000 claims 3
- 125000003349 3-pyridyl group Chemical group N1=C([H])C([*])=C([H])C([H])=C1[H] 0.000 claims 3
- 201000004681 Psoriasis Diseases 0.000 claims 3
- 239000003937 drug carrier Substances 0.000 claims 3
- 239000008194 pharmaceutical composition Substances 0.000 claims 3
- 125000004353 pyrazol-1-yl group Chemical group [H]C1=NN(*)C([H])=C1[H] 0.000 claims 3
- 206010039073 rheumatoid arthritis Diseases 0.000 claims 3
- 125000004793 2,2,2-trifluoroethoxy group Chemical group FC(CO*)(F)F 0.000 claims 2
- RZVAJINKPMORJF-UHFFFAOYSA-N Acetaminophen Chemical class CC(=O)NC1=CC=C(O)C=C1 RZVAJINKPMORJF-UHFFFAOYSA-N 0.000 claims 2
- 208000006673 asthma Diseases 0.000 claims 2
- 125000003785 benzimidazolyl group Chemical group N1=C(NC2=C1C=CC=C2)* 0.000 claims 2
- 125000001164 benzothiazolyl group Chemical group S1C(=NC2=C1C=CC=C2)* 0.000 claims 2
- 208000035475 disorder Diseases 0.000 claims 2
- 125000003453 indazolyl group Chemical group N1N=C(C2=C1C=CC=C2)* 0.000 claims 2
- 125000001041 indolyl group Chemical group 0.000 claims 2
- 230000001404 mediated effect Effects 0.000 claims 2
- OKKJLVBELUTLKV-UHFFFAOYSA-N methanol Natural products OC OKKJLVBELUTLKV-UHFFFAOYSA-N 0.000 claims 2
- 125000004528 pyrimidin-5-yl group Chemical group N1=CN=CC(=C1)* 0.000 claims 2
- 208000011580 syndromic disease Diseases 0.000 claims 2
- 125000001889 triflyl group Chemical group FC(F)(F)S(*)(=O)=O 0.000 claims 2
- 125000004200 2-methoxyethyl group Chemical group [H]C([H])([H])OC([H])([H])C([H])([H])* 0.000 claims 1
- 125000000175 2-thienyl group Chemical group S1C([*])=C([H])C([H])=C1[H] 0.000 claims 1
- 206010002556 Ankylosing Spondylitis Diseases 0.000 claims 1
- XGVZUUCROYNYPA-UHFFFAOYSA-N C1CN(C)CCN1C1=NC2=CC=C(C(O)(C=3N(C=NC=3)C)C=3C=NC(=CC=3)C(F)(F)F)C=C2C(Cl)=C1CC1=CC=C(N2N=CC=C2)C=C1 Chemical compound C1CN(C)CCN1C1=NC2=CC=C(C(O)(C=3N(C=NC=3)C)C=3C=NC(=CC=3)C(F)(F)F)C=C2C(Cl)=C1CC1=CC=C(N2N=CC=C2)C=C1 XGVZUUCROYNYPA-UHFFFAOYSA-N 0.000 claims 1
- BKVZCSCWPPMUFQ-UHFFFAOYSA-N CC(=O)NCCOC1=NC2=CC=C(C(O)(C=3N(C=NC=3)C)C=3C=CC(Cl)=CC=3)C=C2C(O)=C1CC(C=C1)=CC=C1N1C=CC=N1 Chemical compound CC(=O)NCCOC1=NC2=CC=C(C(O)(C=3N(C=NC=3)C)C=3C=CC(Cl)=CC=3)C=C2C(O)=C1CC(C=C1)=CC=C1N1C=CC=N1 BKVZCSCWPPMUFQ-UHFFFAOYSA-N 0.000 claims 1
- 206010009900 Colitis ulcerative Diseases 0.000 claims 1
- 208000011231 Crohn disease Diseases 0.000 claims 1
- 208000019693 Lung disease Diseases 0.000 claims 1
- 201000001263 Psoriatic Arthritis Diseases 0.000 claims 1
- 208000036824 Psoriatic arthropathy Diseases 0.000 claims 1
- 108091008778 RORγ2 Proteins 0.000 claims 1
- 201000006704 Ulcerative Colitis Diseases 0.000 claims 1
- 229940121363 anti-inflammatory agent Drugs 0.000 claims 1
- 239000002260 anti-inflammatory agent Substances 0.000 claims 1
- 125000004567 azetidin-3-yl group Chemical group N1CC(C1)* 0.000 claims 1
- 230000001684 chronic effect Effects 0.000 claims 1
- 238000002648 combination therapy Methods 0.000 claims 1
- 229940079593 drug Drugs 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 1
- 125000004005 formimidoyl group Chemical group [H]\N=C(/[H])* 0.000 claims 1
- 125000002962 imidazol-1-yl group Chemical group [*]N1C([H])=NC([H])=C1[H] 0.000 claims 1
- 125000003037 imidazol-2-yl group Chemical group [H]N1C([*])=NC([H])=C1[H] 0.000 claims 1
- 229940125721 immunosuppressive agent Drugs 0.000 claims 1
- 239000003018 immunosuppressive agent Substances 0.000 claims 1
- 230000002757 inflammatory effect Effects 0.000 claims 1
- 238000000034 method Methods 0.000 claims 1
- 239000000203 mixture Substances 0.000 claims 1
- 201000006417 multiple sclerosis Diseases 0.000 claims 1
- 210000000440 neutrophil Anatomy 0.000 claims 1
- 230000000414 obstructive effect Effects 0.000 claims 1
- 125000004307 pyrazin-2-yl group Chemical group [H]C1=C([H])N=C(*)C([H])=N1 0.000 claims 1
- 125000004550 quinolin-6-yl group Chemical group N1=CC=CC2=CC(=CC=C12)* 0.000 claims 1
- 201000000596 systemic lupus erythematosus Diseases 0.000 claims 1
- 125000003718 tetrahydrofuranyl group Chemical group 0.000 claims 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/47—Quinolines; Isoquinolines
- A61K31/4709—Non-condensed quinolines and containing further heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- 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
-
- 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
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- 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
- A61P17/06—Antipsoriatics
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- 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
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- 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
- A61P37/00—Drugs for immunological or allergic disorders
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- 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
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
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- 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
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- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
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- 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
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- Pulmonology (AREA)
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- Pain & Pain Management (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Physical Education & Sports Medicine (AREA)
- Dermatology (AREA)
- Biomedical Technology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Steroid Compounds (AREA)
Claims (17)
1. Jedinjenje formule I pri čemu: R1 je pirolil, pirazolil, imidazolil, triazolil, tiazolil, piridil, piridil N-oksid, pirazinil, pirimidinil, piridazil, piperidinil, hinazolinil, cinolinil, benzotiazolil, indazolil, tetrahidropiranil, tetrahidrofuranil, furanil, fenil, oksazolil, izoksazolil, tiofenil, benzoksazolil, benzimidazolil, indolil, tiadiazolil, oksadiazolil ili hinolinil; pri čemu su pomenuti piridil, piridil N-oksid, pirazinil, pirimidinil, piridazil, piperidinil, hinazolinil, cinolinil, benzotiazolil, indazolil, imidazolil, fenil, tiofenil, benzoksazolil, benzimidazolil, indolil, hinolinil, i pirazolil po potrebi supstituisani sa C(O)C(1-4)alkil, C(O)NH2, C(O)NHC(1-2)alkil, C(O)N(C(1-2)alkil)2, NHC(O)C(1-4)alkil, NHSO2C(1-4)alkil, C(1-4)alkil, CF3, CH2CF3, Cl, F, -CN, OC(1-4)alkil, N(C(1-4)alkil)2, -(CH2)3OCH3, SC(1-4)alkil, OH, CO2H, CO2C(1-4)alkil, C(O)CF3, SO2CF3, OCF3, OCHF2, SO2CH3, SO2NH2, SO2NHC(1-2)alkil, SO2N(C(1-2)alkil)2, C(O)NHSO2CH3, ili OCH2OCH3; i po potrebi supstituisani sa do dva dodatna supstituenta koji su nezavisno odabrani iz grupe koja se sastoji iz Cl, C(1-2)alkil, SCH3, OC(1-2)alkil, CF3, -CN, i F; i pri čemu su pomenuti triazolil, oksazolil, izoksazolil, pirolil, i tiazolil po potrebi supstituisani sa do dva dodatna supstituenta koja su nezavisno odabrana iz grupe koja se sastoji iz SO2CH3, SO2NH2, C(O)NH2, -CN, OC(1-2)alkil, (CH2)(2-3)OCH3, SCH3, CF3, F, Cl, i C(1-2)alkil; i pomenuti tiadiazolil i oksadiazolil su po potrebi supstituisani sa C(1-2)alkil; i pomenuti piridil, piridil-N-oksid, pirimidinil, piridazil, i pirazinil su po potrebi supstituisani sa do tri dodatna supstituenta koji su nezavisno odabrani iz grupe koja se sastoji od C(O)NHC(1-2)alkil, C(O)N(C(1-2)alkil)2, NHC(O)C(1-4)alkil, NHSO2C(1-4)alkil, C(O)CF3, SO2CF3, SO2NHC(1-2)alkil, SO2N(C(1-2)alkil)2, C(O)NHSO2CH3, SO2CH3, SO2NH2, C(O)NH2, -CN, OC(1-4)alkil, (CH2)(2-3)OCH3, SC(1-4)alkil, CF3, F, Cl, i C(1-4)alkil; R2 je triazolil, piridil, piridil-N-oksid, pirazolil, pirimidinil, oksazolil, izoksazolil, azetidin-3-il, N-acetil-azetidin-3-il, N-metilsulfonil-azetidin-3-il, N-Bok-azetidin-3-il, N-acetil piperidinil, 1-H-piperidinil, N-Bok-piperidinil, N-C(1-3)alkil-piperidinil, tiazolil, piridazil, pirazinil, 1-(3-metoksipropil)-imidazolil, tiadiazolil, oksadiazolil, ili imidazolil; pri čemu je pomenuti imidazolil po potrebi supstituisan sa do tri dodatna supstituenta koji su nezavisno odabrani iz grupe koja se sastoji iz C(1-2)alkil, SCH3, OC(1-2)alkil, CF3, -CN, F, i Cl; i pomenuti piridil, piridil-N-oksid, pirimidinil, piridazil, i pirazinil, su po potrebi supstituisani sa do tri dodatna supstituenta koji su nezavisno odabrani iz grupe koja se sastoji od SO2CH3, SO2NH2, C(O)NH2, -CN, OC(1-2)alkil, (CH2)(2-3)OCH3, SCH3, CF3, F, Cl, ili C(1-2)alkil; i pomenuti triazolil, tiazolil, oksazolil i izoksazolil su po potrebi supstituisani sa do dva supstituenta koji su nezavisno odabrani iz grupe koja se sastoji iz SO2CH3, SO2NH2, C(O)NH2, -CN, OC(1-2)alkil, (CH2)(2-3)OCH3, SCH3, CF3, F, Cl, i C(1-2)alkil; i pomenuti tiadiazolil i oksadiazolil su po potrebi supstituisani sa C(1-2)alkil; i pomenuti pirazolil je po potrebi supstituisan sa do tri CH3 grupe; R3 je H, OH, OCH3, ili NH2; R4 je H, ili F; R5 je H, Cl, -CN, CF3, SC(1-4)alkil, OC(1-4)alkil, OH, C(1-4)alkil, N(CH3)OCH3, NH(C(1-4)alkil), N(C(1-4)alkil)2, ili 4-hidroksi-piperidinil; R6 je fenil, piridil, benzotiofenil, tiofenil, pirimidinil, piridazil, ili pirazinil; pri čemu su pomenuti pirimidinil, piridazil, ili pirazinil po potrebi supstituisani sa Cl, F, CH3, SCH3, OC(1-4)alkil, -CN, CONH2, SO2NH2, ili SO2CH3; i pri čemu je pomenuti fenil ili pomenuti piridil po potrebi supstitisan do dva puta sa OCF3, SO2C(1-4)alkil, CF3, CHF2, pirazolil, triazolil, imidazolil, tetrazolil, oksazolil, tiazolil, C(1-4)alkil, C(3-4)cikloalkil, OC(1-4)alkil, N(CH3)2, SO2NH2, SO2NHCH3, SO2N(CH3)2, CONH2, CONHCH3, CON(CH3)2, Cl, F,-CN, CO2H, OH, CH2OH, NHCOC(1-2)alkil, COC(1-2)alkil, SCH3, CO2C(1-4)alkil, NH2, NHC(1-2)alkil, ili OCH2CF3; pri čemu je odabir svakog supstituenta po potrebi nezavisan; i pri čemu su pomenuti pirazolil, triazolil, imidazolil, tetrazolil, oksazolil, i tiazolil po potrebi supstituisani sa CH3; R7 je H, Cl, -CN, C(1-4)alkil, OC(1-4)alkilCF3, OCF3, OCHF2, OCH2CH2OC(1-4)alkil, CF3, SCH3, C(1-4)alkilNA1A2, CH2OC(2-3)alkilNA1A2, NA1A2, C(O)NA1A2, CH2NHC(2-3)alkilNA1A2, CH2N(CH3)C(2-3)alkilNA1A2, NHC(2-3)alkilNA1A2, N(CH3)C(2-4)alkilNA1A2, OC(2-4)alkilNA1A2, OC(1-4)alkil, OCH2-(1-metil)-imidazol-2-il, fenil, tiofenil, furil, pirazolil, imidazolil, piridil, piridazil, pirazinil, ili pirimidinil; pri čemu su pomenuti fenil, tiofenil, furil, pirazolil, imidazolil, piridil, piridazil, pirazinil, i pirimidinil po potrebi supstituisani sa do tri supstituenta koji su nezavisno odabrani iz grupe koja se sastoji iz F, Cl, CH3, CF3, i OCH3; A1 je H, ili C(1-4)alkil; A2 je H, C(1-4)alkil, C(1-4)alkilOC(1-4)alkil, C(1-4)alkilOH, C(O)C(1-4)alkil, ili OC(1-4)alkil; ili A1 i A2 mogu da se uzmu zajedno sa njihovim vezanim azotom da se dobije prsten koji je izabran iz grupe koja se sastoji od: i Ra je H, OC(1-4)alkil, CH2OH, NH(CH3), N(CH3)2, NH2, CH3, F, CF3, SO2CH3, ili OH; Rb je H, CO2C(CH3)3, C(1-4)alkil, C(O)C(1-4)alkil, SO2C(1-4)alkil, CH2CH2CF3, CH2CF3, CH2-ciklopropil, fenil, CH2-fenil, ili C(3-6)cikloalkil; R8 je H, C(1-3)alkil, OC(1-3)alkil, CF3, NH2, NHCH3, -CN, ili F; R9 je H, ili F; i njegove farmaceutski prihvatljive soli; pod uslovom da su (4-hloro-2-metoksi-3-(4-(trifluorometil)benzil)hinolin-6-il)bis(1,2,5-trimetil-1H-imidazol-4-il)metanol, N-(2-((3-(4-(1H-pirazol-1-il)benzil)-6-((4-hlorofenil)(hidroksi)(1-metil-1H-imidazol-5-il)metil)-4-hidroksihinolin-2-il)oksi)etil)acetamid i (3-(4-(1H-pirazol-1-il)benzil)-4-hloro-2-(4-metilpiperazin-1-il)hinolin-6-il)(1-metil-1H-imidazol-5-il)(6-(trifluorometil)piridin-3-il)metanol isključeni iz zahteva.
2. Jedinjenje prema zahtevu 1 pri čemu: R1 je pirolil, pirazolil, imidazolil, triazolil, tiazolil, piridil, piridil N-oksid, pirazinil, pirimidinil, piridazil, piperidinil, tetrahidropiranil, fenil, oksazolil, izoksazolil, tiofenil, benzoksazolil, ili hinolinil; pri čemu su pomenuti piperidinil, imidazolil, fenil, tiofenil, benzoksazolil, pirazolil, piridil, piridil N-oksid, pirazinil, pirimidinil, piridazil, ili hinolinil po potrebi supstituisani sa C(O)C(1-4)alkil, C(O)NH2, C(1-4)alkil, CF3, CH2CF3, Cl, F, -CN, OC(1-4)alkil, N(C(1-4)alkil)2, -(CH2)3OCH3, SC(1-4)alkil, OH, CO2H, CO2C(1-4)alkil, OCF3, OCHF2, SO2CH3, SO2NH2, ili OCH2OCH3; i po potrebi supstituisani sa do dva dodatna supstituenta koji su nezavisno odabrani iz grupe koja se sastoji iz Cl, C(1-2)alkil, SCH3, OC(1-2)alkil, CF3, -CN, i F; i pri čemu su pomenuti triazolil, oksazolil, izoksazolil, pirolil, i tiazolil po potrebi supstituisani sa do dva supstituenta koji su nezavisno odabrani iz grupe koja se sastoji iz SO2CH3, SO2NH2, C(O)NH2, -CN, OC(1-2)alkil, (CH2)(2-3)OCH3, SCH3, CF3, F, Cl, i C(1-2)alkil; i pomenuti piridil, i piridil-N-oksid su po potrebi supstituisani sa do tri dodatna supstituenta koji su nezavisno odabrani iz grupe koja se sastoji iz do tri dodatna supstituenta koji su nezavisno odabrani iz grupe koja se sastoji iz SO2CH3, SO2NH2, C(O)NH2, -CN, OC(1-4)alkil, (CH2)(2-3)OCH3, SC(1-4)alkil, CF3, F, Cl, i C(1-4)alkil; R2 je 1-metil triazolil, piridil, piridil-N-oksid, 1-metil pirazolil, pirimidinil, oksazolil, izoksazolil, N-acetilazetidin-3-il, N-metilsulfonil-azetidin-3-il, N-Bok-azetidin-3-il, N-acetil piperidinil, 1-H-piperidinil, N-Bok-piperidinil, N-C(1-3)alkil-piperidinil, tiazolil, piridazil, pirazinil, 1-(3-metoksipropil)-imidazolil, ili 1-C(1-2)alkil imidazolil; pri čemu je pomenuti 1-C(1-2)alkil imidazolil po potrebi supstituisan sa do dva dodatna supstituenta koji su nezavisno odabrani iz grupe koja se sastoji iz C(1-2)alkil, SCH3, OC(1-2)alkil, CF3, -CN, F, i Cl; i pomenuti piridil, i piridil-N-oksid su po potrebi supstituisani sa do tri dodatna supstituenta koji su nezavisno odabrani iz grupe koja se sastoji iz SO2CH3, SO2NH2, C(O)NH2, -CN, OC(1-2)alkil, (CH2)(2-3)OCH3, SCH3, CF3, F, Cl, i C(1-2)alkil; i pomenuti tiazolil, oksazolil i izoksazolil su po potrebi supstituisani sa do dva supstituenta koji su nezavisno odabrani iz grupe koja se sastoji iz SO2CH3, SO2NH2,C(O)NH2, -CN, OC(1-2)alkil, (CH2)(2-3)OCH3, SCH3, CF3, F, Cl, i C(1-2)alkil; i pomenti 1-metil pirazolil je po potrebi supstituisan sa do dve dodatne CH3 grupe; R6 je fenil, piridil, benzotiofenil, tiofenil, pirimidinil, piridazil, ili pirazinil; pri čemu je pomenuti fenil ili pomenuti piridil po potrebi supstituisan sa OCF3, SO2C(1-4)alkil, CF3, CHF2, pirazolil, triazolil, imidazolil, tetrazolil, oksazolil, tiazolil, C(1-4)alkil, C(3-4)cikloalkil, OC(1-4)alkil, N(CH3)2, SO2NH2, SO2NHCH3, SO2N(CH3)2, CONH2, CONHCH3, CON(CH3)2, Cl, F, -CN, CO2H, OH, CH2OH, NHCOC(1-2)alkil, COC(1-2)alkil, ili SCH3; R7 je H, Cl, -CN, C(1-4)alkil, OC(1-4)alkilCF3, OCH2CH2OC(1-4)alkil, CF3, SCH3, CH2NA1A2, CH2OC(2-3)alkiNA1A2, NA1A2, C(O)NA1A2, N(CH3)C(2-4)alkilNA1A2, OC(2-4)alkilNA1A2, OC(1-4)alkil, OCH2-(1-metil)-imidazol-2-il, furil, pirazolil, imidazolil, piridil, piridazil, pirazinil, ili pirimidinil; pri čemu je pomenuti imidazolil ili pirazolil po potrebi supstituisan sa jednom CH3 grupom; A1 je H ili C(1-4)alkil; A2 je H, C(1-4)alkil, C(1-4)alkilOC(1-4)alkil, C(1-4)alkilOH, C(O)C(1-4)alkil, ili OC(1-4)alkil; ili A1 i A2 mogu da se uzmu zajedno sa njihovim vezanim azotom da se dobije prsten koji je izabran iz grupe koja se sastoji od: i Ra je H, OC(1-4)alkil, CH2OH, NH(CH3), N(CH3)2, NH2, CH3, F, ili OH; Rb je H, CO2C(CH3)3, C(1-4)alkil, C(O)C(1-4)alkil, SO2C(1-4)alkil, CH2CH2CF3, CH2CF3, CH2-ciklopropil, fenil, CH2-fenil, ili C(3-6)cikloalkil; R8 je H, CH3, OCH3, ili F; i njegove farmaceutski prihvatljive soli.
3. Jedinjenje prema zahtevu 2 pri čemu: R1 je pirolil, pirazolil, imidazolil, triazolil, tiazolil, piridil, piridil N-oksid, pirazinil, pirimidinil, piridazil, piperidinil, tetrahidropiranil, fenil, oksazolil, izoksazolil, tiofenil, benzoksazolil, ili hinolinil; pri čemu su pomenuti piperidinil, piridil, piridil N-oksid, imidazolil, fenil, tiofenil, benzoksazolil, i pirazolil po potrebi supstituisani sa C(O)C(1-4)alkil, C(O)NH2, C(1-4)alkil, CF3, CH2CF3, Cl, F, -CN, OC(1-4)alkil, N(C(1-4)alkil)2, -(CH2)3OCH3, SC(1-4)alkil, OH, CO2H, CO2C(1-4)alkil, OCF3, OCHF2, SO2CH3, SO2NH2, ili OCH2OCH3; i po potrebi supstituisani sa do dva dodatna supstituenta koji su nezavisno odabrani iz grupe koja se sastoji od Cl, OCH3, i CH3; i pri čemu su pomenuti triazolil, oksazolil, izoksazolil, i tiazolil po potrebi supstituisani sa jednom ili dve CH3 grupe; R2 je 1-metil triazolil, piridil, piridil-N-oksid, 1-metil pirazolil, pirimidinil, pirazinil, oksazolil, izoksazolil, N-acetil-azetidin-3-il, N-metilsulfonil-azetidin-3-il, N-Bok-azetidin-3-il, N-acetil piperidinil, 1-H-piperidinil, N-Bok-piperidinil, N-C(1-2)alkil-piperidinil, tiazolil, piridazil, 1-(3-metoksipropil)-imidazolil, ili 1-C(1-2)alkil imidazolil; pri čemu je pomenuti 1-C(1-2)alkil imidazolil po potrebi supstituisan sa do dve dodatne CH3 grupe, ili sa jednim supstituentom koji je odabran iz grupe koja se sastoji iz SCH3, i Cl; i pomenuti piridil, i piridil-N-oksid su po potrebi supstituisani sa do dva supstituenta koji su nezavisno odabrani iz grupe koja se sastoji iz SO2CH3, SO2NH2, C(O)NH2, -CN, OCH3, CF3, Cl, i CH3; i pomenuti tiazolil, oksazolil i izoksazolil su po potrebi supstituisani sa do dve CH3 grupe; i pomenuti 1-metil pirazolil je po potrebi supstituisan sa do dve dodatne CH3 grupe; R6 je fenil, piridil, benzotiofenil, tiofenil, pirimidinil, piridazil, ili pirazinil; pri čemu je pomenuti fenil ili pomenuti piridil po potrebi supstituisan sa OCF3, SO2CH3, CF3, CHF2, pirazolil, triazolil, imidazolil, tetrazolil, oksazolil, tiiazolil, CH3, OCH3, N(CH3)2, SO2NH2, CONH2, Cl, F, -CN, CO2H, OH, CH2OH, NHCOCH3, ili COCH3; R7 je H, Cl, -CN, C(1-4)alkil, OC(1-4)alkilCF3, OCH2CH2OC(1-4)alkil, CF3, SCH3, NA1A2, C(O)NA1A2, N(CH3)C(2-4)alkiNA1A2, OC(2-4)alkilNA1A2, OC(1-4)alkil, OCH2-(1-metil)-imidazol-2-il, imidazolil, furil, pirazolil, piridil, ili pirimidinil; pri čemu je pomenuti imidazolil ili pirazolil po potrebi supstituisan sa jednom CH3 grupom; A1 je H, ili C(1-4)alkil; A2 je H, C(1-4)alkil, C(1-4)alkilOC(1-4)alkil, C(1-4)alkilOH, C(O)C(1-4)alkil, ili OC(1-4)alkil; ili A1 i A2 mogu da se uzmu zajedno sa njihovim vezanim azotom da se dobije prsten koji je izabran iz grupe koja se sastoji od: i Ra je H, F, OC(1-4)alkil, ili OH; Rb je C(1-4)alkil, C(O)CH3, ili fenil; i njegove farmaceutski prihvatljive soli.
4. Jedinjenje prema zahtevu 3 pri čemu: R1 je pirolil, pirazolil, imidazolil, triazolil, tiazolil, piridil, piridil N-oksid, pirazinil, pirimidinil, piridazil, piperidinil, tetrahidropiranil, fenil, oksazolil, izoksazolil, tiofenil, benzoksazolil, ili hinolinil; pri čemu su pomenuti piperidinil, piridil, piridil N-oksid, imidazolil, fenil, tiofenil, benzoksazolil, i pirazolil po potrebi supstituisani sa SO2CH3, C(O)CH3, C(O)NH2, CH3, CH2CH3, CF3, Cl, F, -CN, OCH3, N(CH3)2, -(CH2)3OCH3, SCH3, OH, CO2H, CO2C(CH3)3, ili OCH2OCH3; i po potrebi supstituisani sa do dva dodatna supstituenta koji su nezavisno odabrani iz grupe koja se sastoji iz Cl, OCH3, i CH3; i pri čemu su pomenuti triazolil, oksazolil, izoksazolil, i tiazolil po potrebi supstituisani sa jednom ili dve CH3 grupe; R2 je 1-metil-1,2,3-triazolil, piridil, piridil-N-oksid, 1-metil pirazol-4-il, pirimidin-5-il, piridazil, pirazin-2-il, izoksazolil, N-acetil-azetidin-3-il, N-metilsulfonil-azetidin-3-il, N-Bok-azetidin-3-il, N-acetil piperidinil, 1-H-piperidinil, N-Bok-piperidinil, N-C(1-2)alkil-piperidinil, tiazol-5-il, 1-(3-metoksipropil)-imidazol-5-il, ili 1-C(1-2)alkil imidazol-5-il; pri čemu je pomenuti 1-C(1-2)alkil imidazol-5-il po potrebi supstituisan sa do dve dodatne CH3 grupe, ili sa jednim supstituentom koji je odabran iz grupe koja se sastoji iz SCH3, i Cl; i pomenuti piridil, i piridil-N-oksid su po potrebi supstituisani sa do dva supstituenta koji su nezavisno odabrani iz grupe koja se sastoji iz C(O)NH2, -CN, OCH3, CF3, Cl, i CH3; i pomenuti tiazol-5-il, i pomenuti izoksazolil su po potrebi supstituisani sa do dve CH3 grupe; i pomenuti 1-metil pirazol-4-il je po potrebi supstituisan sa do dve dodatne CH3 grupe; R5 je H, Cl, -CN, CF3, SCH3, OC(1-3)alkil, OH, C(1-4)alkil, N(CH3)OCH3, NH(C(1-2)alkil), N(C(1-2)alkil)2, ili 4-hidroksi-piperidinil; R6 je piridil, fenil, benzotiofenil, ili tiofenil; pri čemu je pomenuti piridil ili fenil je po potrebi supstituisan sa OCF3, SO2CH3, CF3, CHF2, imidazol-1-il, pirazol-1-il, 1,2,4-triazol-1-il, CH3, OCH3, Cl, F, ili -CN; R7 je H, Cl, -CN, C(1-4)alkil, OCH2CF3, OCH2CH2OCH3, CF3, SCH3, NA1A2, C(O)NHCH3, N(CH3)CH2CH2NA1A2, OCH2CH2NA1A2, OC(1-3)alkil, OCH2-(1-metil)-imidazol-2-il, imidazol-2-il, fur-2-il, pirazol-4-il, pirid-3-il, ili pirimidin-5-il; pri čemu je pomenuti imidazolil ili pirazolil po potrebi supstituisan sa jednom CH3 grupom; A1 je H, ili C(1-4)alkil; A2 je H, C(1-4)alkil, C(1-4)alkilOC(1-4)alkil, C(1-4)alkilOH, C(O)C(1-2)alkil, ili OCH3; ili A1 i A2 mogu da se uzmu zajedno sa njihovim vezanim azotom da se dobije prsten koji je izabran iz grupe koja se sastoji od: i Ra je H, F, OCH3, ili OH; Rb je CH3, ili fenil; i njegove farmaceutski prihvatljive soli.
5. Jedinjenje prema zahtevu 4 pri čemu: R1 je imidazolil, pirimidinil, triazolil, tetrahidropiranil, tiazolil, piridil, piperidinil, fenil, ili oksazolil; pri čemu su pomenuti piperidinil, piridil, imidazolil, i fenil po potrebi supstituisani sa SO2CH3, C(O)CH3, CH3, CF3, Cl, F, -CN, OCH3, -CF3, ili N(CH3)2; i po potrebi supstituisani sa do jednom dodatnom grupom koja je nezavisno odabrana iz Cl, OCH3, i CH3; i pri čemu su pomenuti triazolil, oksazolil, i tiazolil po potrebi supstituisani sa do jednom ili dve CH3 grupe; R2 je 1-metil-1,2-3triazol-5-il, pirid-3-il, 1-metil pirazol-4-il, tiazol-5-il, N-acetil-piperidin-4-il, N-acetilazetidin-3-il, N-metilsulfonil-azetidin-3-il, N-Bok-azetidin-3-il, 1,2-dimetil imidazol-5-il ili 1-metil imidazol-5-il; R3 je OH, ili NH2; R4 je H; R5 je H, Cl, -CN, CF3, CH3, OH, N(CH3)OCH3, ili OCH3; R6 je piridil, fenil, benzotiofenil, ili tiofenil; pri čemu je pomenuti piridil ili fenil je po potrebi supstituisan sa pirazol-1-il, 1,2,4-triazol-1-il, CF3, OCH3, SO2CH3, Cl, F, ili-CN; R7 je Cl, -CN, CF3, C(1-4)alkil, NA1A2, C(O)NHCH3, OCH2CH2OCH3, 1-metil imidazol-2-il, 1-metil pirazol-4-il, ili OC(1-2)alkil; A1 je C(1-2)alkil; A2 je C(1-2)alkil, CH2CH2OCH3, ili OCH3; ili A1 i A2 mogu da se uzmu zajedno sa njihovim vezanim azotom da se dobije prsten koji je izabran iz grupe koja se sastoji od: i Ra je OH, OCH3, F, ili H; R9 je H; i njegove farmaceutski prihvatljive soli.
6. Jedinjenje prema zahtevu 5 pri čemu: R1 je imidazolil, triazolil, tiazolil, piridil, piperidinil, fenil, ili oksazolil; pri čemu su pomenuti piperidinil, piridil, imidazolil, i fenil po potrebi supstituisani sa C(O)CH3, CH3, CF3, Cl, F, -CN, OCH3, ili N(CH3)2; i po potrebi supstituisani sa do jednom dodatnom grupom koja je nezavisno odabrana od Cl, OCH3, i CH3; i pri čemu su pomenuti triazolil, oksazolil, i tiazolil po potrebi supstituisani sa jednom ili dve CH3 grupe; R2 je 1-metil-1,2-3triazol-5-il, pirid-3-il, 1-metil pirazol-4-il, tiazol-5-il, N-acetil-piperidin-4-il, 1,2-dimetil imidazol-5-il ili 1-metil imidazol-5-il; R3 je OH; R5 je H, Cl, -CN, CF3, CH3, ili OCH3; R6 je fenil, tiofen-2-il, benzotiofen-2-il; pri čemu je pomenuti fenil po potrebi supstituisan sa pirazol-1-il, 1,2,4-triazol-1-il, OCH3, SO2CH3, Cl, F, CF3, ili -CN; R7 je Cl, -CN, CH3, NA1A2, C(O)NHCH3, ili OC(1-2)alkil; A1 je C(1-2)alkil; A2 je C(1-2)alkil, ili OCH3; ili A1 i A2 mogu da se uzmu zajedno sa njihovim vezanim azotom da se dobije prsten koji je izabran iz grupe koja se sastoji od: i njegove farmaceutski prihvatljive soli.
7. Jedinjenje prema zahtevu 1 koje je odabrano iz grupe koja se sastoji od: i njegove farmaceutski prihvatljive soli.
8. Jedinjenje prema zahtevu 1 koje je odabrano iz grupe koja se sastoji od: i njegove farmaceutski prihvatljive soli.
9. Jedinjenje koje je i njegove farmaceutski prihvatljive soli.
10. Farmaceutska kompozicija, koja obuhvata jedinjenje prema zahtevu 1 i farmaceutski prihvatljivi nosač.
11. Farmaceutska kompozicija koja se dobija mešanjem jedinjenja prema zahtevu 1 i farmaceutski prihvatljivog nosača.
12. Postupak za dobijanje farmaceutske kompozicije koji obuhvata mešanje jedinjenja prema zahtevu 1 i farmaceutski prihvatljivog nosača.
13. Jedinjenje prema zahtevu 1 za upotrebu u lečenju ili ublažavanju RORγt posredovanog zapaljenskog sindroma, poremećaja ili bolesti.
14. Jedinjenje prema zahtevu 1 korišćeno prema zahtevu 13, pri čemu je bolest odabrana iz grupe koja se sastoji od: reumatoidnog artritisa, psorijaze, hroničnog opstruktivnog poremećaja pluća, psorijatičnog artritisa, ankilozirajućeg spondilitisa, Kronove bolesti, astme posredovane neutrofilima, astme koja je rezistentna na steroide, multiple skleroze, sistemskog lupusa eritematozusa, i ulcerativnog kolitisa.
15. Jedinjenje prema zahtevu 1 korišćeno prema zahtevu 13, pri čemu je bolest psorijaza.
16. Jedinjenje prema zahtevu 1 korišćeno prema zahtevu 13, pri čemu je bolest reumatoidni artritis.
17. Jedinjenje prema zahtevu 1 ili kompozicija ili njegov lek za upotrebu u kombinovanoj terapiji sa jednim ili više anti-inflamatornim agensima, ili imunosupresivnim agensima, za lečenje ili ublažavanje sindroma, poremećaja ili bolesti koja je odabrana iz grupe koja se sastoji iz: reumatoidnog artritisa, i psorijaze.
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Families Citing this family (32)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| MX2014008856A (es) * | 2012-02-13 | 2014-12-15 | Hoffmann La Roche | Derivados de imidazolilcetona como inhibidores de aldosterona sintasa. |
| AU2014230814B2 (en) | 2013-03-14 | 2017-12-21 | Boehringer Ingelheim International Gmbh | Substituted 2-Aza-bicyclo[2.2.1]heptane-3-carboxylic acid (benzyl-cyano-methyl)-amides inhibitors of Cathepsin C |
| TWI627174B (zh) | 2013-03-14 | 2018-06-21 | 比利時商健生藥品公司 | Ｐ２ｘ７調控劑 |
| ES2689526T3 (es) | 2013-03-14 | 2018-11-14 | Janssen Pharmaceutica Nv | Moduladores de P2X7 |
| EP3112366B1 (en) | 2013-03-14 | 2018-02-28 | Janssen Pharmaceutica NV | P2x7 modulators |
| JO3773B1 (ar) | 2013-03-14 | 2021-01-31 | Janssen Pharmaceutica Nv | معدلات p2x7 |
| CN105705501B (zh) | 2013-09-09 | 2019-04-19 | 百时美施贵宝公司 | RORγ调节剂 |
| US9284308B2 (en) * | 2013-10-15 | 2016-03-15 | Janssen Pharmaceutica Nv | Methylene linked quinolinyl modulators of RORγt |
| US9403816B2 (en) | 2013-10-15 | 2016-08-02 | Janssen Pharmaceutica Nv | Phenyl linked quinolinyl modulators of RORγt |
| KR20160068956A (ko) * | 2013-10-15 | 2016-06-15 | 얀센 파마슈티카 엔.브이. | RORyT의 퀴놀리닐 조절제 |
| AU2014334619A1 (en) | 2013-10-15 | 2016-04-21 | Janssen Pharmaceutica Nv | Alkyl linked quinolinyl modulators of RORyt |
| CN105636952A (zh) * | 2013-10-15 | 2016-06-01 | 詹森药业有限公司 | Rorγt的仲醇喹啉基调节剂 |
| US10555941B2 (en) | 2013-10-15 | 2020-02-11 | Janssen Pharmaceutica Nv | Alkyl linked quinolinyl modulators of RORγt |
| KR20160068957A (ko) * | 2013-10-15 | 2016-06-15 | 얀센 파마슈티카 엔.브이. | Ror-gamma-t의 메틸렌 결합 퀴놀리닐 조절제 |
| ES2716966T3 (es) * | 2014-05-28 | 2019-06-18 | Glaxosmithkline Ip Dev Ltd | Derivados de piperazina como moduladores de ROR-gamma |
| AU2015301891B2 (en) | 2014-08-11 | 2019-12-05 | Angion Biomedica Corporation | Cytochrome P450 inhibitors and uses thereof |
| EA201790600A1 (ru) | 2014-09-12 | 2017-07-31 | Янссен Фармацевтика Нв | Модулирующие p2x7 n-ацил-триазолопиразины |
| KR102510588B1 (ko) | 2014-09-12 | 2023-03-17 | 베링거 인겔하임 인터내셔날 게엠베하 | 카텝신 c의 스피로사이클릭 억제제 |
| WO2016039977A1 (en) | 2014-09-12 | 2016-03-17 | Janssen Pharmaceutica Nv | P2x7 modulators |
| EP3240778A4 (en) | 2014-12-31 | 2018-07-11 | Angion Biomedica Corp. | Methods and agents for treating disease |
| WO2020065613A1 (en) | 2018-09-28 | 2020-04-02 | Janssen Pharmaceutica Nv | Monoacylglycerol lipase modulators |
| MA53722A (fr) | 2018-09-28 | 2022-03-30 | Janssen Pharmaceutica Nv | Modulateurs de la monoacylglycérol lipase |
| US10947253B2 (en) | 2019-08-05 | 2021-03-16 | Ankh Life Sciences Limited | Fused polycyclic dimers |
| CN114555596B (zh) | 2019-09-30 | 2025-02-25 | 詹森药业有限公司 | 放射性标记的mgl pet配体 |
| US20220411380A1 (en) * | 2019-10-31 | 2022-12-29 | Jiangsu Hengrui Medicine Co., Ltd. | ACID ADDITION SALT OF RORy REGULATOR |
| US11891387B2 (en) | 2020-03-26 | 2024-02-06 | Janssen Pharmaceutica Nv | Monoacylglycerol lipase modulators |
| EP4143179B1 (en) | 2020-04-30 | 2025-10-22 | Idorsia Pharmaceuticals Ltd | Azetidin-3-ylmethanol derivatives as ccr6 receptor modulators for the treatment of cancer |
| US12129265B2 (en) | 2020-07-21 | 2024-10-29 | Ankh Life Sciences Limited | Therapeutic agents and uses thereof |
| CN112939974B (zh) * | 2021-03-11 | 2023-10-20 | 中山大学 | 一种氮杂苯并薁衍生物的制备方法 |
| WO2023057548A1 (en) | 2021-10-07 | 2023-04-13 | Idorsia Pharmaceuticals Ltd | Ccr6 receptor modulators |
| WO2023072924A1 (en) | 2021-10-26 | 2023-05-04 | Idorsia Pharmaceuticals Ltd | Ccr6 receptor modulators |
| KR20240090693A (ko) | 2021-10-28 | 2024-06-21 | 이도르시아 파마슈티컬스 리미티드 | Ccr6 수용체 조절인자 |
Family Cites Families (102)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3472859A (en) | 1966-11-01 | 1969-10-14 | Sterling Drug Inc | 1-alkyl-1,4-dihydro-4-oxo-3 quinoline-carboxylic acids and esters |
| JPS4826772Y1 (me) | 1969-04-04 | 1973-08-06 | ||
| ATE27451T1 (de) | 1981-03-24 | 1987-06-15 | Ciba Geigy Ag | Acyl-chinolinonderivate, verfahren zu ihrer herstellung, diese enthaltende pharmazeutische praeparate und ihre verwendung. |
| US4910327A (en) | 1982-05-25 | 1990-03-20 | American Cyanamid Company | Alkyl esters of substituted 2-methyl-3-quinolinecarboxylic acid and quinoline-2,3-dicarboxylic acid: dialkyl 3-(substituted)phenylaminobut-2-ene-dioates and methods for the preparation thereof |
| US4656283A (en) | 1982-05-25 | 1987-04-07 | American Cyanamid Company | Alkyl esters of substituted 2-methyl-3-quinolinecarboxylic acid and quinoline-2,3-dicarboxylic acid |
| US4710507A (en) | 1983-12-22 | 1987-12-01 | Pfizer Inc. | Quinolone inotropic agents |
| FR2634483B2 (fr) | 1987-12-29 | 1994-03-04 | Esteve Labor Dr | Derives des acides 7-(1-azetidinyl)-1,4-dihydro-4-oxoquinoleine-3-carboxyliques, leur preparation et leur application en tant que medicaments |
| CA2002864C (en) | 1988-11-29 | 1999-11-16 | Eddy J. E. Freyne | (1h-azol-1-ylmethyl) substituted quinoline, quinazoline or quinoxaline derivatives |
| ES2108120T3 (es) | 1991-05-10 | 1997-12-16 | Rhone Poulenc Rorer Int | Compuestos bis arilicos y heteroarilicos mono- y biciclicos que inhiben tirosina quinasa receptora de egf y/o pdgf. |
| US5478832A (en) | 1992-05-08 | 1995-12-26 | The Green Cross Corporation | Quinoline compounds |
| JPH0826772A (ja) | 1994-07-22 | 1996-01-30 | Sony Corp | 融着用ガラス、その製造方法及び製造装置、並びに磁気ヘッドの製造方法 |
| ES2136782T3 (es) | 1994-10-27 | 1999-12-01 | Asahi Glass Co Ltd | Procedimiento para producir compuestos de acido quinolin-2-il-benzoico. |
| GB9523267D0 (en) | 1995-11-14 | 1996-01-17 | Sandoz Ltd | Organic compounds |
| SI1162201T1 (sl) | 1995-12-08 | 2006-08-31 | Janssen Pharmaceutica Nv | (Imidazol-5-il)metil-2-kinolinonski derivati kot inhibitorji farnezil protein transferaze |
| AU710926B2 (en) | 1996-05-20 | 1999-09-30 | Merck & Co., Inc. | Antagonists of gonadotropin releasing hormone |
| ATE222104T1 (de) * | 1997-06-02 | 2002-08-15 | Janssen Pharmaceutica Nv | (imidazol-5-yl)methyl-2-quinolinone derivativen als inhibitoren von proliferation der glatten muskelzellen |
| US6093732A (en) | 1997-12-22 | 2000-07-25 | Pharmacia & Upjohn Company | 4-hydroxyquinoline-3-carboxamides and hydrazides as antiviral agents |
| FR2776388B1 (fr) | 1998-03-20 | 2006-04-28 | Lipha | Utilisation de recepteurs de la famille ror pour le criblage de substances utiles pour le traitement de l'atherosclerose |
| US6399629B1 (en) | 1998-06-01 | 2002-06-04 | Microcide Pharmaceuticals, Inc. | Efflux pump inhibitors |
| PT1094839E (pt) | 1998-07-06 | 2003-09-30 | Janssen Pharmaceutica Nv | Inibidores da proteina farnesil transferase com propriedades de radiossensibilizacao (in vivo) |
| HRP20000904A2 (en) | 1998-07-06 | 2001-12-31 | Janssen Pharmaceutica Nv | Farnesyl protein transferase inhibitors for treating arthropathies |
| JP2000169451A (ja) | 1998-09-30 | 2000-06-20 | Kyorin Pharmaceut Co Ltd | ６，７―ジ置換キノリンカルボン酸誘導体とその付加塩及びそれらの製造方法 |
| EA004542B1 (ru) | 1998-12-23 | 2004-06-24 | Янссен Фармацевтика Н.В. | 1, 2-аннелированные производные хинолина |
| US6248736B1 (en) | 1999-01-08 | 2001-06-19 | Pharmacia & Upjohn Company | 4-oxo-1,4-dihydro-3-quinolinecarboxamides as antiviral agents |
| US6248739B1 (en) | 1999-01-08 | 2001-06-19 | Pharmacia & Upjohn Company | Quinolinecarboxamides as antiviral agents |
| AU2124800A (en) | 1999-02-11 | 2000-08-29 | Pfizer Products Inc. | Heteroaryl-substituted quinolin-2-one derivatives useful as anticancer agents |
| ES2212971T3 (es) | 1999-11-30 | 2004-08-16 | Pfizer Products Inc. | Derivados de quinolina utiles para la inhibicion de la farnesil protein transferasa. |
| SI1255537T1 (sl) | 2000-02-04 | 2006-10-31 | Janssen Pharmaceutica Nv | Inhibitorji farnezil protein transferaze za zdravljenje raka dojk |
| EP1267848B1 (en) | 2000-02-24 | 2007-10-17 | Janssen Pharmaceutica N.V. | Dosing regimen comprising a farnesyl protein transferase inhibitor for the treatment of cancer |
| EP1263437A2 (en) | 2000-02-29 | 2002-12-11 | Janssen Pharmaceutica N.V. | Farnesyl protein transferase inhibitor combinations with vinca alkaloids |
| WO2001064246A2 (en) | 2000-02-29 | 2001-09-07 | Janssen Pharmaceutica N.V. | Farnesyl protein transferase inhibitor combinations with an her2 antibody |
| JP2003525245A (ja) | 2000-02-29 | 2003-08-26 | ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプ | ファルネシルタンパク質トランスフェラーゼ阻害剤組み合わせ剤 |
| EP1261341A2 (en) | 2000-02-29 | 2002-12-04 | Janssen Pharmaceutica N.V. | Farnesyl protein transferase inhibitor combinations with camptothecin compounds |
| EP1261356A2 (en) | 2000-02-29 | 2002-12-04 | Janssen Pharmaceutica N.V. | Farnesyl protein transferase inhibitor combinations with platinum compounds |
| JP2003525235A (ja) | 2000-02-29 | 2003-08-26 | ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプ | 抗腫瘍ヌクレオシド誘導体とのファルネシルタンパク質トランスフェラーゼ阻害剤の組み合わせ剤 |
| WO2001064217A2 (en) | 2000-02-29 | 2001-09-07 | Janssen Pharmaceutica N.V. | Combinations of a farnesyl protein transferase inhibitor with nitrogen mustard or nitrosourea alkylating agents |
| CA2397253A1 (en) | 2000-02-29 | 2001-09-07 | Janssen Pharmaceutica N.V. | Farnesyl protein transferase inhibitor combinations with anti-tumor anthracycline derivatives |
| CA2397425A1 (en) | 2000-02-29 | 2001-09-07 | Ivan David Horak | Farnesyl protein transferase inhibitor combinations with taxane compounds |
| JP2003525238A (ja) | 2000-02-29 | 2003-08-26 | ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプ | 抗腫瘍性ポドフィロトキシン誘導体とのファルネシルタンパク質トランスフェラーゼ阻害剤組み合わせ剤 |
| EP1261374A2 (en) | 2000-02-29 | 2002-12-04 | Janssen Pharmaceutica N.V. | Farnesyl protein transferase inhibitor combinations with further anti-cancer agents |
| US6844357B2 (en) | 2000-05-01 | 2005-01-18 | Pfizer Inc. | Substituted quinolin-2-one derivatives useful as antiproliferative agents |
| US6525049B2 (en) | 2000-07-05 | 2003-02-25 | Pharmacia & Upjohn Company | Pyrroloquinolones as antiviral agents |
| US6624159B2 (en) | 2000-07-12 | 2003-09-23 | Pharmacia & Upjohn Company | Heterocycle carboxamides as antiviral agents |
| PT1299395E (pt) | 2000-07-12 | 2005-01-31 | Upjohn Co | Oxazinoquinolonas uteis para o tratamento de infeccoes provocadas por virus |
| EP1322644A1 (en) | 2000-09-25 | 2003-07-02 | Janssen Pharmaceutica N.V. | Farnesyl transferase inhibiting 6-heterocyclylmethyl quinolinone derivatives |
| WO2002024686A2 (en) | 2000-09-25 | 2002-03-28 | Janssen Pharmaceutica N.V. | Farnesyl transferase inhibiting 6-heterocyclylmethyl quinoline and quinazoline derivatives |
| WO2002024682A1 (en) | 2000-09-25 | 2002-03-28 | Janssen Pharmaceutica N.V. | Farnesyl transferase inhibiting quinoline and quinazoline derivatives as farnesyl transferase inhibitors |
| US7115630B2 (en) | 2000-10-02 | 2006-10-03 | Janssen Pharmaceutica N.V. | Metabotropic glutamate receptor antagonists |
| ES2261523T3 (es) | 2000-11-28 | 2006-11-16 | Janssen Pharmaceutica N.V. | Inhibidores de farnesil proteina transferasa para el tratamiento de enfermedad intestinal inflamatoria. |
| WO2002051835A1 (en) | 2000-12-27 | 2002-07-04 | Janssen Pharmaceutica N.V. | Farnesyl transferase inhibiting 4-substituted quinoline and quinazoline derivatives |
| DE60230017D1 (de) | 2001-02-15 | 2009-01-08 | Janssen Pharmaceutica Nv | Farnesyl-protein-transferase hemmer in kombination mit antiöstrogenen |
| JP2004520424A (ja) | 2001-03-01 | 2004-07-08 | ファルマシア・アンド・アップジョン・カンパニー | 抗ウイルス剤としての置換型キノリンカルボキサミド |
| JP2004526776A (ja) | 2001-04-25 | 2004-09-02 | ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプ | 悪液質を治療するためのファルネシルタンパク質トランスフェラーゼ阻害剤 |
| WO2003000705A1 (en) | 2001-06-21 | 2003-01-03 | Ariad Pharmaceuticals, Inc. | Novel quinolines and uses thereof |
| MXPA04006030A (es) | 2001-12-20 | 2004-09-27 | Upjohn Co | Antiviricos de piridoquinoxalina. |
| MXPA04006041A (es) | 2001-12-20 | 2004-09-27 | Upjohn Co | Antivirales de piridoquinoxalina. |
| EP1492571A2 (en) | 2002-03-29 | 2005-01-05 | Janssen Pharmaceutica N.V. | Radiolabelled quinoline and quinolinone derivatives and their use as metabotropic glutamate receptor ligands |
| EP2045242A1 (en) | 2002-08-13 | 2009-04-08 | Shionogi&Co., Ltd. | Heterocyclic compounds having inhibitory activity against HIV integrase |
| US20040186131A1 (en) | 2002-08-30 | 2004-09-23 | Wathen Michael W | Method of preventing or treating atherosclerosis or restenosis |
| GB0222516D0 (en) | 2002-09-27 | 2002-11-06 | Karobio Ab | Novel compounds |
| EP2292620A3 (en) | 2003-07-14 | 2011-06-22 | Arena Pharmaceuticals, Inc. | Fused-aryl and heteroaryl derivatives as modulators of metabolism and the prohylaxis and treatment of disorders related thereto |
| SG150533A1 (en) | 2003-11-20 | 2009-03-30 | Janssen Pharmaceutica Nv | 6-alkenyl and 6-phenylalkyl substituted 2-quinolinones and 2- quinoxalinones as poly(adp-ribose) polymerase inhibitors |
| SG151249A1 (en) | 2003-12-05 | 2009-04-30 | Janssen Pharmaceutica Nv | 6-substituted 2-quinolinones and 2-quinoxalinones as poly(adp-ribose) polymerase inhibitors |
| UA91007C2 (ru) | 2003-12-10 | 2010-06-25 | Янссен Фармацевтика Н.В. | Замещенные 6-циклогексилалкилом замещенные 2-хинолиноны и 2-хиноксалиноны как ингибиторы поли-(адф-рибоза)полимеразы |
| JP2007516258A (ja) | 2003-12-12 | 2007-06-21 | ワイス | 心臓血管の疾患治療に有用なキノリン誘導体 |
| ATE444068T1 (de) | 2004-01-23 | 2009-10-15 | Janssen Pharmaceutica Nv | Chinolinderivate und ihre verwendung als mycobakterielle inhibitoren |
| EA011572B9 (ru) | 2004-01-29 | 2018-01-31 | Янссен Фармацевтика Н.В. | Производные хинолина для применения в качестве микобактериальных ингибиторов |
| JP2005225250A (ja) | 2004-02-10 | 2005-08-25 | Murakami Corp | 車載用監視装置 |
| CN1976906B (zh) | 2004-06-30 | 2010-09-01 | 詹森药业有限公司 | 用作parp抑制剂的取代2-烷基喹唑啉酮衍生物 |
| IL180887A (en) | 2004-08-04 | 2014-04-30 | Nippon Kayaku Kk | Quinoline derivatives and insecticides containing them as active substance |
| KR100686531B1 (ko) | 2004-08-31 | 2007-02-23 | 한국화학연구원 | 히스톤 디아세틸라제 저해활성을 갖는 아릴아미노메틸프로페닐 벤즈하이드록시아마이드 유도체 및 그의 제조방법 |
| WO2006052718A2 (en) | 2004-11-05 | 2006-05-18 | Janssen Pharmaceutica N.V. | Farnesyltransferase inhibitors for treating sepsis |
| JO2952B1 (en) | 2005-08-03 | 2016-03-15 | جانسين فارماسوتيكا ان. في | Quinoline derivatives acting as antibacterial agents |
| JO2855B1 (en) | 2005-08-03 | 2015-03-15 | شركة جانسين فارماسوتيكا ان. في | Quinoline derivatives acting as antibacterial agents |
| WO2007088978A1 (ja) | 2006-02-03 | 2007-08-09 | Meiji Seika Kaisha, Ltd. | 新規キノリン誘導体およびこれを有効成分として含有する農園芸用殺菌剤 |
| US8389739B1 (en) | 2006-10-05 | 2013-03-05 | Orphagen Pharmaceuticals | Modulators of retinoid-related orphan receptor gamma |
| PL2081937T3 (pl) | 2006-10-23 | 2013-01-31 | Sgx Pharmaceuticals Inc | Triazolopirydazynowe modulatory kinaz białkowych |
| JO3271B1 (ar) | 2006-12-06 | 2018-09-16 | Janssen Pharmaceutica Nv | مشتقات الكوينولين المضادة للجراثيم |
| AR065093A1 (es) | 2007-02-05 | 2009-05-13 | Merck Frosst Canada Ltd | Compuestos farmacéuticos inhibidores de la biosintesis de leucotrienos |
| UY30892A1 (es) | 2007-02-07 | 2008-09-02 | Smithkline Beckman Corp | Inhibidores de la actividad akt |
| WO2008112525A2 (en) | 2007-03-09 | 2008-09-18 | Link Medicine Corporation | Treatment of lysosomal storage diseases |
| AU2008254588B2 (en) | 2007-05-21 | 2013-01-17 | Sgx Pharmaceuticals, Inc. | Heterocyclic kinase modulators |
| CN101143845B (zh) | 2007-10-15 | 2010-08-25 | 中国药科大学 | 取代喹啉甲酰胍衍生物、其制备方法及其医药用途 |
| ES2421896T3 (es) | 2008-01-18 | 2013-09-06 | Allergan Inc | Compuestos de aril-(imidazol)-metil-fenilo sustituidos como moduladores selectivos de los subtipos de receptores adrenérgicos alfa 2B y/o alfa 2C |
| WO2009098576A1 (en) | 2008-02-05 | 2009-08-13 | Pfizer Inc. | Pyridinyl amides for the treatment of cns and metabolic disorders |
| EP2296655A1 (en) | 2008-05-13 | 2011-03-23 | Allergan, Inc. | Quinolynylmethylimidizoles as therapeutic agents |
| WO2010068296A1 (en) | 2008-12-11 | 2010-06-17 | Stiefel Laboratories, Inc. | Piperazine carboxamidines as antimicrobial agents |
| WO2010127208A1 (en) | 2009-04-30 | 2010-11-04 | Forest Laboratories Holdings Limited | Inhibitors of acetyl-coa carboxylase |
| CN101899011B (zh) | 2009-05-26 | 2013-01-16 | 北京大学 | 氨基二硫代甲酸酯类化合物、其制备方法和应用 |
| AR077004A1 (es) | 2009-06-09 | 2011-07-27 | Hoffmann La Roche | Compuestos heterociclicos antivirales |
| EA201270013A1 (ru) | 2009-06-25 | 2012-06-29 | Амген Инк. | Гетероциклические соединения и их применение |
| MX2012002179A (es) | 2009-08-20 | 2012-03-16 | Novartis Ag | Compuestos heterociclicos de oxima. |
| EP2368886A1 (en) | 2010-03-01 | 2011-09-28 | Phenex Pharmaceuticals AG | Novel compounds for modulation of orphan nuclear receptor RAR-related orphan receptor-gamma (ROR gamma, NR1F3) activity and for the treatment of chronic inflammatory and autoimmune desease |
| US9101600B2 (en) | 2010-03-11 | 2015-08-11 | New York University | Compounds as RORγt modulators and uses thereof |
| AU2011239447B2 (en) | 2010-04-15 | 2016-03-17 | Chromocell Corporation | Compounds, compositions, and methods for reducing or eliminating bitter taste |
| AU2011326071A1 (en) * | 2010-11-08 | 2013-05-23 | Lycera Corporation | N- sulfonylated tetrahydroquinolines and related bicyclic compounds inhibition of RORy activity and the treatment of diseases |
| EP2678052B1 (en) | 2011-02-24 | 2018-09-26 | Emory University | Jab1 blocking compositions for ossification and methods related thereto |
| JP5902029B2 (ja) | 2011-04-28 | 2016-04-13 | 日本たばこ産業株式会社 | アミド化合物およびその医薬用途 |
| WO2012158784A2 (en) | 2011-05-16 | 2012-11-22 | Theodore Mark Kamenecka | Modulators of the nuclear hormone receptor ror |
| GB201118652D0 (en) | 2011-10-28 | 2011-12-07 | Astex Therapeutics Ltd | New compounds |
| WO2013064231A1 (en) | 2011-10-31 | 2013-05-10 | Phenex Pharmaceuticals Ag | SEVEN-MEMBERED SULFONAMIDES AS MODULATORS OF RAR-RELATED ORPHAN RECEPTOR-GAMMA (RORγ, NR1F3) |
| US9815851B2 (en) | 2011-12-02 | 2017-11-14 | Phenex Pharmaceuticals Ag | Pyrrolo carboxamides as modulators of orphan nuclear receptor RAR-related orphan receptor-gamma (RORγ, NR1F3) activity and for the treatment of chronic inflammatory and autoimmune diseases |
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