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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- Neurology (AREA)
- Neurosurgery (AREA)
- Dermatology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Physical Education & Sports Medicine (AREA)
- Pain & Pain Management (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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