HRP20201087T1 - Supstituirani imidazo-hinolini kao nlrp3 modulatori - Google Patents
Supstituirani imidazo-hinolini kao nlrp3 modulatori Download PDFInfo
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- HRP20201087T1 HRP20201087T1 HRP20201087TT HRP20201087T HRP20201087T1 HR P20201087 T1 HRP20201087 T1 HR P20201087T1 HR P20201087T T HRP20201087T T HR P20201087TT HR P20201087 T HRP20201087 T HR P20201087T HR P20201087 T1 HRP20201087 T1 HR P20201087T1
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- 229960000598 infliximab Drugs 0.000 claims 1
- 201000002313 intestinal cancer Diseases 0.000 claims 1
- 229960004768 irinotecan Drugs 0.000 claims 1
- UWKQSNNFCGGAFS-XIFFEERXSA-N irinotecan Chemical compound C1=C2C(CC)=C3CN(C(C4=C([C@@](C(=O)OC4)(O)CC)C=4)=O)C=4C3=NC2=CC=C1OC(=O)N(CC1)CCC1N1CCCCC1 UWKQSNNFCGGAFS-XIFFEERXSA-N 0.000 claims 1
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 1
- 201000010982 kidney cancer Diseases 0.000 claims 1
- 206010023841 laryngeal neoplasm Diseases 0.000 claims 1
- 208000012987 lip and oral cavity carcinoma Diseases 0.000 claims 1
- 229950011263 lirilumab Drugs 0.000 claims 1
- 201000007270 liver cancer Diseases 0.000 claims 1
- 208000014018 liver neoplasm Diseases 0.000 claims 1
- 201000005202 lung cancer Diseases 0.000 claims 1
- 208000020816 lung neoplasm Diseases 0.000 claims 1
- 201000001441 melanoma Diseases 0.000 claims 1
- GLVAUDGFNGKCSF-UHFFFAOYSA-N mercaptopurine Chemical compound S=C1NC=NC2=C1NC=N2 GLVAUDGFNGKCSF-UHFFFAOYSA-N 0.000 claims 1
- 229960001428 mercaptopurine Drugs 0.000 claims 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 1
- CFCUWKMKBJTWLW-BKHRDMLASA-N mithramycin Chemical compound O([C@@H]1C[C@@H](O[C@H](C)[C@H]1O)OC=1C=C2C=C3C[C@H]([C@@H](C(=O)C3=C(O)C2=C(O)C=1C)O[C@@H]1O[C@H](C)[C@@H](O)[C@H](O[C@@H]2O[C@H](C)[C@H](O)[C@H](O[C@@H]3O[C@H](C)[C@@H](O)[C@@](C)(O)C3)C2)C1)[C@H](OC)C(=O)[C@@H](O)[C@@H](C)O)[C@H]1C[C@@H](O)[C@H](O)[C@@H](C)O1 CFCUWKMKBJTWLW-BKHRDMLASA-N 0.000 claims 1
- 229960004857 mitomycin Drugs 0.000 claims 1
- JJVZSYKFCOBILL-MKMRYRNGSA-N motixafortide Chemical compound NCCCC[C@@H]1NC(=O)[C@H](CCCNC(N)=O)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](CSSC[C@H](NC(=O)[C@H](CCCNC(N)=O)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@@H]2CCCN2C(=O)[C@H](CCCCN)NC1=O)C(=O)N[C@@H](CCCNC(N)=N)C(N)=O)NC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](CCCNC(N)=N)NC(=O)c1ccc(F)cc1 JJVZSYKFCOBILL-MKMRYRNGSA-N 0.000 claims 1
- 210000000214 mouth Anatomy 0.000 claims 1
- 229960003816 muromonab-cd3 Drugs 0.000 claims 1
- 201000000050 myeloid neoplasm Diseases 0.000 claims 1
- 229960002653 nilutamide Drugs 0.000 claims 1
- XWXYUMMDTVBTOU-UHFFFAOYSA-N nilutamide Chemical compound O=C1C(C)(C)NC(=O)N1C1=CC=C([N+]([O-])=O)C(C(F)(F)F)=C1 XWXYUMMDTVBTOU-UHFFFAOYSA-N 0.000 claims 1
- 201000008106 ocular cancer Diseases 0.000 claims 1
- 229960002450 ofatumumab Drugs 0.000 claims 1
- 229960000470 omalizumab Drugs 0.000 claims 1
- 201000005443 oral cavity cancer Diseases 0.000 claims 1
- 201000008968 osteosarcoma Diseases 0.000 claims 1
- DWAFYCQODLXJNR-BNTLRKBRSA-L oxaliplatin Chemical compound O1C(=O)C(=O)O[Pt]11N[C@@H]2CCCC[C@H]2N1 DWAFYCQODLXJNR-BNTLRKBRSA-L 0.000 claims 1
- 229960001756 oxaliplatin Drugs 0.000 claims 1
- 229960000402 palivizumab Drugs 0.000 claims 1
- 229960001972 panitumumab Drugs 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 229960003171 plicamycin Drugs 0.000 claims 1
- 238000001959 radiotherapy Methods 0.000 claims 1
- 229960003876 ranibizumab Drugs 0.000 claims 1
- 208000016691 refractory malignant neoplasm Diseases 0.000 claims 1
- 229960004641 rituximab Drugs 0.000 claims 1
- 201000000849 skin cancer Diseases 0.000 claims 1
- 229950007213 spartalizumab Drugs 0.000 claims 1
- 238000001356 surgical procedure Methods 0.000 claims 1
- 208000011580 syndromic disease Diseases 0.000 claims 1
- NRUKOCRGYNPUPR-QBPJDGROSA-N teniposide Chemical compound COC1=C(O)C(OC)=CC([C@@H]2C3=CC=4OCOC=4C=C3[C@@H](O[C@H]3[C@@H]([C@@H](O)[C@@H]4O[C@@H](OC[C@H]4O3)C=3SC=CC=3)O)[C@@H]3[C@@H]2C(OC3)=O)=C1 NRUKOCRGYNPUPR-QBPJDGROSA-N 0.000 claims 1
- 229960001278 teniposide Drugs 0.000 claims 1
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 claims 1
- 201000003120 testicular cancer Diseases 0.000 claims 1
- ZRKFYGHZFMAOKI-QMGMOQQFSA-N tgfbeta Chemical compound C([C@H](NC(=O)[C@H](C(C)C)NC(=O)CNC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CC(C)C)NC(=O)CNC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](N)CCSC)C(C)C)[C@@H](C)CC)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CC=1C=CC=CC=1)C(=O)N[C@@H](C)C(=O)N1[C@@H](CCC1)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](CC=1C=CC=CC=1)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(C)C)C(=O)N1[C@@H](CCC1)C(=O)N1[C@@H](CCC1)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(O)=O)C1=CC=C(O)C=C1 ZRKFYGHZFMAOKI-QMGMOQQFSA-N 0.000 claims 1
- 238000002560 therapeutic procedure Methods 0.000 claims 1
- 125000000335 thiazolyl group Chemical group 0.000 claims 1
- 201000002510 thyroid cancer Diseases 0.000 claims 1
- 239000003053 toxin Substances 0.000 claims 1
- 231100000765 toxin Toxicity 0.000 claims 1
- 229960000575 trastuzumab Drugs 0.000 claims 1
- 238000011282 treatment Methods 0.000 claims 1
- 229960004824 triptorelin Drugs 0.000 claims 1
- VXKHXGOKWPXYNA-PGBVPBMZSA-N triptorelin Chemical compound C([C@@H](C(=O)N[C@H](CC=1C2=CC=CC=C2NC=1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N1[C@@H](CCC1)C(=O)NCC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@H](CC=1C2=CC=CC=C2NC=1)NC(=O)[C@H](CC=1N=CNC=1)NC(=O)[C@H]1NC(=O)CC1)C1=CC=C(O)C=C1 VXKHXGOKWPXYNA-PGBVPBMZSA-N 0.000 claims 1
- 229950010095 ulocuplumab Drugs 0.000 claims 1
- 229950005972 urelumab Drugs 0.000 claims 1
- 201000005112 urinary bladder cancer Diseases 0.000 claims 1
- 206010046766 uterine cancer Diseases 0.000 claims 1
- 206010046885 vaginal cancer Diseases 0.000 claims 1
- 208000013139 vaginal neoplasm Diseases 0.000 claims 1
- 229960000653 valrubicin Drugs 0.000 claims 1
- ZOCKGBMQLCSHFP-KQRAQHLDSA-N valrubicin Chemical compound O([C@H]1C[C@](CC2=C(O)C=3C(=O)C4=CC=CC(OC)=C4C(=O)C=3C(O)=C21)(O)C(=O)COC(=O)CCCC)[C@H]1C[C@H](NC(=O)C(F)(F)F)[C@H](O)[C@H](C)O1 ZOCKGBMQLCSHFP-KQRAQHLDSA-N 0.000 claims 1
- 229950001067 varlilumab Drugs 0.000 claims 1
- 229960003048 vinblastine Drugs 0.000 claims 1
- JXLYSJRDGCGARV-XQKSVPLYSA-N vincaleukoblastine Chemical compound C([C@@H](C[C@]1(C(=O)OC)C=2C(=CC3=C([C@]45[C@H]([C@@]([C@H](OC(C)=O)[C@]6(CC)C=CCN([C@H]56)CC4)(O)C(=O)OC)N3C)C=2)OC)C[C@@](C2)(O)CC)N2CCC2=C1NC1=CC=CC=C21 JXLYSJRDGCGARV-XQKSVPLYSA-N 0.000 claims 1
- 229960004528 vincristine Drugs 0.000 claims 1
- OGWKCGZFUXNPDA-XQKSVPLYSA-N vincristine Chemical compound C([N@]1C[C@@H](C[C@]2(C(=O)OC)C=3C(=CC4=C([C@]56[C@H]([C@@]([C@H](OC(C)=O)[C@]7(CC)C=CCN([C@H]67)CC5)(O)C(=O)OC)N4C=O)C=3)OC)C[C@@](C1)(O)CC)CC1=C2NC2=CC=CC=C12 OGWKCGZFUXNPDA-XQKSVPLYSA-N 0.000 claims 1
- OGWKCGZFUXNPDA-UHFFFAOYSA-N vincristine Natural products C1C(CC)(O)CC(CC2(C(=O)OC)C=3C(=CC4=C(C56C(C(C(OC(C)=O)C7(CC)C=CCN(C67)CC5)(O)C(=O)OC)N4C=O)C=3)OC)CN1CCC1=C2NC2=CC=CC=C12 OGWKCGZFUXNPDA-UHFFFAOYSA-N 0.000 claims 1
- GBABOYUKABKIAF-GHYRFKGUSA-N vinorelbine Chemical compound C1N(CC=2C3=CC=CC=C3NC=22)CC(CC)=C[C@H]1C[C@]2(C(=O)OC)C1=CC([C@]23[C@H]([C@]([C@H](OC(C)=O)[C@]4(CC)C=CCN([C@H]34)CC2)(O)C(=O)OC)N2C)=C2C=C1OC GBABOYUKABKIAF-GHYRFKGUSA-N 0.000 claims 1
- 229960002066 vinorelbine Drugs 0.000 claims 1
- 201000005102 vulva cancer Diseases 0.000 claims 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—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
- A61K31/4738—Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems
- A61K31/4745—Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems condensed with ring systems having nitrogen as a ring hetero atom, e.g. phenantrolines
-
- 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
- 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
- A61P35/00—Antineoplastic agents
-
- 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
Claims (22)
1. Spoj koje ima formulu (II):
[image]
ili njegova farmaceutski prihvatljiva sol, pri čemu:
R1 je nezavisno nesupstituirani C1-6 alkil, ili C(=O)Ra;
R2 je nezavisno H ili nesupstituirani C1-6 alkil;
R3 je:
(i) H;
(ii) nesupstituirani C1-2 alkil;
(iii) X-R8, pri čemu X je nerazgranati C1-6 alkilen, a R8 je -OH, C1-4 alkoksi, -C1-4 haloalkoksi, CO2Ra, ili -CONRcRd;
(iv) (C1-3 alkilen)-(C6-C10 aril), pri čemu aril je po izboru supstituirani sa od 1-3 supstituenta nezavisno odabrana od C1-6 alkila, C1-4 haloalkila, C1-4 alkoksi, i C1-4 haloalkoksi; ili
(v) (C1-3 alkilen)heteroaril koji uključuje od 5 do 6 atoma u prstenu, pri čemu od 1 do 4 atoma u prstenu su svaki nezavisno odabrani od N, N(Re), O, i S, i pri čemu heteroaril je po izboru supstituirani sa od 1 do 3 supstituenta nezavisno odabrana od C1-6 alkila, C1-4 haloalkila, C1-4 alkoksi, i C1-4 haloalkoksi;
R4 i R5 su svaki nezavisno odabrani od:
(i) H;
(ii) halo;
(iii) -(C0-3 alkilen)-C3-10 cikloalkila, pri čemu cikloalkil je po izboru supstituirani sa od 1 do 4 nezavisno odabrana Rf;
(iv) -(C0-3 alkilen)-heterociklila koji uključuje od 3 do 10 atoma u prstenu, pri čemu od 1 do 3 atoma u prstenu su svaki nezavisno odabrani od: N(Re), O, i S, pri čemu heterociklil je po izboru supstituirani sa od 1 do 4 Rf;
(v) -(C0-3 alkilen)-(C6-C10 arila) po izboru supstituisanog sa od 1 do 4 Rg;
(vi) -(C0-3 alkilen)-heteroarila koji uključuje od 5 do 10 atoma u prstenu, pri čemu od 1 do 4 atoma u prstenu su svaki nezavisno odabrani od: N, NH, O, i S, pri čemu heteroaril je po izboru supstituirani sa od 1 do 3 Rg;
(vii) C1-6 alkila po izboru supstituisanog sa od 1-2 nezavisno odabrana Rh; i
(viii) -(C0-3 alkilen)-C4-10 cikloalkenila, pri čemu cikloalkenil je po izboru supstituirani sa od 1 do 2 Rf;
Ra je:
(i) C1-6 alkil po izboru supstituirani sa od 1 do 2 Rh; ili
(ii) -(C0-3 alkilen)-C3-10 cikloalkil, pri čemu cikloalkil je po izboru supstituirani sa od 1 do 2 Rf;
(iii) -(C1-3 alkilen)-heterociklil koji uključuje od 3 do 10 atoma u prstenu, pri čemu od 1 do 3 atoma u prstenu su svaki nezavisno odabrani od N(Re), O, i S, pri čemu heterociklil je po izboru supstituirani sa od 1 do 4 nezavisno odabrana Rf;
(iv) -(C0-3 alkilen)-fenil po izboru supstituirani sa od 1 do 4 nezavisno odabrana Rg; ili
(v) -(C0-3 alkilen)-heteroaril koji uključuje od 5 do 10 atoma u prstenu, pri čemu od 1 do 4 atoma u prstenu su svaki nezavisno odabrani od N, N(Re), O, i S, pri čemu heteroaril je po izboru supstituirani sa od 1 do 3 nezavisno odabrana Rg;
pri svakom pojavljivanju Rc iRd je nezavisno H ili C1-4 alkil;
pri svakom pojavljivanju Re je nezavisno H ili C1-4 alkil;
pri svakom pojavljivanju Rf je nezavisno C1-6 alkil, C1-4 haloalkil, -OH, F, Cl, C1-4 alkoksi, C1-4 haloalkoksi, cijano, ili fenil po izboru supstituirani sa od 1 do 4 Rg;
pri svakom pojavljivanju Rg je nezavisno halo, cijano, C1-6 alkil, C1-4 haloalkil, C1-4 alkoksi, ili C1-4 haloalkoksi; i
pri svakom pojavljivanju Rh je nezavisno -OH, F, C1-4 alkoksi, C1-4 haloalkoksi, ili cijano.
2. Spoj prema patentnom zahtjevu 1, ili njegova farmaceutski prihvatljiva sol, pri čemu:
R3 je H, nesupstituirani C1-2 alkil, ili X-R8, pri čemu X je nerazgranati C2-6 alkilen, i R8 je CO2Ra, ili -CONRcRd;
R4 je nezavisno H ili halo;
R5 je nezavisno odabran od:
(i) H;
(ii) halo;
(iii) -(C0-3 alkilen)-C3-10 cikloalkila, pri čemu cikloalkil je po izboru supstituirani sa od 1 do 4 nezavisno odabrana Rf;
(iv) -(C0-3 alkilen)-heterociklila koji uključuje od 3 do 10 atoma u prstenu, pri čemu od 1 do 3 atoma u prstenu su svaki nezavisno odabrani od: N(Re), O, i S, pri čemu heterociklil je po izboru supstituirani sa od 1 do 4 Rf;
(v) -(C0-3 alkilen)-(C6-C10 arila) po izboru supstituisanog sa od 1 do 4 Rg;
(vi) -(C0-3 alkilen)-heteroarila koji uključuje od 5 do 10 atoma u prstenu, pri čemu od 1 do 4 atoma u prstenu su svaki nezavisno odabrani od: N, NH, O, i S, pri čemu heteroaril je po izboru supstituirani sa od 1 do 3 Rg;
(vii) C1-6 alkila po izboru supstituisanog sa od 1-2 nezavisno odabrana Rh; i
(viii) -(C0-3 alkilen)-C4-10 cikloalkenila, pri čemu cikloalkenil je po izboru supstituirani sa od 1 do 2 Rf.
3. Spoj prema bilo kojem od patentnih zahtjeva 1-2, ili njegova farmaceutski prihvatljiva sol, pri čemu:
R2 je nezavisno H ili nesupstituirani C1-3 alkil;
R3 je H, nesupstituirani C1-2 alkil, ili X-R8, pri čemu X je nerazgranati C2-4 alkilen, a R8 je CO2Ra, ili -CONRcRd;
R5 je nezavisno odabran od:
(i) C3-6 cikloalkila po izboru supstituisanog sa od 1 do 2 nezavisno odabrana Rf;
(ii) fenila po izboru supstituisanog sa od 1 do 3 Rg;
(iii) heteroarila koji uključuje od 5 do 6 atoma u prstenu, pri čemu od 1 do 3 atoma u prstenu su svaki nezavisno odabrani od: N, NH, O, i S, pri čemu heteroaril je po izboru supstituirani sa od 1 do 3 Rg;
(iv) C1-6 alkila po izboru supstituisanog sa od 1 do 2 nezavisno odabrana Rh; i
(v) C5-6 cikloalkenila po izboru supstituisanog sa od 1 do 2 Rf; i
Ra je H, C1-4 alkil po izboru supstituirani sa OH, C3-6 cikloalkil, fenil, ili heteroaril koji uključuje od 5 do 6 atoma u prstenu, pri čemu od 1 do 4 atoma u prstenu su svaki nezavisno odabrani od N, N(Re), O, i S.
4. Spoj prema bilo kojem od patentnih zahtjeva 1-3, pri čemu:
R2 je nezavisno H, CH3 ili CH2CH3;
R3 je H, CH3, ili -(CH2)3C(=O)OCH3;
R5 je nezavisno CH3, ciklopentil, ciklopentenil, fenil, pirazol-1-il, ili pirazol-3-il; i
Ra je H, CH3, CH2CH3, CH(CH3)2, C(CH3)3, ciklopropil, ili tiazolil.
5. Spoj prema bilo kojem od patentnih zahtjeva 1-4, ili njegova farmaceutski prihvatljiva sol, pri čemu:
R2 je nezavisno H, CH3 ili CH2CH3;
R3 je H ili CH3;
R5 je nezavisno CH3, ciklopentil, ciklopentenil, fenil, pirazol-1-il, ili pirazol-3-il; i
Ra je CH3, CH2CH3, CH(CH3)2, C(CH3)3, ili ciklopropil.
6. Spoj prema bilo kojem od patentnih zahtjeva 1-5, ili njegova farmaceutski prihvatljiva sol, pri čemu:
R1 je nezavisno CH3, CH2CH3, CH(CH3)2, C(CH3)3, ili C(=O)Ra;
R2 je nezavisno H, CH3 ili CH2CH3;
R3 je H;
R5 je nezavisno ciklopentil, ciklopentenil, fenil, pirazol-1-il, ili pirazol-3-il; i
Ra je CH3, CH2CH3, CH(CH3)2, C(CH3)3, ili ciklopropil.
7. Spoj prema patentnom zahtjevu 1, pri čemu spoj je
[image]
ili njegova farmaceutski prihvatljiva sol.
8. Spoj prema patentnom zahtjevu 1, pri čemu spoj je
[image]
9. Spoj prema patentnom zahtjevu 1, pri čemu spoj je
[image]
ili njegova farmaceutski prihvatljiva sol.
10. Spoj prema patentnom zahtjevu 1, pri čemu spoj je
[image]
11. Farmaceutska kompozicija koja sadrži spoj ili njegovu farmaceutski prihvatljivu sol prema bilo kojem od patentnih zahtjeva 1 do 10 i jedan ili više farmaceutski prihvatljivih ekscipijenasa.
12. Spoj ili njegova farmaceutski prihvatljiva sol u skladu sa bilo kojim od patentnih zahtjeva 1 do 10, ili farmaceutska kompozicija u skladu sa patentnim zahtjevom 11, za primjenu kao lijek.
13. Spoj ili njegova farmaceutski prihvatljiva sol u skladu sa bilo kojim od patentnih zahtjeva 1 do 10, ili farmaceutska kompozicija u skladu sa patentnim zahtjevom 11, za primjenu u liječenju raka kod subjekta.
14. Spoj, njegova farmaceutski prihvatljiva sol ili kompozicija za primjenu prema patentnom zahtjevu 13, pri čemu rak je odabran od akutne mijeloidne leukemija, adrenokortikalnog raka, Kaposijevog sarkoma, limfoma, analnog raka, raka apendiksa, teratoidnog/rabdoidnog tumora, raka bazalnih stanica, raka žučnih puteva, raka mjehura, raka kostiju, raka mozga, raka dojke, tumora bronhija, karcinoidnog tumora, kardijačnog tumora, raka grlića materice, hordoma, kronične limfocitne leukemije, kronične mijeloproliferativne neoplazme, raka kolona, kolorektalnog raka, kraniofaringioma, endometrijalnog raka, ependimoma, raka jednjaka, estezioneuroblastoma, Evingovog sindroma, raka oka, raka falopijevih cijevi, raka žučne vrećice, gastrointestinalnog karcinoidnog tumora, gastrointestinalnog stromalnog tumora, tumora germinativnih stanica, leukemije vlastastih stanica, raka glave i vrata, raka srca, raka jetre, hipofaringealnog raka, raka gušterače, raka bubrega, laringealnog raka, kronične mijeloične leukemije, raka usne i usne šupljine, raka pluća, melanoma, karcinoma Merkelovih stanica, mezotelioma, raka usta, oralnog raka, osteosarkoma, raka jajnika, raka penisa, faringealnog raka, raka prostate, rektalnog raka, raka žlijezda slinovnica, raka kože, raka tankog crijeva, sarkoma mekog tkiva, raka testisa, raka grla, raka štitnjače, raka uretre, raka maternice, raka vagine, i raka vulve.
15. Spoj, njegova farmaceutski prihvatljiva sol ili kompozicija za primjenu prema patentnom zahtjevu 13 ili patentnom zahtjevu 14, pri čemu rak je refraktorni rak.
16. Spoj, njegova farmaceutski prihvatljiva sol ili kompozicija za primjenu prema patentnom zahtjevu 13, pri čemu rak je odabran od raka dojke, raka kolona, rektalnog raka, kolorektalnog raka, raka gušterača, i raka prostate.
17. Spoj, njegova farmaceutski prihvatljiva sol ili kompozicija za primjenu prema bilo kojem od patentnih zahtjeva 13-16, pri čemu spoj ili kompozicija se administrira u kombinaciji sa jednom ili više dodatnih terapija protiv raka.
18. Spoj, njegova farmaceutski prihvatljiva sol ili kompozicija za primjenu prema patentnom zahtjevu 17, pri čemu jedna ili više dodatnih terapija protiv raka sadrži kirurgiju, radioterapiju, kemoterapiju, terapiju toksinima, imunoterapiju, krioterapiju ili gensku terapiju, ili kombinaciju istih.
19. Spoj, njegova farmaceutski prihvatljiva sol ili kompozicija za primjenu prema patentnom zahtjevu 17, pri čemu dodatna terapija protiv raka sadrži jedan ili više agenasa odabrana od cisplatina, karboplatina, mehloretamina, ciklofosfamida, klorambucila, ifosfamida, oksaliplatina, azatioprina, merkaptopurina, vinkristina, vinblastina, vinorelbina, vindesina, taksola, paklitaksela, docetaksela, irinotekana, amsakrina, etopozida, etopozid fosfata, tenipozida, aktinomicina, antraciklina, doksorubicina, daunorubicina, valrubicina, idarubicina, epirubicina, bleomicina, plikamicina, mitomicina, leuprolidina, goserelina, triptorelina, histrelina, bikalutamida, flutamida, nilutamida, abciksimaba, adalimumaba, alemtuzumaba, atlizumaba, baziliksimaba, belimumaba, bevacizumaba, brentuksimab vedotina, kanakinumaba, cetuksimaba, certolizumab pegola, daklizumaba, denozumaba, ekulizumaba, efalizumaba, gemtuzumaba, golimumaba, ibritumomab tiuksetana, infliksimaba, ipilimumaba, muromonab-CD3, natalizumaba, ofatumumaba, omalizumaba, palivizumaba, panitumumaba, ranibizumaba, rituksimaba, tocilizumaba, tozitumomaba, trastuzumaba, interleukina-2, indolamin 2,3-dioksigenaze, IL-10, transformirajućeg faktora rasta-β, CD39, CD73 adenozin-CD39-CD73, i CXCR4-CXCL12.
20. Spoj, njegova farmaceutski prihvatljiva sol ili kompozicija za primjenu prema patentnom zahtjevu 17, pri čemu dodatna terapija protiv raka sadrži jedan ili više agenasa odabrana od urelumaba, PF-05082566, MEDI6469, TRX518, varlilumaba, CP-870893, pembrolizumaba, nivolumaba, atezolizumaba, MEDI4736, avelumaba, PDR001, BMS-986016, MGA271, lirilumaba, IPH2201, emaktuzumaba, INCB024360, galunisertiba, ulokuplumaba, BKT140, bavituksimaba, CC-90002, bevacizumaba, i MNRP1685A.
21. Spoj, njegova farmaceutski prihvatljiva sol ili kompozicija za primjenu prema patentnom zahtjevu 17, pri čemu dodatna terapija protiv raka sadrži jedan ili više agenasa odabrana od nivolumaba, ipilimumaba, pembrolizumaba, atezolizumaba, i avelumaba.
22. Spoj, njegova farmaceutski prihvatljiva sol ili kompozicija za primjenu prema bilo kojem od patentnih zahtjeva 12-20 pri čemu spoj se administrira intratumoralno ili sustavno.
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| WO2017132827A1 (en) | 2016-02-02 | 2017-08-10 | Innovent Biologics (Suzhou) Co., Ltd. | Pd-1 antibodies |
| CN111491362B (zh) | 2016-02-02 | 2023-10-24 | 华为技术有限公司 | 确定发射功率的方法、用户设备和基站 |
| US10533007B2 (en) | 2016-04-19 | 2020-01-14 | Innate Tumor Immunity, Inc. | NLRP3 modulators |
| AU2017252640A1 (en) | 2016-04-19 | 2018-12-06 | Innate Tumor Immunity, Inc. | NLRP3 modulators |
| TWI674261B (zh) | 2017-02-17 | 2019-10-11 | 美商英能腫瘤免疫股份有限公司 | Nlrp3 調節劑 |
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2018
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