HRP20241518T1 - Spojevi koji moduliraju diacilglicerinkinazu - Google Patents
Spojevi koji moduliraju diacilglicerinkinazu Download PDFInfo
- Publication number
- HRP20241518T1 HRP20241518T1 HRP20241518TT HRP20241518T HRP20241518T1 HR P20241518 T1 HRP20241518 T1 HR P20241518T1 HR P20241518T T HRP20241518T T HR P20241518TT HR P20241518 T HRP20241518 T HR P20241518T HR P20241518 T1 HRP20241518 T1 HR P20241518T1
- Authority
- HR
- Croatia
- Prior art keywords
- image
- alkyl
- independently
- cycloalkyl
- heterocycloalkyl
- Prior art date
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- 150000001875 compounds Chemical class 0.000 title claims 21
- 102000011107 Diacylglycerol Kinase Human genes 0.000 title 1
- 108010062677 Diacylglycerol Kinase Proteins 0.000 title 1
- 229910052739 hydrogen Inorganic materials 0.000 claims 100
- 239000001257 hydrogen Substances 0.000 claims 100
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 97
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 80
- 125000003118 aryl group Chemical group 0.000 claims 79
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims 77
- 229910052736 halogen Inorganic materials 0.000 claims 69
- 150000002367 halogens Chemical group 0.000 claims 69
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 claims 66
- 125000004183 alkoxy alkyl group Chemical group 0.000 claims 65
- 125000004093 cyano group Chemical group *C#N 0.000 claims 53
- 125000001072 heteroaryl group Chemical group 0.000 claims 53
- 125000006577 C1-C6 hydroxyalkyl group Chemical group 0.000 claims 46
- 125000006376 (C3-C10) cycloalkyl group Chemical group 0.000 claims 40
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims 38
- 125000005842 heteroatom Chemical group 0.000 claims 35
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 claims 33
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 claims 31
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 29
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 26
- 229910052760 oxygen Inorganic materials 0.000 claims 26
- 125000004737 (C1-C6) haloalkoxy group Chemical group 0.000 claims 24
- 125000004103 aminoalkyl group Chemical group 0.000 claims 21
- 125000000217 alkyl group Chemical group 0.000 claims 19
- 125000000753 cycloalkyl group Chemical group 0.000 claims 19
- -1 -NO Chemical group 0.000 claims 18
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 18
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 17
- 229910052717 sulfur Inorganic materials 0.000 claims 17
- 239000003814 drug Substances 0.000 claims 16
- 229940124597 therapeutic agent Drugs 0.000 claims 16
- 125000006583 (C1-C3) haloalkyl group Chemical group 0.000 claims 14
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims 13
- 150000003839 salts Chemical class 0.000 claims 13
- 125000000304 alkynyl group Chemical group 0.000 claims 12
- 229910052731 fluorine Inorganic materials 0.000 claims 12
- 125000004429 atom Chemical group 0.000 claims 11
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 claims 10
- 125000002768 hydroxyalkyl group Chemical group 0.000 claims 10
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims 8
- JNCMHMUGTWEVOZ-UHFFFAOYSA-N F[CH]F Chemical compound F[CH]F JNCMHMUGTWEVOZ-UHFFFAOYSA-N 0.000 claims 8
- 108010081348 HRT1 protein Hairy Proteins 0.000 claims 8
- 102100021881 Hairy/enhancer-of-split related with YRPW motif protein 1 Human genes 0.000 claims 8
- 125000003342 alkenyl group Chemical group 0.000 claims 8
- 229910052801 chlorine Inorganic materials 0.000 claims 8
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 8
- 125000006274 (C1-C3)alkoxy group Chemical group 0.000 claims 7
- 125000000041 C6-C10 aryl group Chemical group 0.000 claims 7
- 125000001160 methoxycarbonyl group Chemical group [H]C([H])([H])OC(*)=O 0.000 claims 7
- 125000006720 (C1-C6) alkyl (C6-C10) aryl group Chemical group 0.000 claims 6
- 229910052794 bromium Inorganic materials 0.000 claims 6
- 125000004438 haloalkoxy group Chemical group 0.000 claims 6
- 125000004170 methylsulfonyl group Chemical group [H]C([H])([H])S(*)(=O)=O 0.000 claims 6
- 229960003301 nivolumab Drugs 0.000 claims 6
- 229960002621 pembrolizumab Drugs 0.000 claims 6
- 238000002560 therapeutic procedure Methods 0.000 claims 6
- 125000006593 (C2-C3) alkynyl group Chemical group 0.000 claims 5
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims 5
- 206010028980 Neoplasm Diseases 0.000 claims 5
- 229960003852 atezolizumab Drugs 0.000 claims 5
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 5
- 125000006592 (C2-C3) alkenyl group Chemical group 0.000 claims 4
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 4
- AOJJSUZBOXZQNB-TZSSRYMLSA-N Doxorubicin Chemical compound O([C@H]1C[C@@](O)(CC=2C(O)=C3C(=O)C=4C=CC=C(C=4C(=O)C3=C(O)C=21)OC)C(=O)CO)[C@H]1C[C@H](N)[C@H](O)[C@H](C)O1 AOJJSUZBOXZQNB-TZSSRYMLSA-N 0.000 claims 4
- 210000001744 T-lymphocyte Anatomy 0.000 claims 4
- 125000003545 alkoxy group Chemical group 0.000 claims 4
- 201000011510 cancer Diseases 0.000 claims 4
- 210000004027 cell Anatomy 0.000 claims 4
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 4
- 125000002147 dimethylamino group Chemical group [H]C([H])([H])N(*)C([H])([H])[H] 0.000 claims 4
- 229960005386 ipilimumab Drugs 0.000 claims 4
- 238000000034 method Methods 0.000 claims 4
- 239000008194 pharmaceutical composition Substances 0.000 claims 4
- 125000004206 2,2,2-trifluoroethyl group Chemical group [H]C([H])(*)C(F)(F)F 0.000 claims 3
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 3
- 206010035226 Plasma cell myeloma Diseases 0.000 claims 3
- 125000005037 alkyl phenyl group Chemical group 0.000 claims 3
- 239000000427 antigen Substances 0.000 claims 3
- 102000036639 antigens Human genes 0.000 claims 3
- 108091007433 antigens Proteins 0.000 claims 3
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 claims 3
- 125000006222 dimethylaminomethyl group Chemical group [H]C([H])([H])N(C([H])([H])[H])C([H])([H])* 0.000 claims 3
- VUWZPRWSIVNGKG-UHFFFAOYSA-N fluoromethane Chemical compound F[CH2] VUWZPRWSIVNGKG-UHFFFAOYSA-N 0.000 claims 3
- 125000004213 tert-butoxy group Chemical group [H]C([H])([H])C(O*)(C([H])([H])[H])C([H])([H])[H] 0.000 claims 3
- 125000000876 trifluoromethoxy group Chemical group FC(F)(F)O* 0.000 claims 3
- 229960005486 vaccine Drugs 0.000 claims 3
- 125000006582 (C5-C6) heterocycloalkyl group Chemical group 0.000 claims 2
- 208000032791 BCR-ABL1 positive chronic myelogenous leukemia Diseases 0.000 claims 2
- 125000001313 C5-C10 heteroaryl group Chemical group 0.000 claims 2
- 108010019670 Chimeric Antigen Receptors Proteins 0.000 claims 2
- 208000010833 Chronic myeloid leukaemia Diseases 0.000 claims 2
- 206010009944 Colon cancer Diseases 0.000 claims 2
- 208000031671 Large B-Cell Diffuse Lymphoma Diseases 0.000 claims 2
- 208000025205 Mantle-Cell Lymphoma Diseases 0.000 claims 2
- 201000003793 Myelodysplastic syndrome Diseases 0.000 claims 2
- 208000033761 Myelogenous Chronic BCR-ABL Positive Leukemia Diseases 0.000 claims 2
- 208000014767 Myeloproliferative disease Diseases 0.000 claims 2
- 208000015914 Non-Hodgkin lymphomas Diseases 0.000 claims 2
- 239000012269 PD-1/PD-L1 inhibitor Substances 0.000 claims 2
- 229910006074 SO2NH2 Inorganic materials 0.000 claims 2
- 208000036142 Viral infection Diseases 0.000 claims 2
- 208000033559 Waldenström macroglobulinemia Diseases 0.000 claims 2
- 125000004397 aminosulfonyl group Chemical group NS(=O)(=O)* 0.000 claims 2
- 229940034982 antineoplastic agent Drugs 0.000 claims 2
- 239000002246 antineoplastic agent Substances 0.000 claims 2
- 201000007455 central nervous system cancer Diseases 0.000 claims 2
- 238000002512 chemotherapy Methods 0.000 claims 2
- 210000004405 cytokine-induced killer cell Anatomy 0.000 claims 2
- 210000004443 dendritic cell Anatomy 0.000 claims 2
- 206010012818 diffuse large B-cell lymphoma Diseases 0.000 claims 2
- 229960004679 doxorubicin Drugs 0.000 claims 2
- 229960005277 gemcitabine Drugs 0.000 claims 2
- SDUQYLNIPVEERB-QPPQHZFASA-N gemcitabine Chemical compound O=C1N=C(N)C=CN1[C@H]1C(F)(F)[C@H](O)[C@@H](CO)O1 SDUQYLNIPVEERB-QPPQHZFASA-N 0.000 claims 2
- 210000002865 immune cell Anatomy 0.000 claims 2
- 238000009169 immunotherapy Methods 0.000 claims 2
- 229910052740 iodine Inorganic materials 0.000 claims 2
- 210000002540 macrophage Anatomy 0.000 claims 2
- 125000006533 methyl amino methyl group Chemical group [H]N(C([H])([H])[H])C([H])([H])* 0.000 claims 2
- 201000000050 myeloid neoplasm Diseases 0.000 claims 2
- 229940121653 pd-1/pd-l1 inhibitor Drugs 0.000 claims 2
- 125000004076 pyridyl group Chemical group 0.000 claims 2
- 125000000714 pyrimidinyl group Chemical group 0.000 claims 2
- 238000001959 radiotherapy Methods 0.000 claims 2
- 238000002271 resection Methods 0.000 claims 2
- 229960004641 rituximab Drugs 0.000 claims 2
- 230000008685 targeting Effects 0.000 claims 2
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 claims 2
- 125000000335 thiazolyl group Chemical group 0.000 claims 2
- 125000001544 thienyl group Chemical group 0.000 claims 2
- 125000001889 triflyl group Chemical group FC(F)(F)S(*)(=O)=O 0.000 claims 2
- 210000003171 tumor-infiltrating lymphocyte Anatomy 0.000 claims 2
- 230000009385 viral infection Effects 0.000 claims 2
- 125000006700 (C1-C6) alkylthio group Chemical group 0.000 claims 1
- 208000024893 Acute lymphoblastic leukemia Diseases 0.000 claims 1
- 208000031261 Acute myeloid leukaemia Diseases 0.000 claims 1
- 208000010839 B-cell chronic lymphocytic leukemia Diseases 0.000 claims 1
- 208000003950 B-cell lymphoma Diseases 0.000 claims 1
- 206010005003 Bladder cancer Diseases 0.000 claims 1
- 206010005949 Bone cancer Diseases 0.000 claims 1
- 208000018084 Bone neoplasm Diseases 0.000 claims 1
- 208000003174 Brain Neoplasms Diseases 0.000 claims 1
- 206010006187 Breast cancer Diseases 0.000 claims 1
- 208000026310 Breast neoplasm Diseases 0.000 claims 1
- 206010008342 Cervix carcinoma Diseases 0.000 claims 1
- 102000019034 Chemokines Human genes 0.000 claims 1
- 108010012236 Chemokines Proteins 0.000 claims 1
- 208000001333 Colorectal Neoplasms Diseases 0.000 claims 1
- 102000004127 Cytokines Human genes 0.000 claims 1
- 108090000695 Cytokines Proteins 0.000 claims 1
- 208000000461 Esophageal Neoplasms Diseases 0.000 claims 1
- 101000917858 Homo sapiens Low affinity immunoglobulin gamma Fc region receptor III-A Proteins 0.000 claims 1
- 101000917839 Homo sapiens Low affinity immunoglobulin gamma Fc region receptor III-B Proteins 0.000 claims 1
- 108060003951 Immunoglobulin Proteins 0.000 claims 1
- 208000008839 Kidney Neoplasms Diseases 0.000 claims 1
- 102100029185 Low affinity immunoglobulin gamma Fc region receptor III-B Human genes 0.000 claims 1
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims 1
- 206010025323 Lymphomas Diseases 0.000 claims 1
- 206010027476 Metastases Diseases 0.000 claims 1
- 208000034578 Multiple myelomas Diseases 0.000 claims 1
- 229910017849 NH2—NH2 Inorganic materials 0.000 claims 1
- 206010030155 Oesophageal carcinoma Diseases 0.000 claims 1
- 206010033128 Ovarian cancer Diseases 0.000 claims 1
- 206010061535 Ovarian neoplasm Diseases 0.000 claims 1
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims 1
- 206010060862 Prostate cancer Diseases 0.000 claims 1
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims 1
- 206010038389 Renal cancer Diseases 0.000 claims 1
- 206010039491 Sarcoma Diseases 0.000 claims 1
- 206010041067 Small cell lung cancer Diseases 0.000 claims 1
- 208000021712 Soft tissue sarcoma Diseases 0.000 claims 1
- 208000005718 Stomach Neoplasms Diseases 0.000 claims 1
- 206010042971 T-cell lymphoma Diseases 0.000 claims 1
- 208000027585 T-cell non-Hodgkin lymphoma Diseases 0.000 claims 1
- 208000007097 Urinary Bladder Neoplasms Diseases 0.000 claims 1
- 208000006105 Uterine Cervical Neoplasms Diseases 0.000 claims 1
- 125000005213 alkyl heteroaryl group Chemical group 0.000 claims 1
- 230000000735 allogeneic effect Effects 0.000 claims 1
- MDFFNEOEWAXZRQ-UHFFFAOYSA-N aminyl Chemical compound [NH2] MDFFNEOEWAXZRQ-UHFFFAOYSA-N 0.000 claims 1
- 239000000611 antibody drug conjugate Substances 0.000 claims 1
- 229940049595 antibody-drug conjugate Drugs 0.000 claims 1
- 238000002659 cell therapy Methods 0.000 claims 1
- 201000010881 cervical cancer Diseases 0.000 claims 1
- 238000011260 co-administration Methods 0.000 claims 1
- 208000029742 colonic neoplasm Diseases 0.000 claims 1
- 125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 claims 1
- 125000004987 dibenzofuryl group Chemical group C1(=CC=CC=2OC3=C(C21)C=CC=C3)* 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 201000004101 esophageal cancer Diseases 0.000 claims 1
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 1
- 201000003444 follicular lymphoma Diseases 0.000 claims 1
- 239000012634 fragment Substances 0.000 claims 1
- 206010017758 gastric cancer Diseases 0.000 claims 1
- 238000001415 gene therapy Methods 0.000 claims 1
- 201000010536 head and neck cancer Diseases 0.000 claims 1
- 208000014829 head and neck neoplasm Diseases 0.000 claims 1
- 208000002672 hepatitis B Diseases 0.000 claims 1
- 206010073071 hepatocellular carcinoma Diseases 0.000 claims 1
- CBOIHMRHGLHBPB-UHFFFAOYSA-N hydroxymethyl Chemical compound O[CH2] CBOIHMRHGLHBPB-UHFFFAOYSA-N 0.000 claims 1
- 102000018358 immunoglobulin Human genes 0.000 claims 1
- 230000003308 immunostimulating effect Effects 0.000 claims 1
- 230000002401 inhibitory effect Effects 0.000 claims 1
- 125000001786 isothiazolyl group Chemical group 0.000 claims 1
- 125000000842 isoxazolyl group Chemical group 0.000 claims 1
- 201000010982 kidney 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
- 210000004698 lymphocyte Anatomy 0.000 claims 1
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims 1
- 201000001441 melanoma Diseases 0.000 claims 1
- 230000009401 metastasis Effects 0.000 claims 1
- 125000006525 methoxy ethyl amino group Chemical group [H]N(*)C([H])([H])C([H])([H])OC([H])([H])[H] 0.000 claims 1
- 125000006261 methyl amino sulfonyl group Chemical group [H]N(C([H])([H])[H])S(*)(=O)=O 0.000 claims 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 1
- 125000000250 methylamino group Chemical group [H]N(*)C([H])([H])[H] 0.000 claims 1
- 125000001624 naphthyl group Chemical group 0.000 claims 1
- 201000002120 neuroendocrine carcinoma Diseases 0.000 claims 1
- 208000002154 non-small cell lung carcinoma Diseases 0.000 claims 1
- 125000002971 oxazolyl group Chemical group 0.000 claims 1
- 201000002528 pancreatic cancer Diseases 0.000 claims 1
- 208000008443 pancreatic carcinoma Diseases 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 102000004169 proteins and genes Human genes 0.000 claims 1
- 108090000623 proteins and genes Proteins 0.000 claims 1
- 125000003373 pyrazinyl group Chemical group 0.000 claims 1
- 125000003226 pyrazolyl group Chemical group 0.000 claims 1
- 125000000168 pyrrolyl group Chemical group 0.000 claims 1
- 210000003289 regulatory T cell Anatomy 0.000 claims 1
- 208000000587 small cell lung carcinoma Diseases 0.000 claims 1
- 201000011549 stomach cancer Diseases 0.000 claims 1
- 208000029729 tumor suppressor gene on chromosome 11 Diseases 0.000 claims 1
- 201000005112 urinary bladder cancer Diseases 0.000 claims 1
- 125000000391 vinyl group Chemical group [H]C([*])=C([H])[H] 0.000 claims 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/535—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
- A61K31/538—1,4-Oxazines, e.g. morpholine ortho- or peri-condensed with carbocyclic ring 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
- A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
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- 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
- A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
- A61K31/553—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and one oxygen as ring hetero atoms, e.g. loxapine, staurosporine
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- A—HUMAN NECESSITIES
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- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/5545—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having eight-membered rings not containing additional condensed or non-condensed nitrogen-containing 3-7 membered rings
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- A—HUMAN NECESSITIES
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- A61K31/695—Silicon compounds
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- 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
- A61K31/70—Carbohydrates; Sugars; Derivatives thereof
- A61K31/7028—Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages
- A61K31/7034—Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin
- A61K31/704—Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin attached to a condensed carbocyclic ring system, e.g. sennosides, thiocolchicosides, escin, daunorubicin
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- A—HUMAN NECESSITIES
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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/70—Carbohydrates; Sugars; Derivatives thereof
- A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
- A61K31/7052—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
- A61K31/706—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom
- A61K31/7064—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines
- A61K31/7068—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid
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- A—HUMAN NECESSITIES
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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K35/00—Medicinal preparations containing materials or reaction products thereof with undetermined constitution
- A61K35/12—Materials from mammals; Compositions comprising non-specified tissues or cells; Compositions comprising non-embryonic stem cells; Genetically modified cells
- A61K35/14—Blood; Artificial blood
- A61K35/15—Cells of the myeloid line, e.g. granulocytes, basophils, eosinophils, neutrophils, leucocytes, monocytes, macrophages or mast cells; Myeloid precursor cells; Antigen-presenting cells, e.g. dendritic cells
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- A—HUMAN NECESSITIES
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- A61K35/12—Materials from mammals; Compositions comprising non-specified tissues or cells; Compositions comprising non-embryonic stem cells; Genetically modified cells
- A61K35/14—Blood; Artificial blood
- A61K35/17—Lymphocytes; B-cells; T-cells; Natural killer cells; Interferon-activated or cytokine-activated lymphocytes
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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- A61K39/395—Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum
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Claims (14)
1. Spoj, naznačen time, da je predstavljen Formulom (I):
[image]
ili njegova farmaceutski prihvatljiva sol, gdje
R1 je vodik, C1-6 alkil, C2-6 alkenil, C2-6 alkinil, C1-6 alkoksi, halogen, C1-6 haloalkil, C1-6 haloalkoksi, ili -CN;
R2 je vodik, C1-6 alkil, C2-6 alkenil, C2-6 alkinil, C1-6 hidroksialkil, C1-6 aminoalkil, C1-6 alkoksi, C2-6 alkoksialkil, halogen, C1-6 haloalkil, C1-6 haloalkoksi, -CN, -NO, -NO2, -C(O)R2a, -C(O)OR2a, -OC(O)R2a, -C(O)N(R2a)(R2b), -N(R2a)C(O)R2b, -OC(O)N(R2a)(R2b), -N(R2a)C(O)OR2b, -C(=NR2a)N(R2b)(R2c), -N(R2a)(R2b), -N(R2a)N(R2b)(R2c), -N(R2a)N=C(R2b)(OR2c), -OR2a, -SR2a, -S(O)R2a, -S(O)(NR2a)(R2b), -S(NR2a)(NR2b)(R2c), -S(O)2R2a, -S(O)2N(R2a)(R2b), -N(R2a)S(O)2(R2b), -P(R2a)(R2b), -P(O)(R2a)(R2b), -P(O)(OR2a)(R2b), -P(O)(OR2a)(OR2b), C3-10 cikloalkil, C1-6 alkil-C3-10 cikloalkil, C6-12 aril, C1-6 alkil-C6-12 aril, heterocikloalkil, C1-6 alkil-(heterocikloalkil), heteroaril, ili C1-6 alkil-(heteroaril), pri čemu je svaki alkil, alkenil ili alkinil neovisno opcionalno supstituiran s 1 do 3 skupine R2d, svaki cikloalkil je opcionalno supstituiran s 1 do 3 skupine R2e, svaki aril je opcionalno supstituiran s 1 do 3 skupine R2f, svaki heterocikloalkil je opcionalno supstituiran s 1 do 3 skupine R2g, i svaki heteroaril je opcionalno supstituiran s 1 do 3 skupine R2h;
svaki od R2a, R2b, i R2c je neovisno vodik, C1-6 alkil, C2-6 alkenil, C2-6 alkinil, C1-6 hidroksialkil, C1-6 aminoalkil, C2-6 alkoksialkil, C1-6 haloalkil, C3-10 cikloalkil, C1-6 alkil-C3-10 cikloalkil, C6-12 aril, C1-6 alkil-C6-12 aril, heterocikloalkil, C1-6 alkil-(heterocikloalkil), heteroaril, ili C1-6 alkil-(heteroaril), pri čemu je svaki aril ili heteroaril opcionalno supstituiran s 1 do 3 R2j;
alternativno, R2a, R2b, i R2c kada su vezani na isti atom, mogu se kombinirati s atomom s kojim su vezani, za tvorbu heterocikloalkila;
svaki R2d je neovisno -CN, -C(O)R2d1, -C(O)OR2d1, -OC(O)R2d1, -C(O)N(R2d1)(R2d2), -N(R2d1)C(O)R2d2, -OC(O)N(R2d1)(R2d2), -N(R2d1)C(O)OR2d2, -N(R2d1)(R2d2), =O, -OR2d1, -SR2d1, -S(O)R2d1, -S(O)(NR2d1)(R2d2), -S(O)2R2d1, -S(O)N(R2d1)(R2d2), -N(R2d1)S(O)2R2d2, C3-10 cikloalkil, C1-6 alkil-C3-10 cikloalkil, C6-12 aril, C1-6 alkil-C6-12 aril, heterocikloalkil, C1-6 alkil-(heterocikloalkil), heteroaril, ili C1-C6 alkil-(heteroaril);
svaki od R2d1 i R2d1 je neovisno vodik, C1-6 alkil, C1-6 hidroksialkil, C1-6 aminoalkil, C2-6 alkoksialkil, ili C1-6 haloalkil;
svaki od R2e, R2f, R2g, i R2h je neovisno vodik, C1-6 alkil, C1-6 hidroksialkil, C1-6 aminoalkil, C1-6 alkoksi, C2-6 alkoksialkil, halogen, C1-6 haloalkil, C1-6 haloalkoksi, -CN, ili -OH;
svaki R2j je neovisno C1-6 alkil, C1-6 hidroksialkil, C1-6 aminoalkil, C1-6 alkoksi, C2-6 alkoksialkil, halogen, C1-6 haloalkil, ili C1-6 haloalkoksi;
R3 je vodik, C1-6 alkil, C2-6 alkenil, C2-6 alkinil, C1-6 hidroksialkil, C1-6 aminoalkil, C1-6 alkoksi, C2-6 alkoksialkil, halogen, C1-6 haloalkil, C1-6 haloalkoksi, -CN, -NO, -NO2, -C(O)R3a, -C(O)OR3a, -OC(O)R3a, -C(O)N(R3a)(R3b), -N(R3a)C(O)R3b, -OC(O)N(R3a)(R3b), -N(R3a)C(O)OR3b, -C(=NR3a)N(R3b)(R3c), -N(R3a)(R3b), -N(R3a)N(R3b)(R3c), -N(R3a)N=C(R3b)(OR3c), -OR3a, -SR3a, -S(O)R3a, -S(O)(NR3a)(R3b), -S(NR3a)(NR3b)(R3c), -S(O)2R3a, -S(O)2N(R3a)(R3b), -N(R3a)S(O)2(R3b), -P(R3a)(R3b), -P(O)(R3a)(R3b), -P(O)(OR3a)(R3b), -P(O)(OR3a)(OR3b), C3-10 cikloalkil, C1-6 alkil-C3-10 cikloalkil, C6-12 aril, C1-6 alkil-C6-12 aril, heterocikloalkil, C1-6 alkil-(heterocikloalkil), heteroaril, ili C1-6 alkil-(heteroaril), pri čemu je svaki alkenil ili alkinil neovisno opcionalno supstituiran s 1 do 3 skupine R3d, svaki cikloalkil je opcionalno supstituiran s 1 do 3 skupine R3e, svaki aril je opcionalno supstituiran s 1 do 3 skupine R3f, svaki heterocikloalkil je opcionalno supstituiran s 1 do 3 skupine R3g, i svaki heteroaril je opcionalno supstituiran s 1 do 3 skupine R3b;
svaki od R3a, R3b, i R3c je neovisno vodik, C1-6 alkil, C1-6 hidroksialkil, C2-6 alkoksialkil, C1-6 haloalkil, C3-10 cikloalkil, C1-6 alkil-C3-10 cikloalkil, C6-12 aril, C1-6 alkil-C6-12 aril, heterocikloalkil, ili heteroaril;
alternativno, R3a, R3b, i R3c kada su vezani na isti atom, mogu se kombinirati s atomom s kojim su vezani, za tvorbu heterocikloalkila;
svaki R3d je neovisno -N(R3d1)(R3d2), -OR3d1, C3-10 cikloalkil, C1-6 alkil-C3-10 cikloalkil, C6-12 aril, C1-6 alkil-C6-12 aril, heterocikloalkil, ili heteroaril;
svaki od R3d1 i R3d1 je neovisno vodik, C1-6 alkil, ili -C(O)O-(C1-6 alkil);
svaki od R3e, R3f, R3g, i R3h je neovisno vodik, C1-6 alkil, C1-6 alkoksi, halogen, C1-6 haloalkil, ili C1-6 haloalkoksi;
R4 je vodik, C1-6 alkil, C2-6 alkenil, C2-6 alkinil, C1-6 alkoksi, halogen, C1-6 haloalkil, C1-6 haloalkoksi, ili -CN;
R5 je vodik, C1-6 alkil, C2-6 alkenil, C2-6 alkinil, C1-6 hidroksialkil, C2-6 alkoksialkil, C1-6 haloalkil, C3-10 cikloalkil, C1-6 alkil-C3-10 cikloalkil, C6-12 aril, C1-6 alkil-C6-12 aril, heterocikloalkil, C1-6 alkil-(heterocikloalkil), heteroaril, ili C1-6 alkil-(heteroaril), pri čemu je alkil opcionalno supstituiran s R5a;
R5a je -OSi(R5a1)(R5a2)(R5a3);
svaki od R5a1, R5a2 i R5a3 je neovisno C1-6 alkil; i
R6 je C1-6 alkil, C2-6 alkenil, C2-6 alkinil, C1-6 haloalkil, C6-12 aril, ili heteroaril, pri čemu je svaki aril ili heteroaril opcionalno supstituiran s 1 do 3 R6a;
svaki R6a je neovisno C1-6 alkil, C2-6 alkenil, C2-6 alkinil, C1-6 hidroksialkil, C1-6 aminoalkil, C1-6 alkoksi, C2-6 alkoksialkil, halogen, C1-6 haloalkil, C1-6 haloalkoksi, -CN, -NO2, -C(O)R6b, -C(O)OR6b, -OC(O)R6b, -C(O)N(R6b)(R6c), -N(R6b)C(O)R6c, -C(=NR6b)N(R6c)(R6d), -N(R6b)(R6c), -OR6b, -SR6b, -S(O)R6b, -S(O)2R6b, -S(NR6b)(NR6c)R6d, -S(O)(NR6b)(R6c), -S(O)2N(R6b)(R6c), -N(R6b)S(O)2(R6c), -P(R6b)(R6c), -P(O)(R6b)(R6c), -P(O)(OR6b)(R6c), -P(O)(OR6b)(OR6c), C3-10 cikloalkil, C1-6 alkil-C3-10 cikloalkil, C6-12 aril, C1-6 alkil-C6-12 aril, heterocikloalkil, C1-6 alkil-(heterocikloalkil), heteroaril, ili C1-6 alkil-(heteroaril), pri čemu je svaki cikloalkil, aril, heterocikloalkil, ili heteroaril opcionalno supstituiran s 1 do 3 R6e, alkil je opcionalno supstituiran s R6f, i alkinil je opcionalno supstituiran s 1 do 4 R6j;
svaki od R6b, R6c, i R6d je neovisno vodik, C1-6 alkil, C1-6 hidroksialkil, C1-6 aminoalkil, C2-6 alkoksialkil, C1-6 haloalkil, C3-10 cikloalkil, C1-6 alkil-C3-10 cikloalkil, C6-12 aril, C1-6 alkil-C6-12 aril, heterocikloalkil, C1-6 alkil-(heterocikloalkil), heteroaril, ili C1-6 alkil-(heteroaril), pri čemu je svaki cikloalkil, aril, heterocikloalkil, ili heteroaril opcionalno supstituiran s 1 do 3 R6k;
svaki R6k je neovisno C1-6 alkil, C1-6 hidroksialkil, C1-6 aminoalkil, C1-6 alkoksi, C2-6 alkoksialkil, C1-6 haloalkil, C1-6 haloalkoksi, C3-10 cikloalkil, C1-6 alkil-C3-10 cikloalkil, heterocikloalkil, ili C1-6 alkil-(heterocikloalkil);
svaki R6e je neovisno C1-6 alkil, C2-6 alkenil, C2-6 alkinil, C1-6 hidroksialkil, C1-6 aminoalkil, C1-6 alkoksi, C2-6 alkoksialkil, halogen, C1-6 haloalkil, C1-C6 haloalkoksi, -CN, -NO2, -C(O)R6e1, -C(O)OR6e1, -OC(O)R6e1, -C(O)N(R6e1)(R6e2), -N(R6e1)C(O)R6e2, -OC(O)N(R6e1)(R6e2), -N(R6e1)C(O)OR6e2, -C(=NR6e1)N(R6e2)(R6e3), -N(R6e1)(R6e2), =O, -OR6e1, -SR6e1, -S(O)R6e1, -S(NR6e1)(NR6e2), -S(O)(NR6e1)(R6e2), -S(O)2R6e1, -S(O)2N(R6e1)(R6e2), -SF5, -N(R6e1)S(O)2(R6e2), -P(R6e1)(R6e2), -P(O)(R6e1)(R6e2), -P(O)(OR6e1)(R6e2), -P(O)(OR6e1)(OR6e2), -Si(R6e1)(R6e2)(R6e3), C3-10 cikloalkil, C1-6 alkil-C3-10 cikloalkil, C6-12 aril, C1-6 alkil-C6-12 aril, heterocikloalkil, C1-6 alkil-heterocikloalkil, heteroaril, ili C1-6 alkil-heteroaril, pri čemu je svaki cikloalkil, aril, heterocikloalkil, ili heteroaril opcionalno supstituiran s 1 do 3 R6h, i alkil je opcionalno supstituiran s 1 do 3 R6m;
svaki od R6e1, R6e2, i R6e3 je neovisno vodik, C1-6 alkil, C1-6 hidroksialkil, C1-6 aminoalkil, C1-6 alkoksialkil, C1-6 haloalkil, C3-10 cikloalkil, C1-6 alkil-C3-10 cikloalkil, C6-10aril, C1-6 alkil-C6-10aril, heterocikloalkil, C1-6 alkil-(heterocikloalkil), heteroaril, ili C1-6 alkil-(heteroaril), pri čemu je svaki cikloalkil, aril, heterocikloalkil, ili heteroaril opcionalno supstituiran s 1 do 3 R6n;
svaki R6n je C1-6 alkil, C2-6 alkenil, C2-6 alkinil, C1-6 hidroksialkil, C1-6 aminoalkil, C1-6 alkoksi, C2-6 alkoksialkil, halogen, C1-6 haloalkil, C1-6 haloalkoksi, -CN, -C(O)R6n1, -C(O)OR6n1, -OC(O)R6n1, -C(O)N(R6n1)(R6n2), -N(R6n1)C(O)R6n2, -OC(O)N(R6n1)(R6n2), -N(R6n1)C(O)OR6n2, -C(=NR6n1)N(R6n2)(R6n3), -N(R6n1)(R6n2), =O, -OH, -SR6n1, -S(O)R6n1, -S(NR6n1)(NR6n2)R6n3, -S(O)(NR6n1)(R6n2), -S(O)2R6n1, -S(O)2N(R6n1)(R6n2), ili -N(R6n1)S(O)2(R6n2);
svaki od R6n1, R6n2, i R6n3 je neovisno vodik, C1-6 alkil, C1-6 hidroksialkil, C1-6 aminoalkil, C2-6 alkoksialkil, C1-6 haloalkil, C3-10 cikloalkil, C1-6 alkil-C3-10 cikloalkil, C6-10 aril, C1-6 alkil-C6-10 aril, heterocikloalkil, C1-6 alkil-(heterocikloalkil), heteroaril, ili C1-6 alkil-(heteroaril);
svaki R6h je neovisno C1-6 alkil, C2-6 alkenil, C2-6 alkinil, C1-6 hidroksialkil, C1-6 aminoalkil, C1-6 alkoksi, C2-6 alkoksialkil, halogen, C1-6 haloalkil, C1-6 haloalkoksi, -CN, -C(O)R6h1, -C(O)OR6h1, -OC(O)R6h1, -C(O)N(R6h1)(R6h2), -N(R6h1)C(O)R6h2, -OC(O)N(R6h1)(R6h2), -N(R6h1)C(O)OR6h2, -C(=NR6h1)N(R6h2)(R6h3), -N(R6h1)(R6h2), =O, -OH, -SR6h1, -S(O)R6h1, -S(NR6h1)(NR6h2)R6h3, -S(O)(NR6h1)(R6h2), -S(O)2R6h1, -S(O)2N(R6h1)(R6h2), -N(R6h1)S(O)2(R6h2), C3-10 cikloalkil, C1-6 alkil-C3-10 cikloalkil, heterocikloalkil, ili C1-6 alkil-(heterocikloalkil);
svaki od R6h1, R6h2, i R6h3 je neovisno vodik, C1-6 alkil, C1-6 hidroksialkil, C1-6 aminoalkil, C2-6 alkoksialkil, C1-6 haloalkil, C3-10 cikloalkil, C1-6 alkil-C3-10 cikloalkil, C6-10 aril, C1-6 alkil-C6-10 aril, heterocikloalkil, C1-6 alkil-(heterocikloalkil), heteroaril, ili C1-6 alkil-(heteroaril);
svaki R6m je neovisno halogen, C1-6 haloalkil, C1-6 haloalkoksi, -CN, -C(O)R6m1, -C(O)OR6m1, -OC(O)R6m1, -C(O)N(R6m1)(R6m2), -N(R6m1)C(O)R6m2, -OC(O)N(R6m1)(R6m2), -N(R6m1)C(O)OR6m2, -C(=NR6m3)N(R6m1)(R6m2), -N(R6m1)(R6m2), =O, -OH, -SR6m1, -S(O)R6m1, -S(NR6m1)(NR6m2)R6m3, -S(O)(NR6m1)(R6m2), -S(O)2R6m1, -S(O)2N(R6m1)(R6m2), ili -N(R6m3)S(O)2(R6m2);
svaki od R6m1, R6m2, i R6m3 je neovisno vodik, C1-6 alkil, C1-6 hidroksialkil, C1-6 aminoalkil, C2-6 alkoksialkil, C1-6 haloalkil, C3-10 cikloalkil, C1-6 alkil-C3-10 cikloalkil, C6-10 aril, C1-6 alkil-C6-10 aril, heterocikloalkil, C1-6 alkil-(heterocikloalkil), heteroaril, ili C1-6 alkil-(heteroaril);
R6f je -OSi(R6f1)(R6f2)(R6f3);
svaki od R6f1, R6f2, i R6f3 je neovisno C1-6 alkil;
svaki R6j je neovisno C2-6 alkoksialkil, halogen, C1-6 haloalkil, C1-6 haloalkoksi, -CN, -C(O)R6j1, -C(O)OR6j1, -OC(O)R6j1, -C(O)N(R6j1)(R6j2), -N(R6j3)C(O)R6j2, -OC(O)N(R6j1)(R6j2), -N(R6j1)C(O)OR6j2, -C(=NR6j3)N(R6j1)(R6j2), -N(R6j1)(R6j2), =O, -SR6j1, -S(O)R6j1, -S(NR6j1)(NR6j2), -S(NR6j1)(NR6j2)R6j3,-S(O)(NR6j1)(R6j2), -S(O)2R6j1, -S(O)2N(R6j1)(R6j2), -N(R6j1)S(O)2(R6j2), -Si(R6j1)(R6j2)(R6j3), C3-10 cikloalkil, C6-12 aril, heterocikloalkil, ili heteroaril, pri čemu je cikloalkil, aril, heterocikloalkil, ili heteroaril opcionalno supstituiran s 1 do 3 R6p;
svaki od R6j1, R6j2, i R6j3 je neovisno vodik, C1-6 alkil, C1-6 hidroksialkil, C1-6 aminoalkil, C2-6 alkoksialkil, C1-6 haloalkil, C3-10 cikloalkil, C1-6 alkil-C3-10 cikloalkil, C6-10 aril, C1-6 alkil-C6-10 aril, heterocikloalkil, C1-6 alkil-(heterocikloalkil), heteroaril, ili C1-6 alkil-(heteroaril);
svaki R6p je neovisno C1-6 alkil, C1-6 hidroksialkil, C1-6 aminoalkil, C1-6 alkoksi, C2-6 alkoksialkil, halogen, C1-6 haloalkil, C1-6 haloalkoksi, -CN, -C(O)R6p1, -C(O)OR6p1, -OC(O)R6p1, -C(O)N(R6p1)(R6p2), -N(R6p1)C(O)R6p2, -OC(O)N(R6p1)(R6p2), -N(R6p1)C(O)OR6p2, -C(=NR6p3)N(R6p1)(R6p2), -N(R6p1)(R6p2), -O, -OH, -SR6p1, -S(O)R6p1, -S(NR6p1)(NR6p2)R6p3, -S(O)(NR6p1)(R6p2), -S(O)2R6p1, -S(O)2N(R6p1)(R6p2), ili -N(R6p1)S(O)2(R6p2);
svaki od R6p1, R6p2, i R6p3 je neovisno vodik, C1-6 alkil, C1-6 hidroksialkil, C1-6 aminoalkil, C2-6 alkoksialkil, C1-6 haloalkil, C3-10 cikloalkil, C1-6 alkil-C3-10 cikloalkil, C6-10 aril, C1-6 alkil-C6-10 aril, heterocikloalkil, C1-6 alkil-(heterocikloalkil), heteroaril, ili C1-6 alkil-(heteroaril);
ili R5 i jedan R6a zajedno s atomima s kojima su vezani, tvore heterocikloalkil, opcionalno supstituiran s 1 do 3 R6g;
svaki R6g je neovisno C1-6 alkil, C2-6 alkenil, C2-6 alkinil, C1-6 hidroksialkil, C1-6 aminoalkil, C2-6 alkoksialkil, halogen, C1-6 haloalkil, C1-6 haloalkoksi, ili -CN;
R' je vodik, C1-6 alkil, C1-6 hidroksialkil, C1-6 aminoalkil, C1-6 alkoksi, C2-6 alkoksialkil, C1-6 alkiltio, halogen, C1-6 haloalkil, -CN, -OH, -NH2, C3-10 cikloalkil, C1-6 alkil-C3-10 cikloalkil, heterocikloalkil, ili C1-6 alkil-(heterocikloalkil);
svaki heterocikloalkil je 3 do 20-člani prsten koji ima 1 do 4 heteroatoma od kojih je svaki neovisno N, O ili S; i
svaki heteroaril je 5 do 18-člani prsten koji ima 1 do 4 heteroatoma od kojih je svaki neovisno N, O ili S;
uz uvjet da R5 i R6 nisu oba C1-4 alkil; i
kada R5 je vodik, R6 nije izopropil ili fenil supstituiran s 2-Me.
2. Spoj prema patentnom zahtjevu 1, ili njegova farmaceutski prihvatljiva sol, naznačen time, da
R1 je vodik, C1-6 alkil, C2-6 alkenil, C2-6 alkinil, C1-6 alkoksi, halogen, C1-6 haloalkil, C1-6 haloalkoksi, ili -CN;
R2 je vodik, C1-6 alkil, C2-6 alkenil, C2-6 alkinil, C1-6 hidroksialkil, C1-6 alkoksi, C2-6 alkoksialkil, halogen, C1-6 haloalkil, C1-6 haloalkoksi, -CN, -NO, -NO2, -C(O)R2a, -C(O)OR2a, -OC(O)R2a, -C(O)N(R2a)(R2b), -N(R2a)C(O)R2b, -OC(O)N(R2a)(R2b), -N(R2a)C(O)OR2b, -C(=NR2a)N(R2b)(R2c), -N(R2a)(R2b), -OR2a, -SR2a, -S(O)R2a, -S(O)2R2a, -S(O)2N(R2a)(R2b), -N(R2a)S(O)2(R2b), -P(O)(R2a)(R2b), -P(O)(OR2a)(R2b), -P(O)(OR2a)(OR2b), C3-10 cikloalkil, C1-6 alkil-C3-10 cikloalkil, C6-12 aril, C1-6 alkil-C6-12 aril, heterocikloalkil, ili heteroaril, pri čemu je svaki alkenil ili alkinil neovisno opcionalno supstituiran s 1 do 3 skupine R2d, svaki cikloalkil je opcionalno supstituiran s 1 do 3 skupine R2e, svaki aril je opcionalno supstituiran s 1 do 3 skupine R2f, svaki heterocikloalkil je opcionalno supstituiran s 1 do 3 skupine R2g, i svaki heteroaril je opcionalno supstituiran s 1 do 3 skupine R2b;
svaki od R2a, R2b, i R2c je neovisno vodik, C1-6 alkil, C1-6 hidroksialkil, C2-6 alkoksialkil, C1-6 haloalkil, C3-10 cikloalkil, C1-6 alkil-C3-10 cikloalkil, C6-12 aril, C1-6 alkil-C6-12 aril, heterocikloalkil, ili heteroaril;
alternativno, R2a, R2b, i R2c kada su vezani na isti atom, mogu se kombinirati s atomom s kojim su vezani, za tvorbu heterocikloalkila;
svaki R2d je neovisno -N(R2d1)(R2d2), -OR2d1, C3-10 cikloalkil, C1-6 alkil-C3-10 cikloalkil, C6-12 aril, C1-6 alkil-C6-12 aril, heterocikloalkil, ili heteroaril;
svaki od R2d1 i R2d2 je neovisno vodik, C1-6 alkil, ili -C(O)O-(C1-6 alkil);
svaki od R2e, R2f, R2g, i R2h je neovisno vodik, C1-6 alkil, C1-6 alkoksi, halogen, C1-6 haloalkil, ili C1-6 haloalkoksi;
R3 je vodik, C1-6 alkil, C2-6 alkenil, C2-6 alkinil, C1-6 hidroksialkil, C1-6 alkoksi, C2-6 alkoksialkil, halogen, C1-6 haloalkil, C1-6 haloalkoksi, -CN, -NO, -NO2, -C(O)R3a, -C(O)OR3a, -OC(O)R3a, -C(O)N(R3a)(R3b), -N(R3a)C(O)R3b, -OC(O)N(R3a)(R3b), -N(R3a)C(O)OR3b, -C(=NR3a)N(R3b)(R3c), -N(R3a)(R3b), -OR3a, -SR3a, -S(O)R3a, -S(O)2R3a, -S(O)2N(R3a)(R3b), -N(R3a)S(O)2(R3b), -P(O)(R3a)(R3b), -P(O)(OR3a)(R3b), -P(O)(OR3a)(OR3b), C3-10 cikloalkil, C1-6 alkil-C3-10 cikloalkil, C6-12 aril, C1-6 alkil-C6-12 aril, heterocikloalkil, ili heteroaril, pri čemu je svaki alkenil ili alkinil neovisno opcionalno supstituiran s 1 do 3 skupine R3d, svaki cikloalkil je opcionalno supstituiran s 1 do 3 skupine R3e, svaki aril je opcionalno supstituiran s 1 do 3 skupine R3f, svaki heterocikloalkil je opcionalno supstituiran s 1 do 3 skupine R3g, i svaki heteroaril je opcionalno supstituiran s 1 do 3 skupine R3b;
svaki od R3a, R3b, i R3c je neovisno vodik, C1-6 alkil, C1-6 hidroksialkil, C2-6 alkoksialkil, C1-6 haloalkil, C3-10 cikloalkil, C1-6 alkil-C3-10 cikloalkil, C6-12 aril, C1-6 alkil-C6-12 aril, heterocikloalkil, ili heteroaril;
alternativno, R3a, R3b, i R3c kada su vezani na isti atom, mogu se kombinirati s atomom s kojim su vezani, za tvorbu heterocikloalkila;
svaki R3d je neovisno -N(R3d1)(R3d2), -OR3d1, C3-10 cikloalkil, C1-6 alkil-C3-10 cikloalkil, C6-12 aril, C1-6 alkil-C6-12 aril, heterocikloalkil, ili heteroaril;
svaki od R3d1 i R3d2 je neovisno vodik, C1-6 alkil, ili -C(O)O-(C1-6 alkil);
svaki od R3e, R3f, R3g, i R3b je neovisno vodik, C1-6 alkil, C1-6 alkoksi, halogen, C1-6 haloalkil, ili C1-6 haloalkoksi;
R4 je vodik, C1-6 alkil, C2-6 alkenil, C2-6 alkinil, C1-6 alkoksi, halogen, C1-6 haloalkil, C1-6 haloalkoksi, ili -CN;
R5 je vodik, C1-6 alkil, C2-6 alkenil, C2-6 alkinil, C1-6 hidroksialkil, C2-6 alkoksialkil, C1-6 haloalkil, C3-10 cikloalkil, C1-6 alkil-C3-10 cikloalkil, C6-12 aril, C1-6 alkil-C6-12 aril, heterocikloalkil, C1-6 alkil-(heterocikloalkil), heteroaril, ili C1-6 alkil-(heteroaril), pri čemu je alkil opcionalno supstituiran s R5a;
R5a je -OSi(R5a1)(R5a2)(R5a3);
svaki od R5a1, R5a2, i R5a3 je neovisno C1-6 alkil; i
R6 je C1-6 alkil, C2-6 alkenil, C2-6 alkinil, C1-6 haloalkil, C6-12 aril, ili heteroaril, pri čemu je svaki aril ili heteroaril opcionalno supstituiran s 1 do 3 R6a;
svaki R6a je neovisno C1-6 alkil, C2-6 alkenil, C2-6 alkinil, C1-6 hidroksialkil, C1-6 alkoksi, C2-6 alkoksialkil, halogen, C1-6 haloalkil, C1-6 haloalkoksi, -CN, -NO2, -C(O)R6b, -C(O)OR6b, -OC(O)R6b, -C(O)N(R6b)(R6c), -N(R6b)C(O)R6c, -C(=NR6b)N(R6c)(R6d), -N(R6b)(R6c), -OR6b, -SR6b, -S(O)R6b, -S(O)2R6b, -S(O)2N(R6b)(R6c), -N(R6b)S(O)2(R6c), C3-10 cikloalkil, C6-12 aril, heterocikloalkil, ili heteroaril, pri čemu je svaki cikloalkil, aril, heterocikloalkil, ili heteroaril opcionalno supstituiran s 1 do 3 R6e, i alkil je opcionalno supstituiran s R6f;
ili R5 i jedan R6a zajedno s atomima s kojima su vezani, tvore heterocikloalkil opcionalno supstituiran s 1 do 3 R6g;
svaki od R6b, R6c, i R6d je neovisno vodik, C1-6 alkil, C1-6 hidroksialkil, C2-6 alkoksialkil, C1-6 haloalkil, C3-10 cikloalkil, C1-6 alkil-C3-10 cikloalkil, C6-12 aril, C1-6 alkil-C6-12 aril, heterocikloalkil, ili heteroaril;
svaki R6e je neovisno C1-6 alkil, C2-6 alkenil, C2-6 alkinil, C1-6 hidroksialkil, C1-6 alkoksi, C2-6 alkoksialkil, halogen, C1-6 haloalkil, C1-6 haloalkoksi, -CN, -NO2, -C(O)R6e1, -C(O)OR6e1, -OC(O)R6e1, -C(O)N(R6e1)(R6e2), -N(R6e1)C(O)R6e2, -C(=NR6e1)N(R6e2)(R6e3), -N(R6e1)(R6e2), -OR6e1, -SR6e1, -S(O)R6e1, -S(O)2R6e1, -S(O)2N(R6e1)(R6e2), -N(R6e1)S(O)2(R6e2), C3-10 cikloalkil, C6-12 aril, heterocikloalkil, ili heteroaril, pri čemu je svaki cikloalkil, aril, heterocikloalkil, ili heteroaril opcionalno supstituiran s 1 do 3 R6h;
svaki od R6e1, R6e2, i R6e3 je neovisno vodik, ili C1-6 alkil;
R6f je -OSi(R6f1)(R6f2)(R6f3);
svaki od R6f1, R6f2, i R6f3 je neovisno C1-6 alkil;
svaki R6g je neovisno C1-6 alkil, C2-6 alkenil, C2-6 alkinil, halogen, C1-6 haloalkil, C1-6 haloalkoksi, ili -CN;
svaki R6b je neovisno C1-6 alkil, C2-6 alkenil, C2-6 alkinil, C1-6 alkoksi, halogen, C1-6 haloalkil, C1-6 haloalkoksi, -C(O)R6h1, -C(O)OR6h1, -OC(O)R6h1, -C(O)N(R6h1)(R6h2), -N(R6h1)C(O)R6h2, -C(=NR6h1)N(R6h2)(R6h3), -N(R6h1)(R6h2), -OH, -SR6h1, -S(O)R6h1, -S(O)2R6h1, -S(O)2N(R6h1)(R6h2), ili -N(R6h1)S(O)2(R6h2);
svaki od R6h1, R6h2, i R6h3 je neovisno vodik, ili C1-6 alkil;
R' je vodik, C1-6 alkil, halogen, C1-6 haloalkil, -CN, ili -OH;
svaki heterocikloalkil je 3 do 10-člani prsten koji ima 1 do 4 heteroatoma od kojih je svaki neovisno N, O ili S; i
svaki heteroaril je 5 do 10-člani prsten koji ima 1 do 4 heteroatoma od kojih je svaki neovisno N, O ili S;
uz uvjet da R5 i R6 nisu oba C1-4 alkil; i
kada R5 je vodik, R6 nije izopropil ili fenil supstituiran s 2-Me.
3. Spoj prema patentnom zahtjevu 1 ili 2, ili njegova farmaceutski prihvatljiva sol, naznačen time, da
(A)
R5 je C1-6 alkil, C2-6 alkenil, C2-6 alkinil, C1-6 hidroksialkil, C2-6 alkoksialkil, C1-6 haloalkil, C3-10 cikloalkil, C1-6 alkil-C3-10 cikloalkil, C6-12 aril, C1-6 alkil-C6-12 aril, heterocikloalkil, C1-6 alkil-(heterocikloalkil), heteroaril, ili C1-6 alkil-(heteroaril), pri čemu je alkil opcionalno supstituiran s R5a; i
R6 je C6-12aril ili heteroaril, pri čemu je svaki aril ili heteroaril opcionalno supstituiran s 1 do 3 s R6a;
ili R5 i R6a zajedno s atomima s kojima su vezani, tvore heterocikloalkil opcionalno supstituiran s 1 do 3 R6g; i/ili
(B) R1 je vodik, C1-6 alkil, C1-6 alkoksi, halogen, C1-6 haloalkil, ili -CN, ili R1 je vodik, C1-3 alkil, C1-3 alkoksi, ili halogen, ili R1 je vodik, Me, -OMe, F, ili Cl, ili R1 je vodik; i/ili
(C)
R2 je vodik, C1-6 alkil, C2-6 alkenil, C2-6 alkinil, C1-6 hidroksialkil, C1-6 alkoksi, C2-6 alkoksialkil, halogen, C1-6 haloalkil, C1-6 haloalkoksi, -CN, -NO, -NO2, -C(O)R2a, -C(O)OR2a, -OC(O)R2a, -C(O)N(R2a)(R2b), -N(R2a)C(O)R2b, -OC(O)N(R2a)(R2b), -N(R2a)C(O)OR2b, -N(R2a)(R2b), -OR2a, -S(O)2N(R2a)(R2b), -N(R2a)S(O)2(R2b), C3-10 cikloalkil, C1-6 alkil-C3-10 cikloalkil, C6-12 aril, C1-6 alkil-C6-12 aril, 3 do 8-člani heterocikloalkilni prsten koji ima 1 do 3 heteroatoma od kojih je svaki neovisno N, O ili S, ili 5 do 10-člani heteroarilni prsten koji ima 1 do 3 heteroatoma od kojih je svaki neovisno N, O ili S, pri čemu svaki alkenil ili alkinil je neovisno opcionalno supstituiran s 1 do 3 skupine R2d, i svaki aril je opcionalno supstituiran s 1 do 3 skupine R2f;
svaki od R2a i R2b je neovisno vodik, C1-6 alkil, C1-6 hidroksialkil, C2-6 alkoksialkil, ili C1-6 haloalkil;
svaki R2d je neovisno -N(R2d1)(R2d2), -OR2d1, C3-10 cikloalkil, C1-6 alkil-C3-10 cikloalkil, C6-12 aril, C1-6 alkil-C6-12 aril;
svaki od R2d1 i R2d2 je neovisno vodik, C1-6 alkil, ili -C(O)O-(C1-6 alkil); i
svaki R2f je neovisno vodik, C1-6 alkil, C1-6 alkoksi, ili halogen; i/ili
(D)
R2 je vodik, C1-6 alkil, C2-6 alkenil, C2-6 alkinil, C1-6 hidroksialkil, C1-6 alkoksi, C2-6 alkoksialkil, halogen, C1-6 haloalkil, -CN, -NO, -NO2, -C(O)R2a, -C(O)OR2a, -N(R2a)C(O)R2b, -N(R2a)(R2b), -OR2a, -N(R2a)S(O)2(R2b), C3-10 cikloalkil, C6-10 aril, 5 do 8-člani heterocikloalkilni prsten koji ima 1 do 2 heteroatoma od kojih je svaki neovisno N, O ili S, ili 5 do 6-člani heteroarilni prsten koji ima 1 do 3 heteroatoma od kojih je svaki neovisno N, O ili S, pri čemu je svaki alkenil ili alkinil neovisno opcionalno supstituiran s 1 do 3 skupine R2d, i svaki aril je opcionalno supstituiran s 1 do 3 skupine R2f;
svaki od R2a i R2b je neovisno vodik, C1-6 alkil, C1-6 hidroksialkil, ili C2-6 alkoksialkil;
svaki R2d je neovisno -N(R2d1)(R2d2), -OR2d1, C3-10 cikloalkil, ili C6-12 aril;
svaki od R2d1 i R2d2 je neovisno vodik, C1-4alkil, ili -C(O)O-(C1-4alkil); i
svaki R2f je neovisno C1-6 alkoksi, ili halogen; i/ili
(E)
R2 je vodik, C1-3alkil, C2-3alkenil, C2-6 alkinil, C1-3hidroksialkil, C1-3alkoksi, C2-3alkoksialkil, halogen, C1-3haloalkil, -CN, -NO, -NO2, -C(O)R2a, -C(O)OR2a, -N(R2a)C(O)R2b, -N(R2a)(R2b), -N(R2a)S(O)2(R2b), C3-6cikloalkil, fenil, 5 do 6-člani heterocikloalkilni prsten koji ima 1 do 2 heteroatoma od kojih je svaki neovisno N ili O, ili 5 do 6-člani heteroarilni prsten koji ima 1 do 2 heteroatoma od kojih je svaki neovisno N, O ili S, pri čemu je svaki alkenil ili alkinil neovisno opcionalno supstituiran s jednom skupinom R2d, i svaki fenil je opcionalno supstituiran s jednom skupinom R2f;
svaki od R2a i R2b je neovisno vodik, C1-3alkil, C1-3hidroksialkil, ili C2-3alkoksialkil;
svaki R2d je neovisno -N(R2d1)(R2d2), -OR2d1, C3-8cikloalkil, ili fenil;
svaki od R2d1 i R2d2 je neovisno vodik, ili -C(O)O-(C1-4 alkil); i
svaki R2f je neovisno C1-3alkoksi, ili halogen; i/ili
(F) R2 je vodik, Me, Et, iPr, -CH=CH2, -CH=CHMe, -C(Me)=CH2, -CMe=CHMe, -CH=C(Me)2, -CH=CHEt, -C=CH, -C=C-Me, -C=C-Et, -C=C-tBu, -C≡C-CH2OH, -C≡C-CMe2(OH), -C≡C-CH2NH2, -C≡C-CH2NHC(O)OtBu, -C=C-CMe2(SO2Me), -CH2OH, -CH2CH2CH2OH, -CH(OH)CH2CH3, -OMe, -OEt, -OCH2CH=CH2, -CH2OMe, -CH2NHMe, -CH2NMe2, -CH2CH2COOEt, F, Cl, Br, I, -CF3, -CN, -NO, -NO2, -C(O)H, -COOH, -COOMe, -NHCOMe, -NH2, -NHMe, -NMe2, -NHCH2CH2OH, -NHCH2CH2OMe, -NHSO2Me,-OH, -NH-N=CH-OEt, -NH2-NH2, SMe, -SO2Me, ciklopropil,
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i/ili
(G)
R3 je vodik, C1-6 alkil, C2-6 alkenil, C2-6 alkinil, C1-6 hidroksialkil, C1-6 alkoksi, C2-6 alkoksialkil, halogen, C1-6 haloalkil, C1-6 haloalkoksi, -CN, -NO, -NO2, -C(O)R3a, -C(O)OR3a, -OC(O)R3a, -C(O)N(R3a)(R3b), -N(R3a)C(O)R3b, -OC(O)N(R3a)(R3b), -N(R3a)C(O)OR3b, -N(R3a)(R3b), -OR3a, -S(O)2N(R3a)(R3b), -N(R3a)S(O)2(R3b), C3-10 cikloalkil, C1-6 alkil-C3-10 cikloalkil, C6-12 aril, C1-6 alkil-C6-12 aril, 3 do 8-člani heterocikloalkilni prsten koji ima 1 do 3 heteroatoma od kojih je svaki neovisno N, O ili S, ili 5 do 10-člani heteroarilni prsten koji ima 1 do 3 heteroatoma od kojih je svaki neovisno N, O ili S, pri čemu je svaki alkenil ili alkinil neovisno opcionalno supstituiran s 1 do 3 skupine R3d, i svaki aril je opcionalno supstituiran s 1 do 3 skupine R3f;
svaki od R3a i R3b je neovisno vodik, C1-6 alkil, C1-6 hidroksialkil, ili C2-6 alkoksialkil;
svaki R3d je neovisno -N(R3d1)(R3d2), -OR3d1, C3-10 cikloalkil, ili C6-12 aril;
svaki od R3d1 i R3d2 je neovisno vodik, C1-4alkil, ili -C(O)O-(C1-4alkil); i
svaki R3f je neovisno C1-6 alkoksi, ili halogen; i/ili
(H) R3 je vodik, C1-6 alkil, C1-6 hidroksialkil, C1-6 alkoksi, C2-6 alkoksialkil, halogen, C1-6 haloalkil, -CN, -NO2, -C(O)OR3a, -C(O)N(R3a)(R3b), -N(R3a)(R3b), -N(R3a)S(O)2(R3b), ili 5 do 6-člani heteroarilni prsten koji ima 1 do 3 heteroatoma od kojih je svaki neovisno N, O ili S; i
svaki od R3a i R3b je neovisno vodik, ili C1-6 alkil; i/ili
(I)
R3 je vodik, C1-3 alkil, C1-6 hidroksialkil, C1-6 alkoksi, C2-6 alkoksialkil, halogen, C1-6 haloalkil, -CN, -NO2, -C(O)OR3a, -C(O)N(R3a)(R3b), -N(R3a)(R3b), -N(R3a)S(O)2(R3b), ili 5 do 6-člani heteroarilni prsten koji ima 1 do 2 heteroatoma od kojih je svaki N; i
svaki od R3a i R3b je neovisno vodik ili C1-3alkil; i/ili
(J) R3 je vodik, Me, Et, -CH2OH, -OMe, -CH2OMe, F, Cl, Br, -CF3, -CN, -NO2, -COOMe, -CONH2, -NH2, -NHSO2Me, ili
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ili
(K)
R3 je vodik, C1-6 alkil, C1-6 hidroksialkil, C1-6 alkoksi, C2-6 alkoksialkil, halogen, -CN, -NO2, -C(O)OR3a, -C(O)N(R3a)(R3b), -N(R3a)(R3b), -N(R3a)S(O)2(R3b), ili 5 do 6-člani heteroarilni prsten koji ima 1 do 3 heteroatoma od kojih je svaki neovisno N, O ili S; i
svaki od R3a i R3b je neovisno vodik ili C1-6 alkil; i/ili
(L)
R3 je vodik, C1-3 alkil, C1-3 hidroksialkil, C1-3 alkoksi, C2-3 alkoksialkil, halogen, -CN, -NO2, -C(O)OR3a, -C(O)N(R3a)(R3b), -N(R3a)(R3b), -N(R3a)S(O)2(R3b), ili 5 do 6-člani heteroarilni prsten koji ima 1 ili 2 heteroatoma od kojih je svaki N; i
svaki od R3a i R3b je neovisno vodik ili C1-3 alkil; i/ili
(M) R3 je vodik, Me, Et, -CH2OH, -OMe, -CH2OMe, F, Cl, Br, -CN, -NO2, -COOMe, -CONH2, -NH2, -NHSO2Me, ili
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i/ili
(N) R4 je vodik, C1-6 alkil, C1-6 alkoksi, halogen, C1-6 haloalkil, ili -CN, ili R4 je vodik, C1-6 alkil, ili halogen, ili R4 je vodik, Me, F, Cl, ili Br, ili R4 je vodik; i/ili
(O)
R1 je vodik;
R2 je vodik, C1-3 alkil, C2-3 alkenil, C2-6 alkinil, C1-3 hidroksialkil, C2-3 alkoksialkil, halogen, -CN, -NO, -NO2, -C(O)R2a, -N(R2a)C(O)R2b, -N(R2a)(R2b), -OR2a, ili 5 do 6-člani heteroarilni prsten koji ima 1 do 2 heteroatoma od kojih je svaki neovisno N, O ili S;
svaki od R2a i R2b je neovisno vodik, ili C1-3 alkil;
R3 je vodik, C1-3 alkil, halogen, -CN, ili -NO2; i
R4 je vodik; ili
(P)
R1 je vodik;
R2 je vodik, C1-3 alkil, C2-3 alkenil, C2-6 alkinil, C1-3 hidroksialkil, C2-3 alkoksialkil, halogen, -CN, -NO, -NO2, -C(O)R2a, -N(R2a)C(O)R2b, -N(R2a)(R2b), -OR2a, ili 5 do 6-člani heteroarilni prsten koji ima 1 do 2 heteroatoma od kojih je svaki neovisno N, O ili S;
svaki od R2a i R2b je neovisno vodik, ili C1-3 alkil;
R3 je vodik; i
R4 je vodik; i/ili
(Q)
R5 je C1-6 alkil, C2-6 alkenil, C2-6 alkinil, C1-6 hidroksialkil, C2-6 alkoksialkil, C1-6 haloalkil, C3-10 cikloalkil, C1-6 alkil-C3-10 cikloalkil, C6-12 aril, C1-6 alkil-C6-12 aril, C1-6 alkil-(heterocikloalkil), ili C1-6 alkil-(heteroaril), pri čemu je alkil opcionalno supstituiran s R5a;
R5a je -OSi(R5a1)(R5a2)(R5a3);
svaki od R5a1, R5a2 i R5a3 je neovisno C1-4 alkil; i
heterocikloalkil je 5 do 8-člani prsten koji ima 1 do 2 heteroatoma od kojih je svaki neovisno N, O ili S; i
heteroaril je 5 do 6-člani prsten koji ima 1 do 2 heteroatoma od kojih je svaki neovisno N, O ili S; i/ili
(R)
R5 je C1-6 alkil, C2-6 alkinil, C2-6 alkoksialkil, C1-6 haloalkil, C3-10 cikloalkil, C1-6 alkil-C3-10 cikloalkil, C6-12 aril, C1-6 alkil-C6-12 aril, ili C1-6 alkil-(heterocikloalkil), pri čemu je alkil opcionalno supstituiran s R5a;
R5a je -OSi(R5a1)(R5a2)(R5a3);
svaki od R5a1, R5a2 i R5a3 je neovisno C1-4 alkil, gdje su R5a1 i R5a2 različiti; i
heterocikloalkil je 5 do 6-člani prsten koji ima 1 do 2 heteroatoma od kojih je svaki neovisno N ili O; ili
(S)
R5 je C1-6 alkil, C2-6 alkinil, C2-3alkoksialkil, C1-3haloalkil, C3-8cikloalkil, C1-3alkil-C3-8cikloalkil, fenil, C1-3 alkil-fenil, ili C1-3alkil-(heterocikloalkil), pri čemu je alkil opcionalno supstituiran s R5a;
R5a je -OSi(R5a1)(R5a2)(R5a3);
svaki od R5a1, R5a2 i R5a3 je neovisno Me ili tBu, gdje su R5a1 i R5a2 različiti; i
heterocikloalkil je 6-člani prsten koji ima 1 heteroatom N ili O; ili
(T) R5 je Me, Et, nPr, nBu, -CH2CMe3, -CH2C≡CMe, -CH2CH2C≡CH, -CH2CH2OMe, -CH2CH2OSi(Me)2(tBu), -CF3, -CH2CF2H, -CH2CF3,
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Ili
(U)
R5 je C1-6 alkil, C2-6 alkenil, C2-6 alkinil, C1-6 hidroksialkil, C2-6 alkoksialkil, C1-6 haloalkil, C1-6 alkil-C3-10 cikloalkil, C6-12 aril, C1-6 alkil-C6-12 aril, C1-6 alkil-(heterocikloalkil), ili C1-6 alkil-(heteroaril), pri čemu je alkil opcionalno supstituiran s R5a;
R5a je -OSi(R5a1)(R5a2)(R5a3);
svaki od R5a1, R5a2 i R5a3 je neovisno C1-4 alkil; i
heterocikloalkil je 5 do 8-člani prsten koji ima 1 do 2 heteroatoma od kojih je svaki neovisno N, O ili S; i
heteroaril je 5 do 6-člani prsten koji ima 1 do 2 heteroatoma od kojih je svaki neovisno N, O ili S; ili
(V)
R5 je C1-6 alkil, C2-6 alkinil, C2-6 alkoksialkil, C1-6 alkil-C3-10 cikloalkil, C6-12 aril, C1-6 alkil-C6-12 aril, ili C1-6 alkil-(heterocikloalkil), pri čemu je alkil opcionalno supstituiran s R5a;
R5a je -OSi(R5a1)(R5a2)(R5a3);
svaki od R5a1, R5a2 i R5a3 je neovisno C1-4 alkil, gdje su R5a1 i R5a2 različiti; i
heterocikloalkil je 5 do 6-člani prsten koji ima 1 do 2 heteroatoma od kojih je svaki neovisno N ili O; ili
(W)
R5 je C1-6 alkil, C2-6 alkinil, C2-3alkoksialkil, C1-3alkil-C3-8cikloalkil, fenil, C1-3 alkil-fenil, ili C1-3alkil-(heterocikloalkil), pri čemu je alkil opcionalno supstituiran s R5a;
R5a je -OSi(R5a1)(R5a2)(R5a3);
svaki od R5a1, R5a2 i R5a3 je neovisno Me ili tBu, gdje su R5a1 i R5a2 različiti; i
heterocikloalkil je 6-člani prsten koji ima 1 heteroatom N ili O; ili
(X) R5 je Me, Et, nPr, nBu, -CH2CMe3, -CH2C≡CMe, -CH2CH2C≡CH, -CH2CH2OMe, -CH2CH2OSi(Me)2(tBu),
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i/ili
(Y)
R6 je fenil, naftil, tienil, tiazolil, piridil, pirazinil, pirimidinil, ili dibenzofuril, od kojih je svaki opcionalno supstituiran s 1 ili 2 R6a; ili
R6 je fenil, ili 5 do 6-člani heteroarilni prsten koji ima 1 do 3 heteroatoma od kojih je svaki neovisno N, O ili S, od kojih je svaki opcionalno supstituiran s 1 ili 2 R6a; ili
R6 je fenil, tienil, tiazolil, izotiazolil, oksazolil, izoksazolil, pirolil, pirazolil, piridil, ili, pirimidinil, od kojih je svaki opcionalno supstituiran s 1 ili 2 R6a; ili
R6 je
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ili
R6 je
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i/ili
(Z) R7 je vodik, Me, Et, OMe, -CH2OH, -CH2OMe, -CH2NMe2, Cl, CHF2, OH, NH2, SMe, ili
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ili R7 je vodik, Me, Et, OMe, -CH2NMe2, Cl, OH, NH2, SMe, ili
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4. Spoj prema bilo kojem od patentnih zahtjeva 1 do 3, ili njegova farmaceutski prihvatljiva sol, naznačen time, da ima jednu od sljedećih formula:
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gdje n je 0, 1, 2 ili 3;
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5. Spoj prema bilo kojem od patentnih zahtjeva 1 do 4, ili njegova farmaceutski prihvatljiva sol, naznačen time, da
(a)
svaki R6a je neovisno C1-6 alkil, C2-6 alkinil, C1-6 hidroksialkil, C1-6 alkoksi, C2-6 alkoksialkil, halogen, C1-6 haloalkil, C1-6 haloalkoksi, -CN, -NO2, -C(O)R6b, -C(O)OR6b, -C(O)N(R6b)(R6c), -N(R6b)(R6c), -OR6b, C3-10 cikloalkil, C6-12 aril, heterocikloalkil, ili heteroaril, pri čemu je svaki cikloalkil, aril, heterocikloalkil, ili heteroaril opcionalno supstituiran s 1 do 3 R6e, i alkil je opcionalno supstituiran s R6f;
svaki od R6b i R6c je neovisno vodik, ili C1-6 alkil;
svaki R6e je neovisno C1-6 alkil, C2-6 alkenil, C2-6 alkinil, C1-6 hidroksialkil, C1-6 alkoksi, C2-6 alkoksialkil, halogen, C1-6 haloalkil, -C(O)OR6e1, -OC(O)R6e1, -C(O)N(R6e1)(R6e2), -N(R6e1)C(O)R6e2, -OR6e1, -S(O)2N(R6e1)(R6e2), -N(R6e1)S(O)2(R6e2);
svaki od R6e1 i R6e2 je neovisno vodik, ili C1-6 alkil;
R6f je -OSi(R6f1)(R6f2)(R6f3); i
svaki od R6f1, R6f2, i R6f3 je neovisno C1-6 alkil; i/ili
(b)
svaki R6a je neovisno C1-3 alkil, C2-3 alkinil, C1-3 hidroksialkil, C1-3 alkoksi, C2-3 alkoksialkil, halogen, C1-3 haloalkil, C1-3 haloalkoksi, -CN, -NO2, -C(O)R6b, -C(O)OR6b, -C(O)N(R6b)(R6c), -N(R6b)(R6c), -OR6b, C3-8 cikloalkil, fenil, 5 do 6-člani heterocikloalkilni prsten koji ima 1 do 2 heteroatoma od kojih je svaki neovisno N ili O, ili 5 do 6-člani heteroarilni prsten koji ima 1 do 2 heteroatoma od kojih je svaki neovisno N, O ili S, pri čemu je svaki cikloalkil, fenil, heterocikloalkil, ili heteroaril opcionalno supstituiran s 1 do 2 R6e, i alkil je opcionalno supstituiran s R6f;
svaki od R6b i R6c je neovisno vodik, ili C1-3 alkil;
svaki R6e je neovisno C1-6 alkil, C1-6 hidroksialkil, C1-6 alkoksi, C2-6 alkoksialkil, halogen, C1-6 haloalkil, -C(O)OR6e1, -OC(O)R6e1, -N(R6e1)C(O)R6e2, -OR6e1;
svaki od R6e1 i R6e2 je neovisno vodik, ili C1-6 alkil;
R6f je -OSi(R6f1)(R6f2)(R6f3); i
svaki od R6f1, R6f2 i R6f3 je neovisno Me ili tBu; i/ili
(c)
svaki R6e je neovisno C1-6 alkil, C1-3 alkoksi, halogen, C1-6 haloalkil, -N(R6e1)C(O)R6e2, ili -OR6e1; i
svaki od R6e1 i R6e2 je neovisno vodik, ili C1-3 alkil; ili
(d) svaki R6n je neovisno Me ili CO2tBu; ili
(e) svaki R6h je neovisno Me, -CH2OH, -CH2NHMe, OMe, NH2, CF3, CN, -(CO)Me, -(CO)tBu, -(CO)-CH2OH, CO2Me, CO2tBu, =O, ili
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ili
(f) Rm je neovisno OH, CF3, CN, CO2H, CONH2, NMe2, SO2Me, ili
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ili
(g) svaki R6e je neovisno Me, Et, iPr, tBu, -CH2OH, -C(OH)Me2, -OMe, -OEt, -OCH2CH2CH3, -CH2OMe, -OCH2CH2NMe2, F, Cl, Br, CHF2, -CF3, -CH2CHF2, -CH2CF3, -CF2CH3, -C(CH3)2CF3, OCF3, -OCH2CF3, -OCH(CH3)CF3, CN, -C(O)Me, -C(O)tBu, CO2H, CO2Me, CO2tBu, C(O)NH2, =O, OH, NH2, NMe2, -NMeCH2CH2OMe, -NHC(O)Me, -NHC(O)tBu, -NHCO2tBu, SO2Me, SO2Et, SO2(iPr), SO2(tBu), SO2CF3, -CH2SO2Me, SO(N=H)Me, SO2NH2, SO2NHMe, SO2NMe2, -SO2NHCH2CH2OH, -NHSO2Me, SF5, -POMe2,
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ili
(h) svaki R6e je neovisno Me, Et, iPr, tBu, -CH2OH, -C(OH)Me2, -OMe, -OEt, -OCH2CH2CH3, -CH2OMe, -OCH2CH2NMe2, F, Cl, Br, CHF2, -CF3, -CH2CHF2, -CH2CF3, -CF2CH3, -C(CH3)2CF3, OCF3, -OCH2CF3, -OCH(CH3)CF3, CN, -C(O)Me, -C(O)tBu, CO2H, CO2Me, CO2tBu, C(O)NH2, =O, OH, NH2, NMe2, -NMeCH2CH2OMe, -NHC(O)Me, -NHC(O)tBu, -NHCO2tBu, SO2Me, SO2Et, SO2(iPr), SO2(tBu), SO2CF3, -CH2SO2Me, SO(N=H)Me, SO2NH2, SO2NHMe, SO2NMe2, -SO2NHCH2CH2OH, -NHSO2Me, SF5, -POMe2,
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ili
(i) svaki R6e je neovisno Me, Et, tBu, -OMe, F, Cl, -CF3, -NHC(O)Me, ili -OH; ili
(j) svaki R6j je neovisno OH, OMe, CH2OMe, F, CHF2, CF3, CN, NH2, NH(CO)CF3, NH(CO)OtBu, SO2Me, Si(iPr)3,
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ili
(k) svaki R6j je neovisno OH, OMe, F, CHF2, CF3, NH2, NH(CO)OtBu, SO2Me,
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(l) svaki R6p je neovisno Me, Et, iPr, F, Cl, CH2F, CHF2, CF3, CF2CH3, CH2CF3, =O, ili OH, ili je svaki R6p neovisno Me, Cl, CF3, =O, ili OH; ili
(m) svaki R6a je neovisno
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ili
(n) svaki R6a je neovisno Me, Et, -C=CMe, -OMe, -CH2OH, -CH2OMe, -CH2OSi(Me)2(tBu), F, CL, Br, I, -CH2F, -CF3, -OCF3, -CN, -NO2, -C(O)H, -COOH, -COOMe, -CONH2, -NH2, -OH, ciklopropil, cikloheksil, fenil,
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6. Spoj prema bilo kojem od patentnih zahtjeva 1 do 5, ili njegova farmaceutski prihvatljiva sol, naznačen time, da
(1)
R5 je C1-6 alkil, C2-6 alkinil, C2-3 alkoksialkil, C1-3 alkil-C3-8 cikloalkil, fenil, C1-3 alkil-fenil, ili C1-3 alkil-(heterocikloalkil);
R6 je fenil opcionalno supstituiran s R6a;
R6a je neovisno C1-3 alkil, C2-3 alkinil, C1-3 hidroksialkil, C1-3 alkoksi, C2-3 alkoksialkil, halogen, C1-3 haloalkil, C1-3 haloalkoksi, -CN, -NO2, -C(O)R6b, -C(O)OR6b, -C(O)N(R6b)(R6c), -N(R6b)(R6c), -OH, ili fenil, pri čemu je fenil opcionalno supstituiran s R6e;
svaki od R6b i R6c je neovisno vodik, ili C1-3 alkil;
R6e je C1-6 alkil, halogen, C1-3 haloalkil, -N(R6e1)C(O)R6e2, ili -OR6e1;
R6e1 i R6e2 su neovisno vodik, ili C1-3 alkil; i
heterocikloalkil je 6-člani prsten koji ima jedan heteroatom N ili O; i/ili
(2) spoj ima Formulu (Ib):
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u kojoj m je 0, 1, 2 ili 3; ili
(3) R6 je
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ili
(4) R6 je
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7. Spoj prema bilo kojem od patentnih zahtjeva 1 do 3, ili njegova farmaceutski prihvatljiva sol, naznačen time, da:
(i) spoj ima Formulu (Ic):
[image]
gdje
Prsten A je 5 do 8-člani heterocikloalkil koji opcionalno ima 1 do 2 dodatna heteroatoma od kojih je svaki neovisno N, O ili S, i opcionalno gdje je Prsten A supstituiran s 1 ili 2 R6g; i
n je 0, 1 ili 2; ili
(ii) svaki R6g je metil; ili
(iii) spoj ima strukturu Formule (IIc):
[image]
gdje
Prsten A je 5 do 8-člani heterocikloalkil koji opcionalno ima 1 do 2 dodatna heteroatoma od kojih je svaki neovisno N, O ili S, i opcionalno gdje je Prsten A supstituiran s 1 ili 2 R6g; i
n je 0, 1 ili 2; ili
pri čemu opcionalno:
R1 je vodik, C1-3 alkil, ili halogen kao što je vodik ili F;
R2 je vodik, C1-3 alkil, C1-3 hidroksialkil, C2-3 alkoksialkil, halogen, ili -CN;
R3 je vodik, C1-3 alkil, ili halogen;
R4 je vodik, C1-3 alkil, ili halogen kao što je vodik, Me, ili F;
svaki R6a je neovisno C1-3 alkil, C2-3 alkenil, ili C2-3 alkinil, pri čemu je alkinil opcionalno supstituiran s 1 do 3 R6j;
svaki R6j je neovisno C2-3 alkoksialkil, halogen, C1-3 haloalkil, C1-3 haloalkoksi, -CN, C3-8 cikloalkil, ili heterocikloalkil, pri čemu je cikloalkil ili heterocikloalkil opcionalno supstituiran s 1 do 3 R6p;
svaki R6p je neovisno C1-3 alkil, C1-3 hidroksialkil, C2-3 alkoksialkil, halogen, C1-3 haloalkil, C1-3 haloalkoksi, ili -CN; i
R7 je vodik, C1-3 alkil, C2-3 alkoksialkil, C1-3 haloalkil, ili -NH2; ili
(iv) spoj ima strukturu Formule (IIc-1):
[image]
gdje
Prsten A je 5 do 8-člani heterocikloalkil koji opcionalno ima 1 do 2 dodatna heteroatoma od kojih je svaki neovisno N, O ili S, i opcionalno gdje je Prsten A supstituiran s 1 ili 2 R6g; i
n je 0, 1 ili 2; i/ili
(v) spoj ima strukturu jedne od Formula (Ic), (IIc), i (IIc-1), i
[image]
ima strukturu
[image]
[image]
ili
[image]
ili
(vi) spoj ima strukturu Formule (IIc-2):
[image]
gdje n je 0, 1 ili 2; i/ili
(vii)
[image]
ima strukturu
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ili
(viii)
[image]
ima strukturu
[image]
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[image]
8. Spoj prema patentnom zahtjevu 7, ili njegova farmaceutski prihvatljiva sol, naznačen time, da spoj ima strukturu Formule (IIc) ili Formule (IIc-1) i
R2 je vodik, C1-3 alkil, C1-3 hidroksialkil, C2-3 alkoksialkil, halogen, ili -CN;
R3 je vodik, C1-3 alkil, ili halogen;
svaki R6a je neovisno C1-3 alkil, C2-3 alkenil, ili C2-3 alkinil, pri čemu je alkinil opcionalno supstituiran s 1 do 3 R6j;
svaki R6j je neovisno C2-3 alkoksialkil, halogen, C1-3 haloalkil, C1-3 haloalkoksi, -CN, C3-8 cikloalkil, ili heterocikloalkil, pri čemu je cikloalkil ili heterocikloalkil opcionalno supstituiran s 1 do 3 R6p;
svaki R6p je neovisno C1-3 alkil, C1-3 hidroksialkil, C2-3 alkoksialkil, halogen, C1-3 haloalkil, C1-3 haloalkoksi, ili -CN;
R7 je vodik, ili C1-3 alkil; i
[image]
ima strukturu
[image]
pri čemu opcionalno:
(a) R2 je vodik, halogen, ili -CN; ili R2 je vodik, F, ili Cl; i/ili
(b) R3 je vodik, F, ili Cl; i/ili
(c) svaki R6a je neovisno C2-3 alkinil ili halogen, pri čemu je alkinil opcionalno supstituiran s 1 do 3 R6j, ili svaki R6a je
[image]
supstituiran s jednim R6j; ili
(d)
svaki R6j je neovisno C2-3 alkoksialkil, halogen, C1-3 haloalkil, -CN, C3-6 cikloalkil, ili heterocikloalkil, pri čemu je cikloalkil ili heterocikloalkil opcionalno supstituiran s 1 do 3 R6p, i svaki heterocikloalkil je 3 do 6-člani prsten koji ima 1 do 2 heteroatoma od kojih je svaki neovisno N, O ili S; ili
svaki R6j je neovisno halogen, C1-3 haloalkil, C3-6 cikloalkil, ili heterocikloalkil, pri čemu je cikloalkil ili heterocikloalkil opcionalno supstituiran s 1 do 2 R6p, i svaki heterocikloalkil je 3 do 6-člani prsten koji ima 1 do 2 heteroatoma od kojih je svaki neovisno N, O ili S; ili
svaki R6j je neovisno halogen, C1-3 haloalkil, ili C3-6 cikloalkil, pri čemu je cikloalkil opcionalno supstituiran s jednim R6p; ili
svaki R6j je neovisno F, CH2F, CHF2, CF3, CH2CF3, CF2CH3, ili ciklopropil, pri čemu je ciklopropil opcionalno supstituiran s jednim R6p; i/ili
(e) svaki R6p je neovisno C1-3 alkil, C1-3 hidroksialkil, halogen, C1-3 haloalkil, ili -CN, ili svaki R6p je neovisno Me, Et, CH2OH, F, CH2F, CHF2, CF3, CH2CF3, CF2CH3, ili -CN, i/ili
(f)
[image]
ima strukturu
[image]
[image]
9. Farmaceutski pripravak, naznačen time, da sadrži farmaceutski učinkovitu količinu spoja prema bilo kojem od patentnih zahtjeva 1-8, ili njegove farmaceutski prihvatljive soli, i farmaceutski prihvatljiv nosač ili pomoćno sredstvo.
10. Farmaceutski pripravak prema patentnom zahtjevu 9, naznačen time, da nadalje sadrži jedno ili više dodatnih terapijskih sredstava, pri čemu opcionalno, jedno ili više dodatnih terapijskih sredstava neovisno su anti-neoplastično saredstvo, nivolumab, pembrolizumab, atezolizumab, ipilimumab, kemoterapija, terapija zračenjem, ili resekcijska terapija, ili jedno ili više dodatnih terapijskih sredstava neovisno su rituksan, doksorubicin, gemcitabin, nivolumab, pembrolizumab, artezolizumab, nivolumab, pembrolizumab, atezolizumab, ili ipilimumab, ili jedno ili više dodatnih terapijskih sredstava jest inhibitor PD-1/PD-L1, ili jedno ili više dodatnih terapijskih sredstava jest cjepivo.
11. Spoj prema bilo kojem od patentnih zahtjeva 1-8, ili njegova farmaceutski prihvatljiva sol, ili farmaceutski pripravak prema patentnom zahtjevu 9 ili 10, naznačen time, da je za uporabu u postupku za liječenje raka, pri čemu opcionalno:
(A) rak je rak gušterače, rak mokraćnog mjehura, kolorektalni rak, rak dojke, rak prostate, rak bubrega, hepatocelularni rak, rak pluća, rak jajnika, rak cerviksa, rak želuca, rak jednjaka, rak glave i vrata, melanom, neuroendokrini rak, rak središnjeg živčanog sustava (CNS rak), rak mozga, rak kostiju, sarkom mekog tkiva, rak ne-malih stanica pluća, rak malih stanica pluća ili rak debelog crijeva, ili je rak akutna limfoblastična leukemija (ALL), akutna mijeloična leukemija (AML), kronična limfocitna leukemija (CLL), limfom malih limfocita (SLL), mijelodisplastični sindrom (MDS), mijeloproliferativna bolest (MPD), kronična mijeloična leukemija (CML), multipli mijelom (MM), ne-Hodgkinov limfom (NHL), limfom plaštenih stanica (MCL), folikularni limfom, Waldenströmova makroglobulinemija (WM), limfom T stanica, limfom B stanica ili difuzni limfom velikih B stanica (DLBCL), i/ili
(B) postupak nadalje obuhvaća davanje jednog ili više dodatnih terapijskih sredstava pojedincu,
pri čemu opcionalno, jedno ili više dodatnih terapijskih sredstava neovisno su anti-neoplastično sredstvo, nivolumab, pembrolizumab, atezolizumab, ipilimumab, kemoterapija, terapija zračenjem, ili resekcijska terapija, ili
jedno ili više dodatnih terapijskih sredstava neovisno su rituksan, doksorubicin, gemcitabin, nivolumab, pembrolizumab, atezolizumab, nivolumab, pembrolizumab, atezolizumab, ili ipilimumab, ili
jedno ili više dodatnih terapijskih sredstava jest inhibitor PD-1/PD-L1, ili
jedno ili više dodatnih terapijskih sredstava sadrže jednu ili više populacija imunosnih stanica odabranih iz skupine koju čine: stanice prirodne ubojice (NK), NK-T stanice, T stanice, citokinom inducirane stanice ubojice (CIK), makrofagi stanice (MAC), limfociti koji se infiltriraju u tumor (TILs) i dendritičke stanice (DCs), ili
jedno ili više dodatnih terapijskih sredstava sadrže populaciju T stanica odabranu iz skupine koju čine: alfa/beta TCR T stanice, gama/delta TCR T stanice, regulatorne T stanice (Treg) i TRuCTM T stanice, ili
jedno ili više dodatnih terapijskih sredstava sadrže populaciju NK-92 stanica, pri čemu opcionalno jedna ili više populacija imunosnih stanica sadrže jedan ili više kimernih antigenskih receptora (CARs) i/ili stanice su alogenske za namijenjenog primatelja, ili
jedno ili više dodatnih terapijskih sredstava sadrže imunoterapiju, imunostimulirajuću terapiju, citokinsku terapiju, kemokinsku terapiju, celularnu terapiju, gensku terapiju, ili njihove kombinacije,
pri čemu opcionalno imunoterapija obuhvaća zajedničku primjenu jednog ili više protutijela ili njegovog fragmenta koji veže antigen, ili njegovog konjugata protutijelo-lijek, multispecifičnih molekula koje ciljaju CD3, multispecifičnih molekula koje ciljaju CD16, ili neimunoglobulinskih domena koje vežu antigen ili mimetičkih proteina protutijela koji su usmjereni protiv jednog ili više ciljeva ili antigena povezanih s tumorom (TAAs), ili
jedno ili više dodatnih terapijskih sredstava sadrže cjepivo.
12. Spoj prema bilo kojem od patentnih zahtjeva 1-8, ili njegova farmaceutski prihvatljiva sol, ili farmaceutski pripravak prema patentnom zahtjevu 9 ili 10, naznačeni time, da su za uporabu u postupku za liječenje virusne HIV infekcije ili hepatitis B virusne infekcije, pri čemu opcionalno: postupak nadalje obuhvaća davanje jednog ili više dodatnih terapijskih sredstava, pri čemu opcionalno jedno ili više terapijskih sredstava sadrže cjepivo.
13. Spoj prema bilo kojem od patentnih zahtjeva 1-8, ili njegova farmaceutski prihvatljiva sol, naznačen time, da je za uporabu u inhibiranju metastaza raka kod pojedinca kojemu je to potrebno.
14. Spoj prema bilo kojem od patentnih zahtjeva 1-8, ili njegova farmaceutski prihvatljiva sol, naznačen time, da je za uporabu u liječenju.
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