HRP20110220T1 - Inhibitori kinaze - Google Patents
Inhibitori kinaze Download PDFInfo
- Publication number
- HRP20110220T1 HRP20110220T1 HR20110220T HRP20110220T HRP20110220T1 HR P20110220 T1 HRP20110220 T1 HR P20110220T1 HR 20110220 T HR20110220 T HR 20110220T HR P20110220 T HRP20110220 T HR P20110220T HR P20110220 T1 HRP20110220 T1 HR P20110220T1
- Authority
- HR
- Croatia
- Prior art keywords
- alkyl
- group
- hetero
- cycloalkyl
- bicycloaryl
- Prior art date
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- 229940043355 kinase inhibitor Drugs 0.000 title abstract 2
- 239000003757 phosphotransferase inhibitor Substances 0.000 title abstract 2
- 150000001875 compounds Chemical class 0.000 claims abstract 31
- 206010012289 Dementia Diseases 0.000 claims abstract 7
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims abstract 5
- 206010028980 Neoplasm Diseases 0.000 claims abstract 4
- 201000011510 cancer Diseases 0.000 claims abstract 4
- 201000010099 disease Diseases 0.000 claims abstract 4
- 206010061218 Inflammation Diseases 0.000 claims abstract 2
- 150000001408 amides Chemical class 0.000 claims abstract 2
- 206010003246 arthritis Diseases 0.000 claims abstract 2
- 150000002148 esters Chemical class 0.000 claims abstract 2
- 230000004054 inflammatory process Effects 0.000 claims abstract 2
- 150000003839 salts Chemical class 0.000 claims abstract 2
- 239000012453 solvate Substances 0.000 claims abstract 2
- 125000000217 alkyl group Chemical group 0.000 claims 101
- 125000005842 heteroatom Chemical group 0.000 claims 56
- 125000000753 cycloalkyl group Chemical group 0.000 claims 49
- 125000000008 (C1-C10) alkyl group Chemical group 0.000 claims 43
- 125000003118 aryl group Chemical group 0.000 claims 31
- -1 cyano, thio, oxy, hydroxy, carbonyloxy Chemical group 0.000 claims 31
- 125000005843 halogen group Chemical group 0.000 claims 27
- 125000001424 substituent group Chemical group 0.000 claims 24
- 125000001072 heteroaryl group Chemical group 0.000 claims 22
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 claims 21
- 150000001602 bicycloalkyls Chemical group 0.000 claims 19
- 125000000475 sulfinyl group Chemical group [*:2]S([*:1])=O 0.000 claims 18
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 17
- 229910052739 hydrogen Inorganic materials 0.000 claims 16
- 239000001257 hydrogen Substances 0.000 claims 16
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 16
- 125000003545 alkoxy group Chemical group 0.000 claims 14
- 125000000472 sulfonyl group Chemical group *S(*)(=O)=O 0.000 claims 14
- 125000003282 alkyl amino group Chemical group 0.000 claims 11
- 125000002813 thiocarbonyl group Chemical group *C(*)=S 0.000 claims 10
- 125000004104 aryloxy group Chemical group 0.000 claims 9
- 125000001841 imino group Chemical group [H]N=* 0.000 claims 8
- 125000005553 heteroaryloxy group Chemical group 0.000 claims 7
- 241000124008 Mammalia Species 0.000 claims 6
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 6
- 125000005740 oxycarbonyl group Chemical group [*:1]OC([*:2])=O 0.000 claims 5
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 claims 4
- 125000004356 hydroxy functional group Chemical group O* 0.000 claims 4
- 201000011240 Frontotemporal dementia Diseases 0.000 claims 3
- 208000010877 cognitive disease Diseases 0.000 claims 3
- 206010027175 memory impairment Diseases 0.000 claims 3
- 230000002265 prevention Effects 0.000 claims 3
- 201000004384 Alopecia Diseases 0.000 claims 2
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 2
- 125000004429 atom Chemical group 0.000 claims 2
- 125000005708 carbonyloxy group Chemical group [*:2]OC([*:1])=O 0.000 claims 2
- 230000003920 cognitive function Effects 0.000 claims 2
- 230000007423 decrease Effects 0.000 claims 2
- 239000003814 drug Substances 0.000 claims 2
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 2
- 238000000926 separation method Methods 0.000 claims 2
- 125000000027 (C1-C10) alkoxy group Chemical group 0.000 claims 1
- LWKMTSGBTDBNNY-UHFFFAOYSA-N 5-(3-ethylsulfonylphenyl)-3,8-dimethyl-9h-pyrido[2,3-b]indole Chemical compound CCS(=O)(=O)C1=CC=CC(C=2C=3C4=CC(C)=CN=C4NC=3C(C)=CC=2)=C1 LWKMTSGBTDBNNY-UHFFFAOYSA-N 0.000 claims 1
- GZQUVLPYFQBCBP-UHFFFAOYSA-N 5-(3-ethylsulfonylphenyl)-8-methyl-9h-pyrido[2,3-b]indole Chemical compound CCS(=O)(=O)C1=CC=CC(C=2C=3C4=CC=CN=C4NC=3C(C)=CC=2)=C1 GZQUVLPYFQBCBP-UHFFFAOYSA-N 0.000 claims 1
- CMAJPRSIBKMYRC-UHFFFAOYSA-N 5-(3-ethylsulfonylphenyl)-9h-pyrido[2,3-b]indole Chemical compound CCS(=O)(=O)C1=CC=CC(C=2C=3C4=CC=CN=C4NC=3C=CC=2)=C1 CMAJPRSIBKMYRC-UHFFFAOYSA-N 0.000 claims 1
- XTEMRAFJCFBHFF-UHFFFAOYSA-N 5-(3-methoxyphenyl)-9h-pyrido[2,3-b]indole Chemical compound COC1=CC=CC(C=2C=3C4=CC=CN=C4NC=3C=CC=2)=C1 XTEMRAFJCFBHFF-UHFFFAOYSA-N 0.000 claims 1
- CMNRVZMJMRCXJI-UHFFFAOYSA-N 5-(3-methylphenyl)-9h-pyrido[2,3-b]indole Chemical compound CC1=CC=CC(C=2C=3C4=CC=CN=C4NC=3C=CC=2)=C1 CMNRVZMJMRCXJI-UHFFFAOYSA-N 0.000 claims 1
- WEOPAFKZSFLZAB-UHFFFAOYSA-N 5-(3-methylsulfonylphenyl)-9h-pyrido[2,3-b]indole Chemical compound CS(=O)(=O)C1=CC=CC(C=2C=3C4=CC=CN=C4NC=3C=CC=2)=C1 WEOPAFKZSFLZAB-UHFFFAOYSA-N 0.000 claims 1
- RGFSBLSURVONPK-UHFFFAOYSA-N 5-benzylsulfanyl-8-methyl-9h-pyrido[2,3-b]indole Chemical compound C1=2C3=CC=CN=C3NC=2C(C)=CC=C1SCC1=CC=CC=C1 RGFSBLSURVONPK-UHFFFAOYSA-N 0.000 claims 1
- NYUWZVUNEZTVSB-UHFFFAOYSA-N 5-benzylsulfanyl-9h-pyrido[2,3-b]indole Chemical compound C=1C=CC=2NC3=NC=CC=C3C=2C=1SCC1=CC=CC=C1 NYUWZVUNEZTVSB-UHFFFAOYSA-N 0.000 claims 1
- BKPLEKGNOVHRJX-UHFFFAOYSA-N 5-phenyl-9h-pyrido[2,3-b]indole Chemical compound C1=CC=CC=C1C1=CC=CC2=C1C1=CC=CN=C1N2 BKPLEKGNOVHRJX-UHFFFAOYSA-N 0.000 claims 1
- BIPOSFOQOCEGNA-UHFFFAOYSA-N 5-phenylsulfanyl-9h-pyrido[2,3-b]indole Chemical compound C=1C=CC=2NC3=NC=CC=C3C=2C=1SC1=CC=CC=C1 BIPOSFOQOCEGNA-UHFFFAOYSA-N 0.000 claims 1
- 208000024827 Alzheimer disease Diseases 0.000 claims 1
- 206010003571 Astrocytoma Diseases 0.000 claims 1
- 208000020925 Bipolar disease Diseases 0.000 claims 1
- 206010005003 Bladder cancer Diseases 0.000 claims 1
- 206010006187 Breast cancer Diseases 0.000 claims 1
- 208000026310 Breast neoplasm Diseases 0.000 claims 1
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims 1
- 208000028698 Cognitive impairment Diseases 0.000 claims 1
- 206010009944 Colon cancer Diseases 0.000 claims 1
- 208000001333 Colorectal Neoplasms Diseases 0.000 claims 1
- 208000011990 Corticobasal Degeneration Diseases 0.000 claims 1
- 206010067889 Dementia with Lewy bodies Diseases 0.000 claims 1
- 201000010374 Down Syndrome Diseases 0.000 claims 1
- YLQBMQCUIZJEEH-UHFFFAOYSA-N Furan Chemical compound C=1C=COC=1 YLQBMQCUIZJEEH-UHFFFAOYSA-N 0.000 claims 1
- 206010017993 Gastrointestinal neoplasms Diseases 0.000 claims 1
- 208000032612 Glial tumor Diseases 0.000 claims 1
- 206010018338 Glioma Diseases 0.000 claims 1
- 206010019196 Head injury Diseases 0.000 claims 1
- 208000023105 Huntington disease Diseases 0.000 claims 1
- 208000022559 Inflammatory bowel disease Diseases 0.000 claims 1
- 208000007766 Kaposi sarcoma Diseases 0.000 claims 1
- 201000002832 Lewy body dementia Diseases 0.000 claims 1
- 208000019022 Mood disease Diseases 0.000 claims 1
- 208000014060 Niemann-Pick disease Diseases 0.000 claims 1
- 206010033128 Ovarian cancer Diseases 0.000 claims 1
- 206010061535 Ovarian neoplasm Diseases 0.000 claims 1
- 208000018737 Parkinson disease Diseases 0.000 claims 1
- 208000027089 Parkinsonian disease Diseases 0.000 claims 1
- 206010034010 Parkinsonism Diseases 0.000 claims 1
- 108091000080 Phosphotransferase Proteins 0.000 claims 1
- 208000000609 Pick Disease of the Brain Diseases 0.000 claims 1
- 201000004681 Psoriasis Diseases 0.000 claims 1
- 208000000453 Skin Neoplasms Diseases 0.000 claims 1
- 206010041067 Small cell lung cancer Diseases 0.000 claims 1
- 208000006011 Stroke Diseases 0.000 claims 1
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical compound [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 claims 1
- 208000024770 Thyroid neoplasm Diseases 0.000 claims 1
- 206010052779 Transplant rejections Diseases 0.000 claims 1
- 206010044688 Trisomy 21 Diseases 0.000 claims 1
- 208000007097 Urinary Bladder Neoplasms Diseases 0.000 claims 1
- 208000008385 Urogenital Neoplasms Diseases 0.000 claims 1
- 201000004810 Vascular dementia Diseases 0.000 claims 1
- 239000004480 active ingredient Substances 0.000 claims 1
- 230000007000 age related cognitive decline Effects 0.000 claims 1
- 125000002723 alicyclic group Chemical group 0.000 claims 1
- 125000001931 aliphatic group Chemical group 0.000 claims 1
- 125000002947 alkylene group Chemical group 0.000 claims 1
- 125000001118 alkylidene group Chemical group 0.000 claims 1
- 125000004103 aminoalkyl group Chemical group 0.000 claims 1
- 206010002026 amyotrophic lateral sclerosis Diseases 0.000 claims 1
- 206010068168 androgenetic alopecia Diseases 0.000 claims 1
- 201000002996 androgenic alopecia Diseases 0.000 claims 1
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims 1
- 125000004452 carbocyclyl group Chemical group 0.000 claims 1
- 229910052799 carbon Inorganic materials 0.000 claims 1
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 1
- 230000001684 chronic effect Effects 0.000 claims 1
- 239000003433 contraceptive agent Substances 0.000 claims 1
- 230000002254 contraceptive effect Effects 0.000 claims 1
- 125000002993 cycloalkylene group Chemical group 0.000 claims 1
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 1
- 230000006735 deficit Effects 0.000 claims 1
- 208000017004 dementia pugilistica Diseases 0.000 claims 1
- 229940079593 drug Drugs 0.000 claims 1
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 1
- 125000002485 formyl group Chemical class [H]C(*)=O 0.000 claims 1
- 208000005017 glioblastoma Diseases 0.000 claims 1
- 208000024963 hair loss Diseases 0.000 claims 1
- 230000003676 hair loss Effects 0.000 claims 1
- 201000010536 head and neck cancer Diseases 0.000 claims 1
- 208000014829 head and neck neoplasm Diseases 0.000 claims 1
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims 1
- 125000006588 heterocycloalkylene group Chemical group 0.000 claims 1
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 1
- 150000002576 ketones Chemical class 0.000 claims 1
- 125000005647 linker group Chemical group 0.000 claims 1
- 201000001441 melanoma Diseases 0.000 claims 1
- 208000027061 mild cognitive impairment Diseases 0.000 claims 1
- VGPBPWRBXBKGRE-UHFFFAOYSA-N n-(oxomethylidene)hydroxylamine Chemical compound ON=C=O VGPBPWRBXBKGRE-UHFFFAOYSA-N 0.000 claims 1
- ABHMZXIVLIIAIP-UHFFFAOYSA-N n-[3-(9h-pyrido[2,3-b]indol-5-yl)phenyl]ethanesulfonamide Chemical compound CCS(=O)(=O)NC1=CC=CC(C=2C=3C4=CC=CN=C4NC=3C=CC=2)=C1 ABHMZXIVLIIAIP-UHFFFAOYSA-N 0.000 claims 1
- INKIZSXBTRLIHN-UHFFFAOYSA-N n-[4-(9h-pyrido[2,3-b]indol-5-ylsulfanyl)phenyl]acetamide Chemical compound C1=CC(NC(=O)C)=CC=C1SC1=CC=CC2=C1C1=CC=CN=C1N2 INKIZSXBTRLIHN-UHFFFAOYSA-N 0.000 claims 1
- CXHDRBWMWUKPGJ-UHFFFAOYSA-N n-cyclopropyl-3-(9h-pyrido[2,3-b]indol-5-yl)benzenesulfonamide Chemical compound C=1C=CC(C=2C=3C4=CC=CN=C4NC=3C=CC=2)=CC=1S(=O)(=O)NC1CC1 CXHDRBWMWUKPGJ-UHFFFAOYSA-N 0.000 claims 1
- 230000007106 neurocognition Effects 0.000 claims 1
- 230000004770 neurodegeneration Effects 0.000 claims 1
- 208000015122 neurodegenerative disease Diseases 0.000 claims 1
- 210000002682 neurofibrillary tangle Anatomy 0.000 claims 1
- 229910052757 nitrogen Inorganic materials 0.000 claims 1
- 208000002154 non-small cell lung carcinoma Diseases 0.000 claims 1
- 229910052760 oxygen Inorganic materials 0.000 claims 1
- 239000001301 oxygen Substances 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 102000020233 phosphotransferase Human genes 0.000 claims 1
- 201000002212 progressive supranuclear palsy Diseases 0.000 claims 1
- 210000002307 prostate Anatomy 0.000 claims 1
- 201000000980 schizophrenia Diseases 0.000 claims 1
- 201000000849 skin cancer Diseases 0.000 claims 1
- 208000000587 small cell lung carcinoma Diseases 0.000 claims 1
- 206010041823 squamous cell carcinoma Diseases 0.000 claims 1
- 229940124530 sulfonamide Drugs 0.000 claims 1
- 150000003456 sulfonamides Chemical class 0.000 claims 1
- 229910052717 sulfur Inorganic materials 0.000 claims 1
- 239000011593 sulfur Substances 0.000 claims 1
- 201000002510 thyroid cancer Diseases 0.000 claims 1
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 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
- KXDHJXZQYSOELW-UHFFFAOYSA-M Carbamate Chemical compound NC([O-])=O KXDHJXZQYSOELW-UHFFFAOYSA-M 0.000 abstract 1
- 208000035475 disorder Diseases 0.000 abstract 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
- A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
- A61K31/437—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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
- A61P15/18—Feminine contraceptives
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/06—Antipsoriatics
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/14—Drugs for dermatological disorders for baldness or alopecia
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
- A61P25/16—Anti-Parkinson drugs
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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- A61P25/00—Drugs for disorders of the nervous system
- A61P25/24—Antidepressants
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A—HUMAN NECESSITIES
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61P35/04—Antineoplastic agents specific for metastasis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
- A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
-
- 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
- C07D471/12—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 three hetero rings
-
- 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
-
- 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
- C07D487/12—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 three hetero rings
- C07D487/14—Ortho-condensed systems
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Immunology (AREA)
- Psychiatry (AREA)
- Pain & Pain Management (AREA)
- Dermatology (AREA)
- Psychology (AREA)
- Hospice & Palliative Care (AREA)
- Endocrinology (AREA)
- Rheumatology (AREA)
- Cardiology (AREA)
- Transplantation (AREA)
- Heart & Thoracic Surgery (AREA)
- Gynecology & Obstetrics (AREA)
- Oncology (AREA)
- Reproductive Health (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Pyridine Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Hydrogenated Pyridines (AREA)
Abstract
Spoj formule (I): ili njegova farmaceutski prihvatljiva sol, solvat ili hidrat; naznačen time što: R1 je -Y1-R12,svaki Y1 i Y3 nezavisno je odsutan ili linker koji osigurava razdvojenost od 1 ili 2 atoma između R12 ili R14 i prstena za koji je Y1 ili Y3 vezan, pri čemu su atomi koji osiguravaju razdvojenost izabrani iz grupe koju čine ugljik, kisik, dušik i sumpor; R4 je izabran iz grupe koju čine vodik, halo, nitro, cijano, tio, oksi, hidroksi, karboniloksi, alkoksi, karbonil, amino, (C1-5)alkilamino, (C1-5)alkil, halo(C1-5)alkil, karbonil(C1-3)alkil, sulfonil(C1-3)alkil, amino(C1-5)alkil, aril(C1-5)alkil, heteroaril(C1-5)alkil, (C3-6)cikloalkil i hetero(C3-6)cikloalkil, svaki nesupstituiran ili supstituiran sa jednim ili više supstituenata izabranih iz grupe A; R5 je izabran iz grupe koju čine vodik, halo i (C1-5)alkil, nesupstituiran ili supstituiran sa jednim ili više supstituenata izabranih iz grupe A; R6 je izabran iz grupe koju čine vodik, halo, amino, karbonil, alkoksi i (C1-5)alkil, pri čemu je svaki od njih nesupstituiran ili supstituiran sa jednim ili više supstituenata izabranih iz grupe A; R7 je izabran iz grupe koju čine vodik, halo, hidroksi, alkoksi, amino i (C1-5)alkil, pri čemu je svaki od njih nesupstituiran ili supstituiran sa jednim ili više supstituenata izabranih iz grupe A; svako R12 i R13 nezavisno su izabrani iz grupe koju čine vodik, halo, nitro, cijano, tio, oksi, hidroksi, alkoksi, ariloksi, heteroariloksi, karbonil, amino, (C1-10)alkilamino, sulfonamid, imino, sulfonil, sulfinil, (C1-10)alkil, halo(C1-10)alkil, karbonil(C1-3)alkil, tiokarbonil(C1-3)alkil, sulfonil(C1-3)alkil, sulfinil(C1-3)alkil, amino(C1-10)alkil, imino(C1-3)alkil, (C3-12)cikloalkil(C1-5)alkil, hetero(C3-12)cikloalkil(C1-5)alkil, aril(C1-10)alkil, heteroaril(C1-5)alkil, (C9-12)bicikloaril(C1-5)alkil, hetero(C8-12)bicikloaril(C1-5)alkil, (C3-12)cikloalkil, hetero(C3-12)cikloalkil, (C9-12)bicikloalkil, hetero(C3-12)bicikloalkil, aril, heteroaril, (C9-12)bicikloaril i hetero(C4-12)bicikloaril, pri čemu je svaki nesupstituiran ili supstituiran sa jednim ili više supstituenata izabranih iz grupe A, ili R12 i R13 su uzeti zajedno tako da formiraju prsten; R14 je izabran iz grupe koju čine (C3-12)cikloalkil, hetero(C3-12)cikloalkil, (C9-12)bicikloalkil, hetero(C3-12)bicikloalkil, aril, heteroaril, (C9-12)bicikloaril i hetero(C4-12)bicikloaril, pri čemu je svaki nesupstituiran ili supstituiran sa jednim ili više supstituenata izabranih iz grupe A; Grupu A čine aldehidna, aliciklična, alifatična, (C1-10)alkil, alkilen, alkiliden, amidna, amino, aminoalkil, aromatična, aril, bicikloalkil, bicikloaril, karbamoil, karbociklil, karboksil, karbonil grupa, cikloalkil, cikloalkilen, esterske, halo, heterobicikloalkil, heterocikloalkilen, heteroaril, heterobicikloaril, heterocikloalkil, oksol, hidroksi, iminoketon, keton, nitro, oksa alkil i oksolalkil grupe, pri čemu su svaka od njih nesupstituirane ili supstituirane pomoću supstituenta koji je izabran iz Grupe B;
Claims (29)
1. Spoj formule (I):
[image]
ili njegova farmaceutski prihvatljiva sol, solvat ili hidrat;
naznačen time što:
R1 je -Y1-R12,
svaki Y1 i Y3 nezavisno je odsutan ili linker koji osigurava razdvojenost od 1 ili 2 atoma između R12 ili R14 i prstena za koji je Y1 ili Y3 vezan, pri čemu su atomi koji osiguravaju razdvojenost izabrani iz grupe koju čine ugljik, kisik, dušik i sumpor;
R4 je izabran iz grupe koju čine vodik, halo, nitro, cijano, tio, oksi, hidroksi, karboniloksi, alkoksi, karbonil, amino, (C1-5)alkilamino, (C1-5)alkil, halo(C1-5)alkil, karbonil(C1-3)alkil, sulfonil(C1-3)alkil, amino(C1-5)alkil, aril(C1-5)alkil, heteroaril(C1-5)alkil, (C3-6)cikloalkil i hetero(C3-6)cikloalkil, svaki nesupstituiran ili supstituiran sa jednim ili više supstituenata izabranih iz grupe A;
R5 je izabran iz grupe koju čine vodik, halo i (C1-5)alkil, nesupstituiran ili supstituiran sa jednim ili više supstituenata izabranih iz grupe A;
R6 je izabran iz grupe koju čine vodik, halo, amino, karbonil, alkoksi i (C1-5)alkil, pri čemu je svaki od njih nesupstituiran ili supstituiran sa jednim ili više supstituenata izabranih iz grupe A;
R7 je izabran iz grupe koju čine vodik, halo, hidroksi, alkoksi, amino i (C1-5)alkil, pri čemu je svaki od njih nesupstituiran ili supstituiran sa jednim ili više supstituenata izabranih iz grupe A;
svako R12 i R13 nezavisno su izabrani iz grupe koju čine vodik, halo, nitro, cijano, tio, oksi, hidroksi, alkoksi, ariloksi, heteroariloksi, karbonil, amino, (C1-10)alkilamino, sulfonamid, imino, sulfonil, sulfinil, (C1-10)alkil, halo(C1-10)alkil, karbonil(C1-3)alkil, tiokarbonil(C1-3)alkil, sulfonil(C1-3)alkil, sulfinil(C1-3)alkil, amino(C1-10)alkil, imino(C1-3)alkil, (C3-12)cikloalkil(C1-5)alkil, hetero(C3-12)cikloalkil(C1-5)alkil, aril(C1-10)alkil, heteroaril(C1-5)alkil, (C9-12)bicikloaril(C1-5)alkil, hetero(C8-12)bicikloaril(C1-5)alkil, (C3-12)cikloalkil, hetero(C3-12)cikloalkil, (C9-12)bicikloalkil, hetero(C3-12)bicikloalkil, aril, heteroaril, (C9-12)bicikloaril i hetero(C4-12)bicikloaril, pri čemu je svaki nesupstituiran ili supstituiran sa jednim ili više supstituenata izabranih iz grupe A, ili R12 i R13 su uzeti zajedno tako da formiraju prsten;
R14 je izabran iz grupe koju čine (C3-12)cikloalkil, hetero(C3-12)cikloalkil, (C9-12)bicikloalkil, hetero(C3-12)bicikloalkil, aril, heteroaril, (C9-12)bicikloaril i hetero(C4-12)bicikloaril, pri čemu je svaki nesupstituiran ili supstituiran sa jednim ili više supstituenata izabranih iz grupe A;
Grupu A čine aldehidna, aliciklična, alifatična, (C1-10)alkil, alkilen, alkiliden, amidna, amino, aminoalkil, aromatična, aril, bicikloalkil, bicikloaril, karbamoil, karbociklil, karboksil, karbonil grupa, cikloalkil, cikloalkilen, esterske, halo, heterobicikloalkil, heterocikloalkilen, heteroaril, heterobicikloaril, heterocikloalkil, oksol, hidroksi, iminoketon, keton, nitro, oksa alkil i oksolalkil grupe, pri čemu su svaka od njih nesupstituirane ili supstituirane pomoću supstituenta koji je izabran iz Grupe B; i
Grupu B čine halo, nitro, cijano, tio, oksi, hidroksi, karboniloksi, (C1-10)alkoksi, (C4-12)ariloksi, hetero(C1-10)ariloksi, karbonil, oksikarbonil, aminokarbonil, amino, (C1-10)alkilamino, sulfonamido, imino, sulfonil, sulfinil, (C1-10)alkil, halo(C1-10)alkil, hidroksi(C1-10)alkil, karbonil(C1-10)alkil, tiokarbonil(C1-10)alkil, sulfonil(C1-10)alkil, sulfinil(C1-10)alkil, (C1-10)azaalkil, imino(C1-10)alkil, (C3-12)cikloalkil(C1-5)alkil, hetero(C3-12)cikloalkil(C1-10)alkil, aril(C1-10)alkil, hetero(C1-10)aril(C1-5)alkil, (C9-12)bicikloaril(C1-5)alkil, hetero(C8-12)bicikloaril(C1-5)alkil, (C3-12)cikloalkil, hetero(C3-12)cikloalkil, (C9-12)bicikloalkil, hetero(C3-12)bicikloalkil, (C4-12)aril, hetero(C1-10)aril, (C9-12)bicikloaril i hetero(C4-12)bicikloaril.
2. Spoj prema patentnom zahtjevu 1, formule (IA):
[image]
naznačen time što
n je izabran iz grupe koju čine 0, 1, 2, 3 i 4; i
R15 je izabran iz grupe koju čine vodik, halo, nitro, cijano, tio, oksi, hidroksi, alkoksi, ariloksi, heteroariloksi, karbonil, amino, (C1-10)alkilamino, sulfonamido, imino, sulfonil, sulfinil, (C1-10)alkil, halo(C1-10)alkil, karbonil(C1-3)alkil, tiokarbonil(C1-3)alkil, sulfonil(C1-3)alkil, sulfinil(C1-3)alkil, amino (C1-10)alkil, imino(C1-3)alkil, (C3-12)cikloalkil(C1-5)alkil, hetero(C3-12)cikloalkil(C1-5)alkil, aril(C1-10)alkil, heteroaril(C1-5)alkil, (C9-12)bicikloaril(C1-5)alkil, hetero(C8-12)bicikloaril(C1-5)alkil, (C3-12)cikloalkil, hetero(C3-12)cikloalkil, (C9-12)bicikloalkil, hetero(C3-12)bicikloalkil, aril, heteroaril, (C9-12)bicikloaril i hetero(C4-12)bicikloaril, pri čemu je svaki od njih nesupstituiran ili supstituiran sa jednim ili više supstituenata koji su izabrani iz grupe A, ili bilo koja dva R15 uzeti su zajedno tako da formiraju prsten.
3. Spoj prema patentnom zahtjevu 1, formule (IB):
[image]
naznačen time što
n je izabran iz grupe koju čine 0, 1, 2, 3 i 4; i
R15 je izabran iz grupe koju čine vodik, halo, nitro, cijano, tio, oksi, hidroksi, alkoksi, ariloksi, heteroariloksi, karbonil, amino, (C1-10)alkilamino, sulfonamido, imino, sulfonil, sulfinil, (C1-10)alkil, halo(C1-10)alkil, karbonil(C1-3)alkil, tiokarbonil(C1-3)alkil, sulfonil(C1-3)alkil, sulfinil(C1-3)alkil, amino (C1-10)alkil, imino(C1-3)alkil, (C3-12)cikloalkil(C1-5)alkil, hetero(C3-12)cikloalkil(C1-5)alkil, aril(C1-10)alkil, heteroaril(C1-5)alkil, (C9-12)bicikloaril(C1-5)alkil, hetero(C8-12)bicikloaril(C1-5)alkil, (C3-12)cikloalkil, hetero(C3-12)cikloalkil, (C9-12)bicikloalkil, hetero(C3-12)bicikloalkil, aril, heteroaril, (C9-12)bicikloaril i hetero(C4-12)bicikloaril, pri čemu je svaki od njih nesupstituiran ili supstituiran sa jednim ili više supstituenata koji su izabrani iz grupe A, ili bilo koja dva R15 uzeti su zajedno tako da formiraju prsten.
4. Spoj prema patentnom zahtjevu 1, formule (IC):
[image]
naznačen time što
R16 je izabran iz grupe koju čine amino, (C1-10)alkilamino, (C1-10)alkil, halo(C1-10)alkil, hidroksi (C1-5)alkil, karbonil(C1-3)alkil, tiokarbonil(C1-3)alkil, sulfonil(C1-3)alkil, sulfinil(C1-3)alkil, amino (C1-10)alkil, (C3-12)cikloalkil(C1-5)alkil, hetero(C3-12)cikloalkil(C1-5)alkil, aril(C1-10)alkil, heteroaril(C1-5)alkil, (C3-12)cikloalkil, hetero(C3-12)cikloalkil, aril i heteroaril, pri čemu je svaki od njih nesupstituiran ili supstituiran sa jednim ili više supstituenata koji su izabrani iz grupe A.
5. Spoj prema patentnom zahtjevu 1, formule (ID):
[image]
naznačen time što
R16 je izabran iz grupe koju čine amino, (C1-10)alkilamino, (C1-10)alkil, halo(C1-10)alkil, hidroksi(C1-5)alkil, karbonil(C1-3)alkil, tiokarbonil(C1-3)alkil, sulfonil(C1-3)alkil, sulfinil(C1-3)alkil, amino (C1-10)alkil, (C3-12)cikloalkil(C1-5)alkil, hetero(C3-12)cikloalkil(C1-5)alkil, aril(C1-10)alkil, heteroaril(C1-5)alkil, (C3-12)cikloalkil, hetero(C3-12)cikloalkil, aril i heteroaril, pri čemu je svaki od njih nesupstituiran ili supstituiran sa jednim ili više supstituenata koji su izabrani iz grupe A.
6. Spoj prema bilo kojem od patentnih zahtjeva 1-5, naznačen time što je Y1 izabran iz grupe koju čine -CH2-, -NH-, -O- i -S-.
7. Spoj prema bilo kojem od patentnih zahtjeva 1-5, naznačen time što
Y1 je izabran iz grupe koju čine -O-, -(CR19R20)m-, -NR21-, -S i -S-CH2-;
m je izabran iz grupe koju čine 0, 1, 2, 3, 4 i 5;
R19 i R20 izabrani su iz grupe koju čine vodik, halo, cijano, tio, oksi, hidroksi, karboniloksi, alkoksi, ariloksi, heteroariloksi, karbonil, oksikarbonil, aminokarbonil, amino, (C1-10)alkilamino, sulfonamido, imino, sulfonil, sulfinil, (C1-10)alkil, halo(C1-10)alkil, karbonil(C1-3)alkil, tiokarbonil(C1-3)alkil, sulfonil(C1-3)alkil, sulfinil(C1-3)alkil, amino (C1-10)alkil, imino(C1-3)alkil, (C3-12)cikloalkil(C1-5)alkil, hetero(C3-12)cikloalkil(C1-5)alkil, aril(C1-10)alkil, heteroaril(C1-5)alkil, (C9-12)bicikloaril(C1-5)alkil, hetero(C8-12)bicikloaril(C1-5)alkil, (C3-12)cikloalkil, hetero(C3-12)cikloalkil, (C9-12)bicikloalkil, hetero(C3-12)bicikloalkil, aril, heteroaril, (C9-12)bicikloaril i hetero(C4-12)bicikloaril, pri čemu je svaki od njih nesupstituiran ili supstituiran sa jednim ili više supstituenata koji su izabrani iz grupe A, ili R19 i R12 su uzeti zajedno tako da formiraju prsten, nesupstituiran ili supstituiran sa jednim ili više supstituenata koji su izabrani iz grupe A; i
R21 je izabran iz grupe koju čine vodik, karboniloksi, alkoksi, ariloksi, heteroariloksi, karbonil, oksikarbonil, (C1-10)alkilamino, sulfonamido, imino, sulfonil, sulfinil, (C1-10)alkil, halo(C1-10)alkil, karbonil(C1-3)alkil, tiokarbonil(C1-3)alkil, sulfonil(C1-3)alkil, sulfinil(C1-3)alkil, amino (C1-10)alkil, imino(C1-3)alkil, (C3-12)cikloalkil(C1-5)alkil, hetero(C3-12)cikloalkil(C1-5)alkil, aril(C1-10)alkil, heteroaril(C1-5)alkil, (C9-12)bicikloaril(C1-5)alkil, hetero(C8-12)bicikloaril(C1-5)alkil, (C3-12)cikloalkil, hetero(C3-12)cikloalkil, (C9-12)bicikloalkil, hetero(C3-12)bicikloalkil, aril, heteroaril, (C9-12)bicikloaril i hetero(C4-12)bicikloaril, pri čemu je svaki od njih nesupstituiran ili supstituiran sa jednim ili više supstituenata koji su izabrani iz grupe A, ili R21 i R12 uzeti su zajedno tako da formiraju prsten, nesupstituiran ili supstituiran sa jednim ili više supstituenata izabranih iz grupe A.
8. Spoj prema patentnom zahtjevu 1 ili 2, naznačen time što je Y3 izabran iz grupe koju čine -CH2-, -NH-, -O- i -S-.
9. Spoj prema patentnom zahtjevu 1 ili 2, naznačen time što
Y3 je izabran iz grupe koju čine -O-, -(CR19R20)m-, -NR21-, -S i -S-CH2-;
m je izabran iz grupe koju čine 0, 1, 2, 3, 4 i 5;
R19 i R20 izabrani su iz grupe koju čine vodik, halo, cijano, tio, oksi, hidroksi, karboniloksi, alkoksi, ariloksi, heteroariloksi, karbonil, oksikarbonil, aminokarbonil, amino, (C1-10)alkilamino, sulfonamido, imino, sulfonil, sulfinil, (C1-10)alkil, halo(C1-10)alkil, karbonil(C1-3)alkil, tiokarbonil(C1-3)alkil, sulfonil(C1-3)alkil, sulfinil(C1-3)alkil, amino (C1-10)alkil, imino(C1-3)alkil, (C3-12)cikloalkil(C1-5)alkil, hetero(C3-12)cikloalkil(C1-5)alkil, aril(C1-10)alkil, heteroaril(C1-5)alkil, (C9-12)bicikloaril(C1-5)alkil, hetero(C8-12)bicikloaril(C1-5) alkil, (C3-12)cikloalkil, hetero(C3-12)cikloalkil, (C9-12)bicikloalkil, hetero(C3-12)bicikloalkil, aril, heteroaril, (C9-12)bicikloaril i hetero(C4-12)bicikloaril, pri čemu je svaki od njih nesupstituiran ili supstituiran sa jednim ili više supstituenata izabranih iz grupe A; i
R21 je izabran iz grupe koju čine vodik, karboniloksi, alkoksi, ariloksi, heteroariloksi, karbonil, oksikarbonil, (C1-10)alkilamino, sulfonamido, imino, sulfonil, sulfinil, (C1-10)alkil, halo(C1-10)alkil, karbonil (C1-3)alkil, tiokarbonil(C1-3)alkil, sulfonil(C1-3)alkil, sulfinil(C1-3)alkil, amino (C1-10)alkil, imino(C1-3)alkil, (C3-12)cikloalkil(C1-5)alkil, hetero(C3-12)cikloalkil(C1-5)alkil, aril(C1-10)alkil, heteroaril(C1-5)alkil, (C9-12)bicikloaril(C1-5)alkil, hetero(C8-12)bicydoaril(C1-5)alkil, (C3-12)cikloalkil, hetero(C3-12)cikloalkil, (C9-12)bicikloalkil, hetero(C3-12)bicikloalkil, aril, heteroaril, (C9-12)bicikloaril i hetero(C4-12)bicikloaril, pri čemu je svaki od njih nesupstituiran ili supstituiran sa jednim ili više supstituenata izabranih iz grupe A.
10. Spoj prema patentnom zahtjevu 1, naznačen time što, -Y3-R14 je izabran iz grupe koju čine aril, heteroaril, (C9-12)bicikloaril i hetero(C4-12)bicikloaril, pri čemu je svaki od njih nesupstituiran ili supstituiran sa jednim ili više supstituenata koji su izabrani iz grupe A.
11. Spoj prema bilo kojem od patentnih zahtjeva 1-5 i 8-10, naznačen time što je R1 izabran iz grupe koju čine vodik, halo, amino, alkoksi, karboniloksi, aminokarbonil, sulfonil, karbonilamino, sulfonilamino, (C1-10)alkil, hetero(C3-12)cikloalkil i aril, pri čemu je svaki od njih nesupstituiran ili supstituiran sa jednim ili više supstituenata koji su izabrani iz grupe A.
12. Spoj prema bilo kojem od patentnih zahtjeva 1-11, naznačen time što je R2 izabran iz grupe koju čine vodik, halo, amino, alkoksi, (C1-10)alkil, hetero(C3-12)cikloalkil i aril, pri čemu je svaki od njih nesupstituiran ili supstituiran sa jednim ili više supstituenata koji su izabrani iz grupe A.
13. Spoj prema bilo kojem od patentnih zahtjeva 1-12, naznačen time što je R4 izabran iz grupe koju čine vodik, halo i (C1-5)alkil, nesupstituiran ili supstituiran sa jednim ili više supstituenata koji su izabrani iz grupe A.
14. Spoj prema bilo kojem od patentnih zahtjeva 1-12, naznačen time što, R4 je metil.
15. Spoj prema bilo kojem od patentnih zahtjeva 1-12, naznačen time što, R4 je trifluorometil.
16. Spoj prema bilo kojem od patentnih zahtjeva 1-15, naznačen time što, R6 je izabran iz grupe koju čine metil, etil, izopropil i ciklopropil, pri čemu je svaki od njih nesupstituiran ili supstituiran sa jednim ili više supstituenata koji su izabrani iz grupe A.
17. Spoj prema bilo kojem od patentnih zahtjeva 1-10 i 12-16, naznačen time što, R12 je izabran iz grupe koju čine vodik, halo, amino, alkoksi, karboniloksi, aminokarbonil, sulfonil, karbonilamino, sulfonilamino, (C1-10)alkil, hetero(C3-12)cikloalkil i aril, pri čemu je svaki od njih nesupstituiran ili supstituiran sa jednim ili više supstituenata koji su izabrani iz grupe A.
18. Spoj prema bilo kojem od patentnih zahtjeva 1-11 i 13-17, naznačen time što, R13 je izabran iz grupe koju čine vodik, halo, amino, alkoksi, karboniloksi, aminokarbonil, sulfonil, karbonilamino, sulfonilamino, (C1-10)alkil, hetero(C3-12)cikloalkil i aril, pri čemu je svaki od njih nesupstituiran ili supstituiran sa jednim ili više supstituenata koji su izabrani iz grupe A.
19. Spoj prema patentnom zahtjevu 1, naznačen time što je izabran iz grupe koju čine:
5-fenil-9H-pirido[2,3-b]indol;
5-(3-(metilsulfonil)fenil)-9H-pirido[2,3-b]indol;
5-(3-(etilsulfonil)fenil)-9H-pirido[2,3-b]indol;
N-(3-(9H-pirido[2,3-b]indol-5-il)fenil)etansulfonamid;
5-m-tolil-9H-pirido[2,3-b]indol;
N-ciklopropil-3-(9H-pirido[2,3-b]indol-5-il)benzensulfonamid;
5-(3-metoksifenil)-9H-pirido[2,3-b]indol;
5-(3-(etilsulfonil)fenil)-8-metil-9H-pirido[2,3-b]indol;
5-(3-(etilsulfonil)fenil)-3,8-dimetil-9H-pirido[2,3-b]indol;
N-(4-(9H-pirido[2,3-b]indol-5-iltio)fenil)acetamid;
5-(benziltio)-9H-pirido[2,3-b]indol;
5-(feniltio)-9H-pirido[2,3-b]indol; i
5-(benziltio)-8-metil-9H-pirido[2,3-b]indol.
20. Farmaceutska kompozicija naznačena time što sadrži, kao aktivni sastojak, spoj prema bilo kojem od patentnih zahtjeva 1-19.
21. Spoj prema bilo kojem od patentnih zahtjeva 1-19, naznačen time, što se koristi za primjenu kao lijek.
22. Spoj prema bilo kojem od patentnih zahtjeva 1-19, naznačen time što se koristi za primjenu u liječenju kancera kod sisavaca.
23. Spoj prema patentnom zahtjevu 22, naznačeno time što je kancer izabran iz grupe koju čine karcinom skvamoznih stanica, astrocitom, Kapošijev sarkom, glioblastom, kancer ne-malih stanica pluća, kancer bešike, kancer glave i vrata, melanom, kancer jajnika, kancer prostate, kancer dojke, kancer malih stanica pluća, gliom, kolorektalni kancer, genitourinarni kancer, gastrointestinalni kancer, kancer tireoideje i kancer kože.
24. Spoj prema bilo kojem od patentnih zahtjeva 1-19, naznačen time što se koristi za primjenu u liječenju inflamacije, inflamatorne bolesti crijeva, psolrijaze ili odbacivanja transplanta kod sisavaca.
25. Spoj prema bilo kojem od patentnih zahtjeva 1-19, naznačen time što se koristi za primjenu u prevenciji ili liječenju amiotrofne lateralne skleroze, kortikobazalne degeneracije, Down-ovog sindroma, Huntington-ove bolesti, Parkinsoln-ove bolesti, post-encefalitičnog parkinsolnizma, progresivne supranuklearne paralize, Pick-ove bolesti, Niemann-Pick-ove bolesti, moždanog udara, traume glave i drugih kroničnih neurodegenerativnih bolesti, bipolarne bolesti, afektivnih poremećaja, depresije, šizofrenije, kognitivnih poremećaja, gubitka kose i kod primjene kontraceptivnih lijekova kod sisavaca.
26. Spoj prema bilo kojem od patentnih zahtjeva 1-19, naznačen time što se koristi za primjenu u prevenciji ili liječenju blagog oštećenja kognitivnih funkcija, oštećenja pamćenja povezanog sa starenjem, opadanja kognitivnih funkcija povezanog sa starenjem, oštećenja kognitivnih funkcija bez demencije, blagog opadanja kognitivnih funkcija, blagog opadanja neurokognitivnih funkcija, zaboravnosti u kasnom životu, oštećenja pamćenja i oštećenja kognitivnih funkcija i androgenetičke alopecije kod sisavaca.
27. Spoj prema bilo kojem od patentnih zahtjeva 1-19, naznačen time što se koristi za primjenu u prevenciji ili liječenju bolesti povezanih sa demencijom, Alzheimer-ove bolesti i stanja povezanih sa kinazama kod sisavaca.
28. Spoj prema patentnom zahtjevu 27, naznačen time što su bolesti povezane sa demencijom izabrane iz grupe koju čine frontotemporalna demencija Parkinsoln-ovog tipa, parkinsolnizam – demencija kojempleks Guam-a, HIV demencija, bolesti sa povezanim neurofibrilarnim čvorovima, predementna stanja, vaskularna demencija, demencija sa Lewy-jevim tijelima, frontotemporalna demencija i dementia pugilistica.
29. Spoj prema bilo kojem od patentnih zahtjeva 1-19, naznačen time što se koristi za primjenu u liječenju artritisa kod sisavaca.
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- 2006-10-10 EP EP06816697A patent/EP1931669A1/en not_active Withdrawn
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