RU2008127263A - ПИРАЗОЛ [1,5-a] ПИРИДИН-3-КАРБОНОВЫЕ КИСЛОТЫ В КАЧЕСТВЕ ИНГИБИТОРОВ EphB-И VEGFR2-КИНАЗЫ - Google Patents
ПИРАЗОЛ [1,5-a] ПИРИДИН-3-КАРБОНОВЫЕ КИСЛОТЫ В КАЧЕСТВЕ ИНГИБИТОРОВ EphB-И VEGFR2-КИНАЗЫ Download PDFInfo
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- RU2008127263A RU2008127263A RU2008127263/04A RU2008127263A RU2008127263A RU 2008127263 A RU2008127263 A RU 2008127263A RU 2008127263/04 A RU2008127263/04 A RU 2008127263/04A RU 2008127263 A RU2008127263 A RU 2008127263A RU 2008127263 A RU2008127263 A RU 2008127263A
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- Prior art keywords
- alkyl
- unsubstituted
- substituted
- phenyl
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- PVNIIMVLHYAWGP-UHFFFAOYSA-N Niacin Chemical class OC(=O)C1=CC=CN=C1 PVNIIMVLHYAWGP-UHFFFAOYSA-N 0.000 title claims 13
- 235000001968 nicotinic acid Nutrition 0.000 title claims 7
- WTKZEGDFNFYCGP-UHFFFAOYSA-N Pyrazole Chemical compound C=1C=NNC=1 WTKZEGDFNFYCGP-UHFFFAOYSA-N 0.000 title 1
- 239000003112 inhibitor Substances 0.000 title 1
- 125000000217 alkyl group Chemical group 0.000 claims abstract 54
- 150000001875 compounds Chemical class 0.000 claims abstract 24
- 229910052739 hydrogen Inorganic materials 0.000 claims abstract 21
- 239000001257 hydrogen Substances 0.000 claims abstract 21
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims abstract 21
- 229910052736 halogen Inorganic materials 0.000 claims abstract 17
- 150000002367 halogens Chemical group 0.000 claims abstract 17
- 229910052757 nitrogen Inorganic materials 0.000 claims abstract 17
- 125000003107 substituted aryl group Chemical group 0.000 claims abstract 17
- 125000000547 substituted alkyl group Chemical group 0.000 claims abstract 15
- 125000000623 heterocyclic group Chemical group 0.000 claims abstract 14
- 125000005346 substituted cycloalkyl group Chemical group 0.000 claims abstract 12
- 229910052717 sulfur Inorganic materials 0.000 claims abstract 10
- 125000004093 cyano group Chemical group *C#N 0.000 claims abstract 9
- 229910052760 oxygen Inorganic materials 0.000 claims abstract 9
- 125000005153 alkyl sulfamoyl group Chemical group 0.000 claims abstract 8
- 125000004432 carbon atom Chemical group C* 0.000 claims abstract 8
- 125000004397 aminosulfonyl group Chemical group NS(=O)(=O)* 0.000 claims abstract 5
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims abstract 4
- 125000002252 acyl group Chemical group 0.000 claims abstract 2
- 125000003118 aryl group Chemical group 0.000 claims abstract 2
- -1 phenoxy , naphthoxy groups Chemical group 0.000 claims 30
- 125000003545 alkoxy group Chemical group 0.000 claims 21
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 19
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 18
- 125000001424 substituent group Chemical group 0.000 claims 17
- 201000010099 disease Diseases 0.000 claims 16
- 125000001624 naphthyl group Chemical group 0.000 claims 16
- 125000003277 amino group Chemical group 0.000 claims 13
- 150000003839 salts Chemical group 0.000 claims 11
- 125000001589 carboacyl group Chemical group 0.000 claims 10
- 125000004390 alkyl sulfonyl group Chemical group 0.000 claims 9
- 206010028980 Neoplasm Diseases 0.000 claims 8
- 102000001253 Protein Kinase Human genes 0.000 claims 8
- 125000004453 alkoxycarbonyl group Chemical group 0.000 claims 8
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 8
- 125000004414 alkyl thio group Chemical group 0.000 claims 7
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 claims 7
- 108060006633 protein kinase Proteins 0.000 claims 7
- 239000011664 nicotinic acid Substances 0.000 claims 6
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 5
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 5
- VORCCRLLTRBNGY-UHFFFAOYSA-N n-(2-methylphenyl)pyridine-3-carboxamide Chemical compound CC1=CC=CC=C1NC(=O)C1=CC=CN=C1 VORCCRLLTRBNGY-UHFFFAOYSA-N 0.000 claims 5
- 230000008929 regeneration Effects 0.000 claims 5
- 238000011069 regeneration method Methods 0.000 claims 5
- 125000005843 halogen group Chemical group 0.000 claims 4
- 230000001537 neural effect Effects 0.000 claims 4
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 4
- 102000004022 Protein-Tyrosine Kinases Human genes 0.000 claims 3
- 108090000412 Protein-Tyrosine Kinases Proteins 0.000 claims 3
- 125000004644 alkyl sulfinyl group Chemical group 0.000 claims 3
- 125000003236 benzoyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C(*)=O 0.000 claims 3
- 201000011510 cancer Diseases 0.000 claims 3
- 229910052799 carbon Inorganic materials 0.000 claims 3
- 230000005764 inhibitory process Effects 0.000 claims 3
- 125000001038 naphthoyl group Chemical group C1(=CC=CC2=CC=CC=C12)C(=O)* 0.000 claims 3
- 125000003170 phenylsulfonyl group Chemical group C1(=CC=CC=C1)S(=O)(=O)* 0.000 claims 3
- 208000037803 restenosis Diseases 0.000 claims 3
- 125000000020 sulfo group Chemical group O=S(=O)([*])O[H] 0.000 claims 3
- GRJIABFMPQBAKK-UHFFFAOYSA-N 3-amino-4-methyl-n-[3-(trifluoromethyl)phenyl]benzamide Chemical compound C1=C(N)C(C)=CC=C1C(=O)NC1=CC=CC(C(F)(F)F)=C1 GRJIABFMPQBAKK-UHFFFAOYSA-N 0.000 claims 2
- UJOBWOGCFQCDNV-UHFFFAOYSA-N 9H-carbazole Chemical compound C1=CC=C2C3=CC=CC=C3NC2=C1 UJOBWOGCFQCDNV-UHFFFAOYSA-N 0.000 claims 2
- 201000001320 Atherosclerosis Diseases 0.000 claims 2
- WKBOTKDWSSQWDR-UHFFFAOYSA-N Bromine atom Chemical compound [Br] WKBOTKDWSSQWDR-UHFFFAOYSA-N 0.000 claims 2
- 206010016654 Fibrosis Diseases 0.000 claims 2
- 206010018364 Glomerulonephritis Diseases 0.000 claims 2
- 241001465754 Metazoa Species 0.000 claims 2
- 206010035226 Plasma cell myeloma Diseases 0.000 claims 2
- 201000004681 Psoriasis Diseases 0.000 claims 2
- DZBUGLKDJFMEHC-UHFFFAOYSA-N acridine Chemical compound C1=CC=CC2=CC3=CC=CC=C3N=C21 DZBUGLKDJFMEHC-UHFFFAOYSA-N 0.000 claims 2
- 125000004423 acyloxy group Chemical group 0.000 claims 2
- 125000003342 alkenyl group Chemical group 0.000 claims 2
- 125000005194 alkoxycarbonyloxy group Chemical group 0.000 claims 2
- 125000000304 alkynyl group Chemical group 0.000 claims 2
- 125000003785 benzimidazolyl group Chemical group N1=C(NC2=C1C=CC=C2)* 0.000 claims 2
- 125000000499 benzofuranyl group Chemical group O1C(=CC2=C1C=CC=C2)* 0.000 claims 2
- 125000001231 benzoyloxy group Chemical group C(C1=CC=CC=C1)(=O)O* 0.000 claims 2
- 125000002619 bicyclic group Chemical group 0.000 claims 2
- 210000004556 brain Anatomy 0.000 claims 2
- GDTBXPJZTBHREO-UHFFFAOYSA-N bromine Substances BrBr GDTBXPJZTBHREO-UHFFFAOYSA-N 0.000 claims 2
- 229910052794 bromium Inorganic materials 0.000 claims 2
- 125000004230 chromenyl group Chemical group O1C(C=CC2=CC=CC=C12)* 0.000 claims 2
- 208000035475 disorder Diseases 0.000 claims 2
- 208000027866 inflammatory disease Diseases 0.000 claims 2
- 208000014674 injury Diseases 0.000 claims 2
- 210000004185 liver Anatomy 0.000 claims 2
- 230000003211 malignant effect Effects 0.000 claims 2
- 238000000034 method Methods 0.000 claims 2
- 125000002950 monocyclic group Chemical group 0.000 claims 2
- 125000002757 morpholinyl group Chemical group 0.000 claims 2
- 125000005186 naphthyloxy group Chemical group C1(=CC=CC2=CC=CC=C12)O* 0.000 claims 2
- 125000005146 naphthylsulfonyl group Chemical group C1(=CC=CC2=CC=CC=C12)S(=O)(=O)* 0.000 claims 2
- 125000005029 naphthylthio group Chemical group C1(=CC=CC2=CC=CC=C12)S* 0.000 claims 2
- 230000035771 neuroregeneration Effects 0.000 claims 2
- 239000008194 pharmaceutical composition Substances 0.000 claims 2
- RDOWQLZANAYVLL-UHFFFAOYSA-N phenanthridine Chemical compound C1=CC=C2C3=CC=CC=C3C=NC2=C1 RDOWQLZANAYVLL-UHFFFAOYSA-N 0.000 claims 2
- 125000000951 phenoxy group Chemical group [H]C1=C([H])C([H])=C(O*)C([H])=C1[H] 0.000 claims 2
- 125000003356 phenylsulfanyl group Chemical group [*]SC1=C([H])C([H])=C([H])C([H])=C1[H] 0.000 claims 2
- 125000003386 piperidinyl group Chemical group 0.000 claims 2
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 2
- 125000003373 pyrazinyl group Chemical group 0.000 claims 2
- 125000000719 pyrrolidinyl group Chemical group 0.000 claims 2
- 150000003254 radicals Chemical class 0.000 claims 2
- 229920006395 saturated elastomer Polymers 0.000 claims 2
- 125000005420 sulfonamido group Chemical group S(=O)(=O)(N*)* 0.000 claims 2
- 125000004568 thiomorpholinyl group Chemical group 0.000 claims 2
- GVNVAWHJIKLAGL-UHFFFAOYSA-N 2-(cyclohexen-1-yl)cyclohexan-1-one Chemical compound O=C1CCCCC1C1=CCCCC1 GVNVAWHJIKLAGL-UHFFFAOYSA-N 0.000 claims 1
- JZIBVTUXIVIFGC-UHFFFAOYSA-N 2H-pyrrole Chemical compound C1C=CC=N1 JZIBVTUXIVIFGC-UHFFFAOYSA-N 0.000 claims 1
- ICFWMKHWGKSYOP-UHFFFAOYSA-N 3-amino-n-[4-methoxy-3-(trifluoromethyl)phenyl]-4-methylbenzamide Chemical compound C1=C(C(F)(F)F)C(OC)=CC=C1NC(=O)C1=CC=C(C)C(N)=C1 ICFWMKHWGKSYOP-UHFFFAOYSA-N 0.000 claims 1
- 125000004939 6-pyridyl group Chemical group N1=CC=CC=C1* 0.000 claims 1
- 208000032791 BCR-ABL1 positive chronic myelogenous leukemia Diseases 0.000 claims 1
- 206010004446 Benign prostatic hyperplasia Diseases 0.000 claims 1
- 101100381481 Caenorhabditis elegans baz-2 gene Proteins 0.000 claims 1
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical group [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims 1
- 201000009030 Carcinoma Diseases 0.000 claims 1
- PGLIUCLTXOYQMV-UHFFFAOYSA-N Cetirizine hydrochloride Chemical group Cl.Cl.C1CN(CCOCC(=O)O)CCN1C(C=1C=CC(Cl)=CC=1)C1=CC=CC=C1 PGLIUCLTXOYQMV-UHFFFAOYSA-N 0.000 claims 1
- ZAMOUSCENKQFHK-UHFFFAOYSA-N Chlorine atom Chemical compound [Cl] ZAMOUSCENKQFHK-UHFFFAOYSA-N 0.000 claims 1
- 101150065749 Churc1 gene Proteins 0.000 claims 1
- 208000011231 Crohn disease Diseases 0.000 claims 1
- 208000007342 Diabetic Nephropathies Diseases 0.000 claims 1
- 206010012689 Diabetic retinopathy Diseases 0.000 claims 1
- 201000009273 Endometriosis Diseases 0.000 claims 1
- 102000050554 Eph Family Receptors Human genes 0.000 claims 1
- 108091008815 Eph receptors Proteins 0.000 claims 1
- 102100031968 Ephrin type-B receptor 2 Human genes 0.000 claims 1
- DNXHEGUUPJUMQT-CBZIJGRNSA-N Estrone Chemical compound OC1=CC=C2[C@H]3CC[C@](C)(C(CC4)=O)[C@@H]4[C@@H]3CCC2=C1 DNXHEGUUPJUMQT-CBZIJGRNSA-N 0.000 claims 1
- 208000010412 Glaucoma Diseases 0.000 claims 1
- 208000022461 Glomerular disease Diseases 0.000 claims 1
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- 208000022559 Inflammatory bowel disease Diseases 0.000 claims 1
- 208000007766 Kaposi sarcoma Diseases 0.000 claims 1
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- 208000028389 Nerve injury Diseases 0.000 claims 1
- 208000008589 Obesity Diseases 0.000 claims 1
- 208000031481 Pathologic Constriction Diseases 0.000 claims 1
- 108091000080 Phosphotransferase Proteins 0.000 claims 1
- 208000004403 Prostatic Hyperplasia Diseases 0.000 claims 1
- 102100038239 Protein Churchill Human genes 0.000 claims 1
- 108091008551 RET receptors Proteins 0.000 claims 1
- 101100372762 Rattus norvegicus Flt1 gene Proteins 0.000 claims 1
- 108091005682 Receptor kinases Proteins 0.000 claims 1
- 208000017442 Retinal disease Diseases 0.000 claims 1
- 206010038923 Retinopathy Diseases 0.000 claims 1
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- 206010039710 Scleroderma Diseases 0.000 claims 1
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- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical group [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 claims 1
- 208000007536 Thrombosis Diseases 0.000 claims 1
- 206010052779 Transplant rejections Diseases 0.000 claims 1
- 108091008605 VEGF receptors Proteins 0.000 claims 1
- 102000009484 Vascular Endothelial Growth Factor Receptors Human genes 0.000 claims 1
- 208000027418 Wounds and injury Diseases 0.000 claims 1
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- 230000033115 angiogenesis Effects 0.000 claims 1
- 238000002399 angioplasty Methods 0.000 claims 1
- 206010003246 arthritis Diseases 0.000 claims 1
- 125000004429 atom Chemical group 0.000 claims 1
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical group [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims 1
- 125000004069 aziridinyl group Chemical group 0.000 claims 1
- 125000004045 azirinyl group Chemical group 0.000 claims 1
- 125000004196 benzothienyl group Chemical group S1C(=CC2=C1C=CC=C2)* 0.000 claims 1
- 210000004204 blood vessel Anatomy 0.000 claims 1
- ZADPBFCGQRWHPN-UHFFFAOYSA-N boronic acid Chemical compound OBO ZADPBFCGQRWHPN-UHFFFAOYSA-N 0.000 claims 1
- 201000008275 breast carcinoma Diseases 0.000 claims 1
- 125000003739 carbamimidoyl group Chemical group C(N)(=N)* 0.000 claims 1
- 125000002837 carbocyclic group Chemical group 0.000 claims 1
- 150000001721 carbon Chemical group 0.000 claims 1
- 150000001732 carboxylic acid derivatives Chemical class 0.000 claims 1
- 230000004663 cell proliferation Effects 0.000 claims 1
- 210000003169 central nervous system Anatomy 0.000 claims 1
- 230000008859 change Effects 0.000 claims 1
- 210000000038 chest Anatomy 0.000 claims 1
- 239000000460 chlorine Substances 0.000 claims 1
- 229910052801 chlorine Inorganic materials 0.000 claims 1
- 125000003016 chromanyl group Chemical group O1C(CCC2=CC=CC=C12)* 0.000 claims 1
- 208000023819 chronic asthma Diseases 0.000 claims 1
- 208000037976 chronic inflammation Diseases 0.000 claims 1
- 208000037893 chronic inflammatory disorder Diseases 0.000 claims 1
- 125000000259 cinnolinyl group Chemical group N1=NC(=CC2=CC=CC=C12)* 0.000 claims 1
- 230000007882 cirrhosis Effects 0.000 claims 1
- 208000019425 cirrhosis of liver Diseases 0.000 claims 1
- 210000001072 colon Anatomy 0.000 claims 1
- 201000002758 colorectal adenoma Diseases 0.000 claims 1
- 238000009833 condensation Methods 0.000 claims 1
- 230000005494 condensation Effects 0.000 claims 1
- 125000000753 cycloalkyl group Chemical group 0.000 claims 1
- 230000006378 damage Effects 0.000 claims 1
- 208000033679 diabetic kidney disease Diseases 0.000 claims 1
- IYYZUPMFVPLQIF-UHFFFAOYSA-N dibenzothiophene Chemical class C1=CC=C2C3=CC=CC=C3SC2=C1 IYYZUPMFVPLQIF-UHFFFAOYSA-N 0.000 claims 1
- 125000005303 dithiazolyl group Chemical group S1SNC(=C1)* 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 230000004761 fibrosis Effects 0.000 claims 1
- 239000012634 fragment Substances 0.000 claims 1
- 125000002541 furyl group Chemical group 0.000 claims 1
- 210000001035 gastrointestinal tract Anatomy 0.000 claims 1
- 208000005017 glioblastoma Diseases 0.000 claims 1
- 201000002222 hemangioblastoma Diseases 0.000 claims 1
- 201000011066 hemangioma Diseases 0.000 claims 1
- 125000005842 heteroatom Chemical group 0.000 claims 1
- 125000001183 hydrocarbyl group Chemical group 0.000 claims 1
- 206010020718 hyperplasia Diseases 0.000 claims 1
- 230000001146 hypoxic effect Effects 0.000 claims 1
- 125000002632 imidazolidinyl group Chemical group 0.000 claims 1
- 125000002883 imidazolyl group Chemical group 0.000 claims 1
- 210000000987 immune system Anatomy 0.000 claims 1
- 125000003453 indazolyl group Chemical group N1N=C(C2=C1C=CC=C2)* 0.000 claims 1
- 125000001041 indolyl group Chemical group 0.000 claims 1
- 125000001977 isobenzofuranyl group Chemical group C=1(OC=C2C=CC=CC12)* 0.000 claims 1
- 125000000904 isoindolyl group Chemical group C=1(NC=C2C=CC=CC12)* 0.000 claims 1
- 125000001786 isothiazolyl group Chemical group 0.000 claims 1
- 125000000842 isoxazolyl group Chemical group 0.000 claims 1
- 210000003734 kidney Anatomy 0.000 claims 1
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- 201000001441 melanoma Diseases 0.000 claims 1
- 210000003584 mesangial cell Anatomy 0.000 claims 1
- AFCCDDWKHLHPDF-UHFFFAOYSA-M metam-sodium Chemical compound [Na+].CNC([S-])=S AFCCDDWKHLHPDF-UHFFFAOYSA-M 0.000 claims 1
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 1
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- UFOJNUSJWKEEEQ-UHFFFAOYSA-N n-(3-amino-4-methylphenyl)-3-(trifluoromethyl)benzamide Chemical compound C1=C(N)C(C)=CC=C1NC(=O)C1=CC=CC(C(F)(F)F)=C1 UFOJNUSJWKEEEQ-UHFFFAOYSA-N 0.000 claims 1
- SYSQUGFVNFXIIT-UHFFFAOYSA-N n-[4-(1,3-benzoxazol-2-yl)phenyl]-4-nitrobenzenesulfonamide Chemical class C1=CC([N+](=O)[O-])=CC=C1S(=O)(=O)NC1=CC=C(C=2OC3=CC=CC=C3N=2)C=C1 SYSQUGFVNFXIIT-UHFFFAOYSA-N 0.000 claims 1
- 125000004593 naphthyridinyl group Chemical group N1=C(C=CC2=CC=CN=C12)* 0.000 claims 1
- 230000009826 neoplastic cell growth Effects 0.000 claims 1
- 201000009925 nephrosclerosis Diseases 0.000 claims 1
- 230000008764 nerve damage Effects 0.000 claims 1
- 230000000626 neurodegenerative effect Effects 0.000 claims 1
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims 1
- 235000020824 obesity Nutrition 0.000 claims 1
- 210000001672 ovary Anatomy 0.000 claims 1
- 125000002971 oxazolyl group Chemical group 0.000 claims 1
- 125000000466 oxiranyl group Chemical group 0.000 claims 1
- 239000001301 oxygen Chemical group 0.000 claims 1
- 210000000496 pancreas Anatomy 0.000 claims 1
- 125000005327 perimidinyl group Chemical group N1C(=NC2=CC=CC3=CC=CC1=C23)* 0.000 claims 1
- 210000001428 peripheral nervous system Anatomy 0.000 claims 1
- 125000001791 phenazinyl group Chemical group C1(=CC=CC2=NC3=CC=CC=C3N=C12)* 0.000 claims 1
- 125000001484 phenothiazinyl group Chemical group C1(=CC=CC=2SC3=CC=CC=C3NC12)* 0.000 claims 1
- 125000001644 phenoxazinyl group Chemical group C1(=CC=CC=2OC3=CC=CC=C3NC12)* 0.000 claims 1
- 102000020233 phosphotransferase Human genes 0.000 claims 1
- 125000004592 phthalazinyl group Chemical group C1(=NN=CC2=CC=CC=C12)* 0.000 claims 1
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- 230000002062 proliferating effect Effects 0.000 claims 1
- 230000035755 proliferation Effects 0.000 claims 1
- 210000002307 prostate Anatomy 0.000 claims 1
- CPNGPNLZQNNVQM-UHFFFAOYSA-N pteridine Chemical compound N1=CN=CC2=NC=CN=C21 CPNGPNLZQNNVQM-UHFFFAOYSA-N 0.000 claims 1
- 125000004309 pyranyl group Chemical group O1C(C=CC=C1)* 0.000 claims 1
- 125000003072 pyrazolidinyl group Chemical group 0.000 claims 1
- 125000003226 pyrazolyl group Chemical group 0.000 claims 1
- 125000002098 pyridazinyl group Chemical group 0.000 claims 1
- 125000004076 pyridyl group Chemical group 0.000 claims 1
- 125000000714 pyrimidinyl group Chemical group 0.000 claims 1
- 125000001422 pyrrolinyl group Chemical group 0.000 claims 1
- 125000002294 quinazolinyl group Chemical group N1=C(N=CC2=CC=CC=C12)* 0.000 claims 1
- 125000005493 quinolyl group Chemical group 0.000 claims 1
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- 208000011580 syndromic disease Diseases 0.000 claims 1
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 claims 1
- CWXPZXBSDSIRCS-UHFFFAOYSA-N tert-butyl piperazine-1-carboxylate Chemical compound CC(C)(C)OC(=O)N1CCNCC1 CWXPZXBSDSIRCS-UHFFFAOYSA-N 0.000 claims 1
- 125000003718 tetrahydrofuranyl group Chemical group 0.000 claims 1
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- AIFRHYZBTHREPW-UHFFFAOYSA-N β-carboline Chemical class N1=CC=C2C3=CC=CC=C3NC2=C1 AIFRHYZBTHREPW-UHFFFAOYSA-N 0.000 claims 1
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 abstract 2
- 125000001475 halogen functional group Chemical group 0.000 abstract 2
- 125000000229 (C1-C4)alkoxy group Chemical group 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
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| UA103006C2 (ru) | 2007-08-27 | 2013-09-10 | Басф Се | Пиразольные соединения для борьбы с бесхребетными вредителями |
| US8455477B2 (en) * | 2008-08-05 | 2013-06-04 | Merck Sharp & Dohme Corp. | Therapeutic compounds |
| KR101364869B1 (ko) | 2008-09-24 | 2014-02-21 | 바스프 에스이 | 무척추 해충을 방제하기 위한 피라졸 화합물 |
| BRPI0919085B1 (pt) | 2008-09-24 | 2021-05-11 | Basf Se | métodos não terapêuticos para controlar pragas invertebradas e para proteger material de propagação de plantas e/ou plantas que se desenvolvem dos mesmos, compostos de pirazol ou um sal ou um n-óxido dos mesmos, e, composição agrícola |
| EP2348860B1 (en) | 2008-10-31 | 2015-05-27 | Genentech, Inc. | Pyrazolopyrimidine jak inhibitor compounds and methods |
| UA110324C2 (en) | 2009-07-02 | 2015-12-25 | Genentech Inc | Jak inhibitory compounds based on pyrazolo pyrimidine |
| CN102471330A (zh) | 2009-07-06 | 2012-05-23 | 巴斯夫欧洲公司 | 用于防治无脊椎动物害虫的哒嗪化合物 |
| CN102471321A (zh) | 2009-07-06 | 2012-05-23 | 巴斯夫欧洲公司 | 用于防治无脊椎动物害虫的哒嗪化合物 |
| WO2011009804A2 (en) | 2009-07-24 | 2011-01-27 | Basf Se | Pyridine derivatives compounds for controlling invertebrate pests |
| CN105693720B (zh) | 2010-05-20 | 2019-01-18 | 阵列生物制药公司 | 作为trk激酶抑制剂的大环化合物 |
| UY34305A (es) | 2011-09-01 | 2013-04-30 | Novartis Ag | Derivados de heterociclos bicíclicos para el tratamiento de la hipertensión arterial pulmonar |
| CA2858958C (en) * | 2011-12-12 | 2016-10-04 | Dr. Reddy's Laboratories Ltd. | Substituted pyrazolo[1,5-a]pyridine as tropomyosin receptor kinase (trk) inhibitors |
| ES2655030T3 (es) | 2012-11-19 | 2018-02-16 | Novartis Ag | Compuestos y composiciones para el tratamiento de enfermedades parasitarias |
| US8871754B2 (en) | 2012-11-19 | 2014-10-28 | Irm Llc | Compounds and compositions for the treatment of parasitic diseases |
| US9073921B2 (en) | 2013-03-01 | 2015-07-07 | Novartis Ag | Salt forms of bicyclic heterocyclic derivatives |
| HRP20210935T1 (hr) | 2014-05-23 | 2021-08-06 | F. Hoffmann - La Roche Ag | Spojevi 5-kloro-2-difluorometoksifenil pirazolopirimidina koji predstavljaju inhibitore jak |
| NO2719005T3 (enExample) | 2014-07-28 | 2018-01-20 | ||
| CN105524058B (zh) * | 2014-10-21 | 2018-03-27 | 广州艾格生物科技有限公司 | 吡唑并[1,5‑a]吡啶类化合物及其应用 |
| DK3215511T3 (da) | 2014-11-06 | 2024-05-13 | Bial R&D Invest S A | Substituerede pyrazolo(1,5-a)pyrimidiner og deres anvendelse i behandlingen af medicinske lidelser |
| CA2966581A1 (en) | 2014-11-06 | 2016-05-12 | Lysosomal Therapeutics Inc. | Substituted pyrrolo[1,2-a]pyrimidines and their use in the treatment of medical disorders |
| ES2958391T3 (es) | 2014-11-06 | 2024-02-08 | Bial R&D Invest S A | Imidazo[1,5-a]pirimidinas sustituidas y su uso en el tratamiento de trastornos médicos |
| EP3322706B1 (en) | 2015-07-16 | 2020-11-11 | Array Biopharma, Inc. | Substituted pyrazolo[1,5-a]pyridine compounds as ret kinase inhibitors |
| JP7046827B2 (ja) | 2016-04-06 | 2022-04-04 | リソソーマル・セラピューティクス・インコーポレイテッド | イミダゾ［１，５－ａ］ピリミジニルカルボキサミド化合物および医学的障害の処置におけるその使用 |
| WO2017176960A1 (en) | 2016-04-06 | 2017-10-12 | Lysosomal Therapeutics Inc. | Pyrazolo[1,5-a]pyrimidinyl carboxamide compounds and their use in the treatment of medical disorders |
| WO2017176962A1 (en) | 2016-04-06 | 2017-10-12 | Lysosomal Therapeutics, Inc. | Pyrrolo[1,2-a]pyrimidinyl carboxamide compounds and their use in the treatment of medical disorders |
| US11345698B2 (en) | 2016-05-05 | 2022-05-31 | Bial—R&D Investments, S.A. | Substituted imidazo[1,2-a]pyridines, substituted imidazo[1,2-a]pyrazines, related compounds, and their use in the treatment of medical disorders |
| BR112018072552A8 (pt) | 2016-05-05 | 2023-03-14 | Lysosomal Therapeutics Inc | Compostos de imidazo [1,2-b]piridazinas e imidazo [1,5-b] piridazinas substituídas, composição farmacêutica que os compreende e seu uso no tratamento de distúrbios médicos |
| TWI704148B (zh) | 2016-10-10 | 2020-09-11 | 美商亞雷生物製藥股份有限公司 | 作為ｒｅｔ激酶抑制劑之經取代吡唑并[1,5-a]吡啶化合物 |
| JOP20190077A1 (ar) | 2016-10-10 | 2019-04-09 | Array Biopharma Inc | مركبات بيرازولو [1، 5-a]بيريدين بها استبدال كمثبطات كيناز ret |
| CN110267960B (zh) | 2017-01-18 | 2022-04-26 | 阿雷生物药品公司 | 作为RET激酶抑制剂的取代的吡唑并[1,5-a]吡嗪化合物 |
| WO2018136663A1 (en) | 2017-01-18 | 2018-07-26 | Array Biopharma, Inc. | Ret inhibitors |
| JOP20190213A1 (ar) | 2017-03-16 | 2019-09-16 | Array Biopharma Inc | مركبات حلقية ضخمة كمثبطات لكيناز ros1 |
| TW201902896A (zh) | 2017-05-22 | 2019-01-16 | 瑞士商赫孚孟拉羅股份公司 | 治療化合物及組合物及其使用方法 |
| TWI812649B (zh) | 2017-10-10 | 2023-08-21 | 美商絡速藥業公司 | 6-(2-羥基-2-甲基丙氧基)-4-(6-(6-((6-甲氧基吡啶-3-基)甲基)-3,6-二氮雜雙環[3.1.1]庚-3-基)吡啶-3-基)吡唑并[1,5-a]吡啶-3-甲腈之調配物 |
| TWI791053B (zh) | 2017-10-10 | 2023-02-01 | 美商亞雷生物製藥股份有限公司 | 6-(2-羥基-2-甲基丙氧基)-4-(6-(6-((6-甲氧基吡啶-3-基)甲基)-3,6-二氮雜雙環[3.1.1]庚-3-基)吡啶-3-基)吡唑并[1,5-a]吡啶-3-甲腈之結晶形式及其醫藥組合物 |
| WO2019143994A1 (en) | 2018-01-18 | 2019-07-25 | Array Biopharma Inc. | Substituted pyrazolyl[4,3-c]pyridinecompounds as ret kinase inhibitors |
| CN111971286B (zh) | 2018-01-18 | 2023-04-14 | 阿雷生物药品公司 | 作为RET激酶抑制剂的取代的吡咯并[2,3-d]嘧啶化合物 |
| TW201938169A (zh) | 2018-01-18 | 2019-10-01 | 美商亞雷生物製藥股份有限公司 | 作為RET激酶抑制劑之經取代吡唑并[3,4-d]嘧啶化合物 |
| ES2922314T3 (es) | 2018-09-10 | 2022-09-13 | Array Biopharma Inc | Compuestos heterocíclicos condensados como inhibidores de cinasa RET |
| CA3153096A1 (en) | 2019-09-13 | 2021-03-18 | The United States Of America, As Represented By The Secretary, Department Of Health And Human Services | Receptor tyrosine kinase inhibitors for treatment of protein kinase modulation-responsive disease or disorder |
| CN120677155A (zh) * | 2022-12-07 | 2025-09-19 | 第三谐波生物股份有限公司 | 作为c-Kit激酶抑制剂的化合物和组合物 |
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| US20050222171A1 (en) * | 2004-01-22 | 2005-10-06 | Guido Bold | Organic compounds |
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| US7795273B2 (en) | 2010-09-14 |
| KR20080074161A (ko) | 2008-08-12 |
| BRPI0619517A2 (pt) | 2011-10-04 |
| WO2007065664A2 (en) | 2007-06-14 |
| CA2629743A1 (en) | 2007-06-14 |
| WO2007065664A3 (en) | 2007-08-23 |
| AU2006322187A1 (en) | 2007-06-14 |
| US20080300245A1 (en) | 2008-12-04 |
| JP2009518340A (ja) | 2009-05-07 |
| EP1963316A2 (en) | 2008-09-03 |
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