BRPI0619517A2

BRPI0619517A2 - ácidos pirazolo[1,5-a]piridina-3-carboxìlicos como inibidores de ephb e vegfr2 cinase

ácidos pirazolo[1,5-a]piridina-3-carboxìlicos como inibidores de ephb e vegfr2 cinase Download PDF

Info

Publication number: BRPI0619517A2
Authority: BR; Brazil
Prior art keywords: alkyl; formula; phenyl; substituted; unsubstituted
Prior art date: 2005-12-08

Application number

BRPI0619517-2A

Other languages

English (en)

Portuguese (pt)

Inventor

Patricia Imbach

Philipp Holzer

Pascal Furet

Original Assignee

Novartis Ag

Priority date

2005-12-08

Filing date

2006-12-06

Publication date

2011-10-04

2005-12-08 Priority claimed from GB0525065A external-priority patent/GB0525065D0/en

2006-01-17 Priority claimed from GB0600931A external-priority patent/GB0600931D0/en

2006-12-06 Application filed by Novartis Ag filed Critical Novartis Ag

2011-10-04 Publication of BRPI0619517A2 publication Critical patent/BRPI0619517A2/pt

Links

HRSDPDBQVZHCRC-UHFFFAOYSA-N pyrazolo[1,5-a]pyridine-3-carboxylic acid Chemical class C1=CC=CC2=C(C(=O)O)C=NN21 HRSDPDBQVZHCRC-UHFFFAOYSA-N 0.000 title claims abstract description 4
239000003112 inhibitor Substances 0.000 title description 25
102000016549 Vascular Endothelial Growth Factor Receptor-2 Human genes 0.000 title 1
150000003839 salts Chemical class 0.000 claims abstract description 78
239000002253 acid Substances 0.000 claims abstract description 24
150000001875 compounds Chemical class 0.000 claims description 265
-1 phenoxy, naphthyloxy, phenyl Chemical group 0.000 claims description 140
125000000217 alkyl group Chemical group 0.000 claims description 98
208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 98
201000010099 disease Diseases 0.000 claims description 83
229910052757 nitrogen Inorganic materials 0.000 claims description 75
229910052739 hydrogen Inorganic materials 0.000 claims description 69
239000001257 hydrogen Substances 0.000 claims description 69
238000011282 treatment Methods 0.000 claims description 58
102000001253 Protein Kinase Human genes 0.000 claims description 56
108060006633 protein kinase Proteins 0.000 claims description 55
238000000034 method Methods 0.000 claims description 52
125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 52
150000002431 hydrogen Chemical group 0.000 claims description 50
230000005764 inhibitory process Effects 0.000 claims description 45
206010028980 Neoplasm Diseases 0.000 claims description 42
102000020233 phosphotransferase Human genes 0.000 claims description 41
108091000080 Phosphotransferase Proteins 0.000 claims description 40
238000006243 chemical reaction Methods 0.000 claims description 38
108090000623 proteins and genes Proteins 0.000 claims description 37
125000003107 substituted aryl group Chemical group 0.000 claims description 37
125000001424 substituent group Chemical group 0.000 claims description 36
102000004169 proteins and genes Human genes 0.000 claims description 33
125000000623 heterocyclic group Chemical group 0.000 claims description 32
125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims description 31
102000004022 Protein-Tyrosine Kinases Human genes 0.000 claims description 28
108090000412 Protein-Tyrosine Kinases Proteins 0.000 claims description 28
125000000547 substituted alkyl group Chemical group 0.000 claims description 28
229910052717 sulfur Inorganic materials 0.000 claims description 28
229910052760 oxygen Inorganic materials 0.000 claims description 27
125000003545 alkoxy group Chemical group 0.000 claims description 26
IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims description 25
239000000203 mixture Substances 0.000 claims description 23
125000001624 naphthyl group Chemical group 0.000 claims description 23
125000005346 substituted cycloalkyl group Chemical group 0.000 claims description 22
GLUUGHFHXGJENI-UHFFFAOYSA-N Piperazine Chemical compound C1CNCCN1 GLUUGHFHXGJENI-UHFFFAOYSA-N 0.000 claims description 21
125000004432 carbon atom Chemical group C* 0.000 claims description 21
241001465754 Metazoa Species 0.000 claims description 20
125000004356 hydroxy functional group Chemical group O* 0.000 claims description 19
201000011510 cancer Diseases 0.000 claims description 18
239000003446 ligand Substances 0.000 claims description 17
230000008569 process Effects 0.000 claims description 17
OUYCCCASQSFEME-QMMMGPOBSA-N L-tyrosine Chemical compound OC(=O)[C@@H](N)CC1=CC=C(O)C=C1 OUYCCCASQSFEME-QMMMGPOBSA-N 0.000 claims description 15
125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 claims description 15
UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 14
238000004519 manufacturing process Methods 0.000 claims description 14
239000000825 pharmaceutical preparation Substances 0.000 claims description 14
230000002062 proliferating effect Effects 0.000 claims description 14
WKBOTKDWSSQWDR-UHFFFAOYSA-N Bromine atom Chemical compound [Br] WKBOTKDWSSQWDR-UHFFFAOYSA-N 0.000 claims description 13
GDTBXPJZTBHREO-UHFFFAOYSA-N bromine Substances BrBr GDTBXPJZTBHREO-UHFFFAOYSA-N 0.000 claims description 13
229910052794 bromium Inorganic materials 0.000 claims description 13
OUYCCCASQSFEME-UHFFFAOYSA-N tyrosine Natural products OC(=O)C(N)CC1=CC=C(O)C=C1 OUYCCCASQSFEME-UHFFFAOYSA-N 0.000 claims description 13
102000050554 Eph Family Receptors Human genes 0.000 claims description 12
108091008815 Eph receptors Proteins 0.000 claims description 12
125000005153 alkyl sulfamoyl group Chemical group 0.000 claims description 12
125000001589 carboacyl group Chemical group 0.000 claims description 12
229910052799 carbon Inorganic materials 0.000 claims description 12
239000000460 chlorine Substances 0.000 claims description 12
208000035475 disorder Diseases 0.000 claims description 12
125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims description 12
125000002252 acyl group Chemical class 0.000 claims description 11
125000004397 aminosulfonyl group Chemical group NS(=O)(=O)* 0.000 claims description 11
230000015572 biosynthetic process Effects 0.000 claims description 11
125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 11
ZAMOUSCENKQFHK-UHFFFAOYSA-N Chlorine atom Chemical compound [Cl] ZAMOUSCENKQFHK-UHFFFAOYSA-N 0.000 claims description 10
230000033115 angiogenesis Effects 0.000 claims description 10
125000003118 aryl group Chemical group 0.000 claims description 10
229910052801 chlorine Inorganic materials 0.000 claims description 10
125000004093 cyano group Chemical group *C#N 0.000 claims description 10
229910052740 iodine Inorganic materials 0.000 claims description 10
208000032839 leukemia Diseases 0.000 claims description 10
108091008605 VEGF receptors Proteins 0.000 claims description 9
125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims description 9
RWRDLPDLKQPQOW-UHFFFAOYSA-N Pyrrolidine Chemical compound C1CCNC1 RWRDLPDLKQPQOW-UHFFFAOYSA-N 0.000 claims description 8
102000009484 Vascular Endothelial Growth Factor Receptors Human genes 0.000 claims description 8
230000001131 transforming effect Effects 0.000 claims description 8
125000004390 alkyl sulfonyl group Chemical group 0.000 claims description 7
125000003236 benzoyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C(*)=O 0.000 claims description 7
125000003170 phenylsulfonyl group Chemical group C1(=CC=CC=C1)S(=O)(=O)* 0.000 claims description 7
125000003373 pyrazinyl group Chemical group 0.000 claims description 7
125000000020 sulfo group Chemical group O=S(=O)([*])O[H] 0.000 claims description 7
208000032791 BCR-ABL1 positive chronic myelogenous leukemia Diseases 0.000 claims description 6
108010069682 CSK Tyrosine-Protein Kinase Proteins 0.000 claims description 6
125000004453 alkoxycarbonyl group Chemical class 0.000 claims description 6
125000004414 alkyl thio group Chemical group 0.000 claims description 6
BVKZGUZCCUSVTD-UHFFFAOYSA-N carbonic acid Chemical compound OC(O)=O BVKZGUZCCUSVTD-UHFFFAOYSA-N 0.000 claims description 6
239000003937 drug carrier Substances 0.000 claims description 6
230000003211 malignant effect Effects 0.000 claims description 6
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 description 6
125000001038 naphthoyl group Chemical group C1(=CC=CC2=CC=CC=C12)C(=O)* 0.000 claims description 6
230000001537 neural effect Effects 0.000 claims description 6
230000004770 neurodegeneration Effects 0.000 claims description 6
230000008929 regeneration Effects 0.000 claims description 6
238000011069 regeneration method Methods 0.000 claims description 6
208000037803 restenosis Diseases 0.000 claims description 6
ZCYVEMRRCGMTRW-UHFFFAOYSA-N 7553-56-2 Chemical compound [I] ZCYVEMRRCGMTRW-UHFFFAOYSA-N 0.000 claims description 5
102000029330 CSK Tyrosine-Protein Kinase Human genes 0.000 claims description 5
101100381481 Caenorhabditis elegans baz-2 gene Proteins 0.000 claims description 5
102100031968 Ephrin type-B receptor 2 Human genes 0.000 claims description 5
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201000004681 Psoriasis Diseases 0.000 claims description 5
108091008551 RET receptors Proteins 0.000 claims description 5
101100372762 Rattus norvegicus Flt1 gene Proteins 0.000 claims description 5
150000001721 carbon Chemical group 0.000 claims description 5
230000007850 degeneration Effects 0.000 claims description 5
125000004435 hydrogen atom Chemical group [H]* 0.000 claims description 5
239000011630 iodine Substances 0.000 claims description 5
125000004573 morpholin-4-yl group Chemical group N1(CCOCC1)* 0.000 claims description 5
239000011664 nicotinic acid Substances 0.000 claims description 5
QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims description 5
230000035755 proliferation Effects 0.000 claims description 5
210000002307 prostate Anatomy 0.000 claims description 5
239000000523 sample Substances 0.000 claims description 5
229920006395 saturated elastomer Polymers 0.000 claims description 5
125000005420 sulfonamido group Chemical group S(=O)(=O)(N*)* 0.000 claims description 5
238000003786 synthesis reaction Methods 0.000 claims description 5
125000005505 thiomorpholino group Chemical group 0.000 claims description 5
125000004178 (C1-C4) alkyl group Chemical group 0.000 claims description 4
201000001320 Atherosclerosis Diseases 0.000 claims description 4
OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical group [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims description 4
208000034578 Multiple myelomas Diseases 0.000 claims description 4
206010035226 Plasma cell myeloma Diseases 0.000 claims description 4
QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical group [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims description 4
125000000499 benzofuranyl group Chemical group O1C(=CC2=C1C=CC=C2)* 0.000 claims description 4
125000002619 bicyclic group Chemical group 0.000 claims description 4
210000004556 brain Anatomy 0.000 claims description 4
210000000481 breast Anatomy 0.000 claims description 4
206010020718 hyperplasia Diseases 0.000 claims description 4
208000027866 inflammatory disease Diseases 0.000 claims description 4
210000004185 liver Anatomy 0.000 claims description 4
201000001441 melanoma Diseases 0.000 claims description 4
125000002950 monocyclic group Chemical group 0.000 claims description 4
125000005146 naphthylsulfonyl group Chemical group C1(=CC=CC2=CC=CC=C12)S(=O)(=O)* 0.000 claims description 4
125000005029 naphthylthio group Chemical group C1(=CC=CC2=CC=CC=C12)S* 0.000 claims description 4
125000003356 phenylsulfanyl group Chemical group [*]SC1=C([H])C([H])=C([H])C([H])=C1[H] 0.000 claims description 4
125000006413 ring segment Chemical group 0.000 claims description 4
230000001225 therapeutic effect Effects 0.000 claims description 4
206010025323 Lymphomas Diseases 0.000 claims description 3
PVNIIMVLHYAWGP-UHFFFAOYSA-N Niacin Chemical compound OC(=O)C1=CC=CN=C1 PVNIIMVLHYAWGP-UHFFFAOYSA-N 0.000 claims description 3
210000003050 axon Anatomy 0.000 claims description 3
125000003785 benzimidazolyl group Chemical group N1=C(NC2=C1C=CC=C2)* 0.000 claims description 3
210000004204 blood vessel Anatomy 0.000 claims description 3
125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 claims description 3
230000004761 fibrosis Effects 0.000 claims description 3
210000003734 kidney Anatomy 0.000 claims description 3
210000004072 lung Anatomy 0.000 claims description 3
125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims description 3
230000009689 neuronal regeneration Effects 0.000 claims description 3
210000001672 ovary Anatomy 0.000 claims description 3
239000001301 oxygen Chemical group 0.000 claims description 3
210000000496 pancreas Anatomy 0.000 claims description 3
125000000951 phenoxy group Chemical group [H]C1=C([H])C([H])=C(O*)C([H])=C1[H] 0.000 claims description 3
125000002294 quinazolinyl group Chemical group N1=C(N=CC2=CC=CC=C12)* 0.000 claims description 3
230000008054 signal transmission Effects 0.000 claims description 3
230000000638 stimulation Effects 0.000 claims description 3
210000002784 stomach Anatomy 0.000 claims description 3
125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 claims description 3
125000003831 tetrazolyl group Chemical group 0.000 claims description 3
125000001544 thienyl group Chemical group 0.000 claims description 3
210000003932 urinary bladder Anatomy 0.000 claims description 3
125000002471 4H-quinolizinyl group Chemical group C=1(C=CCN2C=CC=CC12)* 0.000 claims description 2
CJPZOHYELJKKEL-UHFFFAOYSA-N 6-(3,4-dimethoxyphenyl)-n-(2-methylphenyl)pyrazolo[1,5-a]pyridine-3-carboxamide Chemical compound C1=C(OC)C(OC)=CC=C1C1=CN2N=CC(C(=O)NC=3C(=CC=CC=3)C)=C2C=C1 CJPZOHYELJKKEL-UHFFFAOYSA-N 0.000 claims description 2
201000009030 Carcinoma Diseases 0.000 claims description 2
208000011231 Crohn disease Diseases 0.000 claims description 2
206010012689 Diabetic retinopathy Diseases 0.000 claims description 2
201000009273 Endometriosis Diseases 0.000 claims description 2
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206010039710 Scleroderma Diseases 0.000 claims description 2
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NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical group [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 claims description 2
208000007536 Thrombosis Diseases 0.000 claims description 2
206010052779 Transplant rejections Diseases 0.000 claims description 2
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125000000641 acridinyl group Chemical group C1(=CC=CC2=NC3=CC=CC=C3C=C12)* 0.000 claims description 2
125000003277 amino group Chemical group 0.000 claims description 2
238000002399 angioplasty Methods 0.000 claims description 2
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125000004069 aziridinyl group Chemical group 0.000 claims description 2
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ZADPBFCGQRWHPN-UHFFFAOYSA-N boronic acid Chemical compound OBO ZADPBFCGQRWHPN-UHFFFAOYSA-N 0.000 claims description 2
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125000000609 carbazolyl group Chemical group C1(=CC=CC=2C3=CC=CC=C3NC12)* 0.000 claims description 2
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210000003679 cervix uteri Anatomy 0.000 claims description 2
208000023819 chronic asthma Diseases 0.000 claims description 2
208000037976 chronic inflammation Diseases 0.000 claims description 2
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230000007882 cirrhosis Effects 0.000 claims description 2
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125000000753 cycloalkyl group Chemical group 0.000 claims description 2
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210000004696 endometrium Anatomy 0.000 claims description 2
125000003838 furazanyl group Chemical group 0.000 claims description 2
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125000002883 imidazolyl group Chemical group 0.000 claims description 2
210000000987 immune system Anatomy 0.000 claims description 2
125000003453 indazolyl group Chemical group N1N=C(C2=C1C=CC=C2)* 0.000 claims description 2
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125000001041 indolyl group Chemical group 0.000 claims description 2
125000001977 isobenzofuranyl group Chemical group C=1(OC=C2C=CC=CC12)* 0.000 claims description 2
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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 description 2
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125000004934 phenanthridinyl group Chemical group C1(=CC=CC2=NC=C3C=CC=CC3=C12)* 0.000 claims description 2
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125000000587 piperidin-1-yl group Chemical group [H]C1([H])N(*)C([H])([H])C([H])([H])C([H])([H])C1([H])[H] 0.000 claims description 2
125000001042 pteridinyl group Chemical group N1=C(N=CC2=NC=CN=C12)* 0.000 claims description 2
125000000561 purinyl group Chemical group N1=C(N=C2N=CNC2=C1)* 0.000 claims description 2
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VOZRGVOHRTXRBW-UHFFFAOYSA-N 6-(4-methoxyphenyl)-n-(2-methylphenyl)pyrazolo[1,5-a]pyridine-3-carboxamide Chemical compound C1=CC(OC)=CC=C1C1=CN2N=CC(C(=O)NC=3C(=CC=CC=3)C)=C2C=C1 VOZRGVOHRTXRBW-UHFFFAOYSA-N 0.000 claims 1
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