JP2016505021A5 - - Google Patents
Download PDFInfo
- Publication number
- JP2016505021A5 JP2016505021A5 JP2015552897A JP2015552897A JP2016505021A5 JP 2016505021 A5 JP2016505021 A5 JP 2016505021A5 JP 2015552897 A JP2015552897 A JP 2015552897A JP 2015552897 A JP2015552897 A JP 2015552897A JP 2016505021 A5 JP2016505021 A5 JP 2016505021A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- pharmaceutically acceptable
- acceptable salt
- amino
- carboxamide
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Granted
Links
- 125000000217 alkyl group Chemical group 0.000 claims description 131
- 229910052736 halogen Inorganic materials 0.000 claims description 43
- 150000002367 halogens Chemical class 0.000 claims description 43
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims description 33
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims description 31
- 125000006272 (C3-C7) cycloalkyl group Chemical group 0.000 claims description 17
- 125000001313 C5-C10 heteroaryl group Chemical group 0.000 claims description 16
- 125000003118 aryl group Chemical group 0.000 claims description 13
- 125000006568 (C4-C7) heterocycloalkyl group Chemical group 0.000 claims description 6
- 238000006467 substitution reaction Methods 0.000 claims description 2
- 150000001875 compounds Chemical class 0.000 claims 103
- 150000003839 salts Chemical class 0.000 claims 93
- 125000001424 substituent group Chemical group 0.000 claims 38
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 claims 29
- 229910052799 carbon Inorganic materials 0.000 claims 26
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims 24
- 125000004432 carbon atom Chemical group C* 0.000 claims 17
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 15
- 125000005843 halogen group Chemical group 0.000 claims 13
- 206010028980 Neoplasm Diseases 0.000 claims 12
- 229910052739 hydrogen Inorganic materials 0.000 claims 12
- 201000011510 cancer Diseases 0.000 claims 10
- 125000003161 (C1-C6) alkylene group Chemical group 0.000 claims 9
- 239000003814 drug Substances 0.000 claims 9
- 229910052757 nitrogen Inorganic materials 0.000 claims 8
- -1 2,6-difluorophenyl Chemical group 0.000 claims 7
- 125000003349 3-pyridyl group Chemical group N1=C([H])C([*])=C([H])C([H])=C1[H] 0.000 claims 7
- 125000003545 alkoxy group Chemical group 0.000 claims 7
- 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 7
- 125000001072 heteroaryl group Chemical group 0.000 claims 6
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 6
- 206010028537 myelofibrosis Diseases 0.000 claims 5
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 5
- 125000004737 (C1-C6) haloalkoxy group Chemical group 0.000 claims 4
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 claims 4
- 125000005842 heteroatom Chemical group 0.000 claims 4
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 4
- 229910052760 oxygen Inorganic materials 0.000 claims 4
- 101100297651 Mus musculus Pim2 gene Proteins 0.000 claims 3
- 101150054691 PIM3 gene Proteins 0.000 claims 3
- 101150056413 Pim1 gene Proteins 0.000 claims 3
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 3
- 125000006413 ring segment Chemical group 0.000 claims 3
- 229910052717 sulfur Inorganic materials 0.000 claims 3
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 2
- WRTSMHBZVNBYRK-UHFFFAOYSA-N 3-amino-n-[4-(3-aminocyclohexyl)pyridin-3-yl]-7-ethylquinoline-2-carboxamide Chemical compound N=1C2=CC(CC)=CC=C2C=C(N)C=1C(=O)NC1=CN=CC=C1C1CCCC(N)C1 WRTSMHBZVNBYRK-UHFFFAOYSA-N 0.000 claims 2
- 208000032791 BCR-ABL1 positive chronic myelogenous leukemia Diseases 0.000 claims 2
- 208000010833 Chronic myeloid leukaemia Diseases 0.000 claims 2
- 208000033761 Myelogenous Chronic BCR-ABL Positive Leukemia Diseases 0.000 claims 2
- NQRYJNQNLNOLGT-UHFFFAOYSA-N Piperidine Chemical class C1CCNCC1 NQRYJNQNLNOLGT-UHFFFAOYSA-N 0.000 claims 2
- 208000017733 acquired polycythemia vera Diseases 0.000 claims 2
- 125000003342 alkenyl group Chemical group 0.000 claims 2
- 125000002947 alkylene group Chemical group 0.000 claims 2
- 201000010099 disease Diseases 0.000 claims 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 2
- 230000000694 effects Effects 0.000 claims 2
- 125000004438 haloalkoxy group Chemical group 0.000 claims 2
- 125000000623 heterocyclic group Chemical group 0.000 claims 2
- 208000026278 immune system disease Diseases 0.000 claims 2
- 208000037244 polycythemia vera Diseases 0.000 claims 2
- 208000003476 primary myelofibrosis Diseases 0.000 claims 2
- 125000003226 pyrazolyl group Chemical group 0.000 claims 2
- RWRDLPDLKQPQOW-UHFFFAOYSA-N tetrahydropyrrole Natural products C1CCNC1 RWRDLPDLKQPQOW-UHFFFAOYSA-N 0.000 claims 2
- 125000004214 1-pyrrolidinyl group Chemical group [H]C1([H])N(*)C([H])([H])C([H])([H])C1([H])[H] 0.000 claims 1
- JUMHXVDASNXZCK-UHFFFAOYSA-N 3-amino-n-[4-(3-amino-4-hydroxy-5-methylpiperidin-1-yl)-5-methylpyridin-3-yl]-7-ethylquinoline-2-carboxamide Chemical compound N=1C2=CC(CC)=CC=C2C=C(N)C=1C(=O)NC1=CN=CC(C)=C1N1CC(C)C(O)C(N)C1 JUMHXVDASNXZCK-UHFFFAOYSA-N 0.000 claims 1
- NKUFQFKOCYCIBU-UHFFFAOYSA-N 3-amino-n-[4-(3-amino-4-hydroxy-5-methylpiperidin-1-yl)pyridin-3-yl]-7-ethoxy-1,8-naphthyridine-2-carboxamide Chemical compound N=1C2=NC(OCC)=CC=C2C=C(N)C=1C(=O)NC1=CN=CC=C1N1CC(C)C(O)C(N)C1 NKUFQFKOCYCIBU-UHFFFAOYSA-N 0.000 claims 1
- GOMYQKXTHKSISF-UHFFFAOYSA-N 3-amino-n-[4-(3-amino-4-hydroxy-5-methylpiperidin-1-yl)pyridin-3-yl]-7-ethylquinoline-2-carboxamide Chemical compound N=1C2=CC(CC)=CC=C2C=C(N)C=1C(=O)NC1=CN=CC=C1N1CC(C)C(O)C(N)C1 GOMYQKXTHKSISF-UHFFFAOYSA-N 0.000 claims 1
- CDIASNJIOWVCSV-UHFFFAOYSA-N 3-amino-n-[4-(3-aminopiperidin-1-yl)-2,3-dihydrofuro[2,3-b]pyridin-5-yl]-7-ethylquinoline-2-carboxamide Chemical compound N=1C2=CC(CC)=CC=C2C=C(N)C=1C(=O)NC1=CN=C2OCCC2=C1N1CCCC(N)C1 CDIASNJIOWVCSV-UHFFFAOYSA-N 0.000 claims 1
- QSUWTJZUEPZOOX-UHFFFAOYSA-N 3-amino-n-[4-(3-aminopiperidin-1-yl)-5-cyanopyridin-3-yl]-7-ethylquinoline-2-carboxamide Chemical compound N=1C2=CC(CC)=CC=C2C=C(N)C=1C(=O)NC1=CN=CC(C#N)=C1N1CCCC(N)C1 QSUWTJZUEPZOOX-UHFFFAOYSA-N 0.000 claims 1
- PCBLQWCMPHDPQE-UHFFFAOYSA-N 3-amino-n-[4-(3-aminopiperidin-1-yl)-5-methylpyridin-3-yl]-7-ethylquinoline-2-carboxamide Chemical compound N=1C2=CC(CC)=CC=C2C=C(N)C=1C(=O)NC1=CN=CC(C)=C1N1CCCC(N)C1 PCBLQWCMPHDPQE-UHFFFAOYSA-N 0.000 claims 1
- QQULFRBGXNZCES-UHFFFAOYSA-N 3-amino-n-[4-(3-aminopiperidin-1-yl)-7-hydroxy-6,7-dihydro-5h-cyclopenta[b]pyridin-3-yl]-7-ethylquinoline-2-carboxamide Chemical compound N=1C2=CC(CC)=CC=C2C=C(N)C=1C(=O)NC1=CN=C2C(O)CCC2=C1N1CCCC(N)C1 QQULFRBGXNZCES-UHFFFAOYSA-N 0.000 claims 1
- NLNNGHVRIKEROZ-UHFFFAOYSA-N 3-amino-n-[4-(3-aminopiperidin-1-yl)pyridin-3-yl]-7-(1-fluoroethyl)quinoline-2-carboxamide Chemical compound N=1C2=CC(C(F)C)=CC=C2C=C(N)C=1C(=O)NC1=CN=CC=C1N1CCCC(N)C1 NLNNGHVRIKEROZ-UHFFFAOYSA-N 0.000 claims 1
- KHJUSTSHPOREIS-UHFFFAOYSA-N 3-amino-n-[4-(3-aminopiperidin-1-yl)pyridin-3-yl]-7-(1-hydroxyethyl)quinoline-2-carboxamide Chemical compound N=1C2=CC(C(O)C)=CC=C2C=C(N)C=1C(=O)NC1=CN=CC=C1N1CCCC(N)C1 KHJUSTSHPOREIS-UHFFFAOYSA-N 0.000 claims 1
- HOJRGISHIKWYJZ-UHFFFAOYSA-N 3-amino-n-[4-(3-aminopiperidin-1-yl)pyridin-3-yl]-7-(2,6-difluorophenyl)quinoline-2-carboxamide Chemical compound C1C(N)CCCN1C1=CC=NC=C1NC(=O)C1=NC2=CC(C=3C(=CC=CC=3F)F)=CC=C2C=C1N HOJRGISHIKWYJZ-UHFFFAOYSA-N 0.000 claims 1
- HNGITTXJRALLSW-UHFFFAOYSA-N 3-amino-n-[4-(3-aminopiperidin-1-yl)pyridin-3-yl]-7-(2-cyano-6-fluorophenyl)quinoline-2-carboxamide Chemical compound C1C(N)CCCN1C1=CC=NC=C1NC(=O)C1=NC2=CC(C=3C(=CC=CC=3F)C#N)=CC=C2C=C1N HNGITTXJRALLSW-UHFFFAOYSA-N 0.000 claims 1
- WSVVRQHNTHXBJZ-UHFFFAOYSA-N 3-amino-n-[4-(3-aminopiperidin-1-yl)pyridin-3-yl]-7-(2-cyanophenyl)quinoline-2-carboxamide Chemical compound C1C(N)CCCN1C1=CC=NC=C1NC(=O)C1=NC2=CC(C=3C(=CC=CC=3)C#N)=CC=C2C=C1N WSVVRQHNTHXBJZ-UHFFFAOYSA-N 0.000 claims 1
- USRTYRAHNYHTKH-UHFFFAOYSA-N 3-amino-n-[4-(3-aminopiperidin-1-yl)pyridin-3-yl]-7-(cyanomethyl)quinoline-2-carboxamide Chemical compound C1C(N)CCCN1C1=CC=NC=C1NC(=O)C1=NC2=CC(CC#N)=CC=C2C=C1N USRTYRAHNYHTKH-UHFFFAOYSA-N 0.000 claims 1
- UDDBBYAKVUDFNK-UHFFFAOYSA-N 3-amino-n-[4-(3-aminopiperidin-1-yl)pyridin-3-yl]-7-(morpholin-4-ylmethyl)quinoline-2-carboxamide Chemical compound C1C(N)CCCN1C1=CC=NC=C1NC(=O)C1=NC2=CC(CN3CCOCC3)=CC=C2C=C1N UDDBBYAKVUDFNK-UHFFFAOYSA-N 0.000 claims 1
- CECWJCILCAIQAC-UHFFFAOYSA-N 3-amino-n-[4-(3-aminopiperidin-1-yl)pyridin-3-yl]-7-(pyrrolidin-1-ylmethyl)quinoline-2-carboxamide Chemical compound C1C(N)CCCN1C1=CC=NC=C1NC(=O)C1=NC2=CC(CN3CCCC3)=CC=C2C=C1N CECWJCILCAIQAC-UHFFFAOYSA-N 0.000 claims 1
- VQDNDMIJBAPVRG-UHFFFAOYSA-N 3-amino-n-[4-(3-aminopiperidin-1-yl)pyridin-3-yl]-7-[(dimethylamino)methyl]quinoline-2-carboxamide Chemical compound N=1C2=CC(CN(C)C)=CC=C2C=C(N)C=1C(=O)NC1=CN=CC=C1N1CCCC(N)C1 VQDNDMIJBAPVRG-UHFFFAOYSA-N 0.000 claims 1
- ZRNUNAHKAVZXIQ-UHFFFAOYSA-N 3-amino-n-[4-(3-aminopiperidin-1-yl)pyridin-3-yl]-7-[hydroxy(phenyl)methyl]quinoline-2-carboxamide Chemical compound C1C(N)CCCN1C1=CC=NC=C1NC(=O)C1=NC2=CC(C(O)C=3C=CC=CC=3)=CC=C2C=C1N ZRNUNAHKAVZXIQ-UHFFFAOYSA-N 0.000 claims 1
- IUWQFPCBLRECFE-UHFFFAOYSA-N 3-amino-n-[4-(3-aminopiperidin-1-yl)pyridin-3-yl]-7-ethoxy-1,8-naphthyridine-2-carboxamide Chemical compound N=1C2=NC(OCC)=CC=C2C=C(N)C=1C(=O)NC1=CN=CC=C1N1CCCC(N)C1 IUWQFPCBLRECFE-UHFFFAOYSA-N 0.000 claims 1
- CTKJRRFLVNYGTD-UHFFFAOYSA-N 3-amino-n-[4-(3-aminopiperidin-1-yl)pyridin-3-yl]-7-ethyl-1,6-naphthyridine-2-carboxamide Chemical compound NC=1C=C2C=NC(CC)=CC2=NC=1C(=O)NC1=CN=CC=C1N1CCCC(N)C1 CTKJRRFLVNYGTD-UHFFFAOYSA-N 0.000 claims 1
- VPQMMXPQFSHBJT-UHFFFAOYSA-N 3-amino-n-[4-(3-aminopiperidin-1-yl)pyridin-3-yl]-7-ethyl-6-fluoroquinoline-2-carboxamide Chemical compound NC=1C=C2C=C(F)C(CC)=CC2=NC=1C(=O)NC1=CN=CC=C1N1CCCC(N)C1 VPQMMXPQFSHBJT-UHFFFAOYSA-N 0.000 claims 1
- HHGGKGRBPVOWBO-UHFFFAOYSA-N 3-amino-n-[4-(3-aminopiperidin-1-yl)pyridin-3-yl]-7-ethylquinoline-2-carboxamide Chemical compound N=1C2=CC(CC)=CC=C2C=C(N)C=1C(=O)NC1=CN=CC=C1N1CCCC(N)C1 HHGGKGRBPVOWBO-UHFFFAOYSA-N 0.000 claims 1
- AMNYMLVTVLXRTN-UHFFFAOYSA-N 3-amino-n-[4-(3-aminopiperidin-1-yl)pyridin-3-yl]-7-piperidin-4-ylquinoline-2-carboxamide Chemical compound C1C(N)CCCN1C1=CC=NC=C1NC(=O)C1=NC2=CC(C3CCNCC3)=CC=C2C=C1N AMNYMLVTVLXRTN-UHFFFAOYSA-N 0.000 claims 1
- FJYFIHVJKOMXRN-UHFFFAOYSA-N 3-amino-n-[4-(3-aminopiperidin-1-yl)pyridin-3-yl]-7-propan-2-ylquinoline-2-carboxamide Chemical compound N=1C2=CC(C(C)C)=CC=C2C=C(N)C=1C(=O)NC1=CN=CC=C1N1CCCC(N)C1 FJYFIHVJKOMXRN-UHFFFAOYSA-N 0.000 claims 1
- LSPMPLWLIFDEJM-UHFFFAOYSA-N 3-amino-n-[4-(3-aminopiperidin-1-yl)pyridin-3-yl]quinoline-2-carboxamide Chemical compound C1C(N)CCCN1C1=CC=NC=C1NC(=O)C1=NC2=CC=CC=C2C=C1N LSPMPLWLIFDEJM-UHFFFAOYSA-N 0.000 claims 1
- JUMHXVDASNXZCK-FPULEUEGSA-N 3-amino-n-[4-[(3r,4r,5s)-3-amino-4-hydroxy-5-methylpiperidin-1-yl]-5-methylpyridin-3-yl]-7-ethylquinoline-2-carboxamide Chemical compound N=1C2=CC(CC)=CC=C2C=C(N)C=1C(=O)NC1=CN=CC(C)=C1N1C[C@H](C)[C@@H](O)[C@H](N)C1 JUMHXVDASNXZCK-FPULEUEGSA-N 0.000 claims 1
- NKUFQFKOCYCIBU-PGICJIBASA-N 3-amino-n-[4-[(3r,4r,5s)-3-amino-4-hydroxy-5-methylpiperidin-1-yl]pyridin-3-yl]-7-ethoxy-1,8-naphthyridine-2-carboxamide Chemical compound N=1C2=NC(OCC)=CC=C2C=C(N)C=1C(=O)NC1=CN=CC=C1N1C[C@H](C)[C@@H](O)[C@H](N)C1 NKUFQFKOCYCIBU-PGICJIBASA-N 0.000 claims 1
- GOMYQKXTHKSISF-OIAISFKWSA-N 3-amino-n-[4-[(3r,4r,5s)-3-amino-4-hydroxy-5-methylpiperidin-1-yl]pyridin-3-yl]-7-ethylquinoline-2-carboxamide Chemical compound N=1C2=CC(CC)=CC=C2C=C(N)C=1C(=O)NC1=CN=CC=C1N1C[C@H](C)[C@@H](O)[C@H](N)C1 GOMYQKXTHKSISF-OIAISFKWSA-N 0.000 claims 1
- CDIASNJIOWVCSV-INIZCTEOSA-N 3-amino-n-[4-[(3s)-3-aminopiperidin-1-yl]-2,3-dihydrofuro[2,3-b]pyridin-5-yl]-7-ethylquinoline-2-carboxamide Chemical compound N=1C2=CC(CC)=CC=C2C=C(N)C=1C(=O)NC1=CN=C2OCCC2=C1N1CCC[C@H](N)C1 CDIASNJIOWVCSV-INIZCTEOSA-N 0.000 claims 1
- QSUWTJZUEPZOOX-KRWDZBQOSA-N 3-amino-n-[4-[(3s)-3-aminopiperidin-1-yl]-5-cyanopyridin-3-yl]-7-ethylquinoline-2-carboxamide Chemical compound N=1C2=CC(CC)=CC=C2C=C(N)C=1C(=O)NC1=CN=CC(C#N)=C1N1CCC[C@H](N)C1 QSUWTJZUEPZOOX-KRWDZBQOSA-N 0.000 claims 1
- PCBLQWCMPHDPQE-KRWDZBQOSA-N 3-amino-n-[4-[(3s)-3-aminopiperidin-1-yl]-5-methylpyridin-3-yl]-7-ethylquinoline-2-carboxamide Chemical compound N=1C2=CC(CC)=CC=C2C=C(N)C=1C(=O)NC1=CN=CC(C)=C1N1CCC[C@H](N)C1 PCBLQWCMPHDPQE-KRWDZBQOSA-N 0.000 claims 1
- QQULFRBGXNZCES-BJQOMGFOSA-N 3-amino-n-[4-[(3s)-3-aminopiperidin-1-yl]-7-hydroxy-6,7-dihydro-5h-cyclopenta[b]pyridin-3-yl]-7-ethylquinoline-2-carboxamide Chemical compound N=1C2=CC(CC)=CC=C2C=C(N)C=1C(=O)NC1=CN=C2C(O)CCC2=C1N1CCC[C@H](N)C1 QQULFRBGXNZCES-BJQOMGFOSA-N 0.000 claims 1
- NLNNGHVRIKEROZ-VYIIXAMBSA-N 3-amino-n-[4-[(3s)-3-aminopiperidin-1-yl]pyridin-3-yl]-7-(1-fluoroethyl)quinoline-2-carboxamide Chemical compound N=1C2=CC(C(F)C)=CC=C2C=C(N)C=1C(=O)NC1=CN=CC=C1N1CCC[C@H](N)C1 NLNNGHVRIKEROZ-VYIIXAMBSA-N 0.000 claims 1
- KHJUSTSHPOREIS-VYIIXAMBSA-N 3-amino-n-[4-[(3s)-3-aminopiperidin-1-yl]pyridin-3-yl]-7-(1-hydroxyethyl)quinoline-2-carboxamide Chemical compound N=1C2=CC(C(O)C)=CC=C2C=C(N)C=1C(=O)NC1=CN=CC=C1N1CCC[C@H](N)C1 KHJUSTSHPOREIS-VYIIXAMBSA-N 0.000 claims 1
- HOJRGISHIKWYJZ-KRWDZBQOSA-N 3-amino-n-[4-[(3s)-3-aminopiperidin-1-yl]pyridin-3-yl]-7-(2,6-difluorophenyl)quinoline-2-carboxamide Chemical compound C1[C@@H](N)CCCN1C1=CC=NC=C1NC(=O)C1=NC2=CC(C=3C(=CC=CC=3F)F)=CC=C2C=C1N HOJRGISHIKWYJZ-KRWDZBQOSA-N 0.000 claims 1
- HNGITTXJRALLSW-IBGZPJMESA-N 3-amino-n-[4-[(3s)-3-aminopiperidin-1-yl]pyridin-3-yl]-7-(2-cyano-6-fluorophenyl)quinoline-2-carboxamide Chemical compound C1[C@@H](N)CCCN1C1=CC=NC=C1NC(=O)C1=NC2=CC(C=3C(=CC=CC=3F)C#N)=CC=C2C=C1N HNGITTXJRALLSW-IBGZPJMESA-N 0.000 claims 1
- WSVVRQHNTHXBJZ-FQEVSTJZSA-N 3-amino-n-[4-[(3s)-3-aminopiperidin-1-yl]pyridin-3-yl]-7-(2-cyanophenyl)quinoline-2-carboxamide Chemical compound C1[C@@H](N)CCCN1C1=CC=NC=C1NC(=O)C1=NC2=CC(C=3C(=CC=CC=3)C#N)=CC=C2C=C1N WSVVRQHNTHXBJZ-FQEVSTJZSA-N 0.000 claims 1
- NSMUWQGNLKGWFQ-INIZCTEOSA-N 3-amino-n-[4-[(3s)-3-aminopiperidin-1-yl]pyridin-3-yl]-7-(2-hydroxypropan-2-yl)quinoline-2-carboxamide Chemical compound N=1C2=CC(C(C)(O)C)=CC=C2C=C(N)C=1C(=O)NC1=CN=CC=C1N1CCC[C@H](N)C1 NSMUWQGNLKGWFQ-INIZCTEOSA-N 0.000 claims 1
- USRTYRAHNYHTKH-INIZCTEOSA-N 3-amino-n-[4-[(3s)-3-aminopiperidin-1-yl]pyridin-3-yl]-7-(cyanomethyl)quinoline-2-carboxamide Chemical compound C1[C@@H](N)CCCN1C1=CC=NC=C1NC(=O)C1=NC2=CC(CC#N)=CC=C2C=C1N USRTYRAHNYHTKH-INIZCTEOSA-N 0.000 claims 1
- UDDBBYAKVUDFNK-IBGZPJMESA-N 3-amino-n-[4-[(3s)-3-aminopiperidin-1-yl]pyridin-3-yl]-7-(morpholin-4-ylmethyl)quinoline-2-carboxamide Chemical compound C1[C@@H](N)CCCN1C1=CC=NC=C1NC(=O)C1=NC2=CC(CN3CCOCC3)=CC=C2C=C1N UDDBBYAKVUDFNK-IBGZPJMESA-N 0.000 claims 1
- CECWJCILCAIQAC-IBGZPJMESA-N 3-amino-n-[4-[(3s)-3-aminopiperidin-1-yl]pyridin-3-yl]-7-(pyrrolidin-1-ylmethyl)quinoline-2-carboxamide Chemical compound C1[C@@H](N)CCCN1C1=CC=NC=C1NC(=O)C1=NC2=CC(CN3CCCC3)=CC=C2C=C1N CECWJCILCAIQAC-IBGZPJMESA-N 0.000 claims 1
- VQDNDMIJBAPVRG-KRWDZBQOSA-N 3-amino-n-[4-[(3s)-3-aminopiperidin-1-yl]pyridin-3-yl]-7-[(dimethylamino)methyl]quinoline-2-carboxamide Chemical compound N=1C2=CC(CN(C)C)=CC=C2C=C(N)C=1C(=O)NC1=CN=CC=C1N1CCC[C@H](N)C1 VQDNDMIJBAPVRG-KRWDZBQOSA-N 0.000 claims 1
- ZRNUNAHKAVZXIQ-DQUNLGLBSA-N 3-amino-n-[4-[(3s)-3-aminopiperidin-1-yl]pyridin-3-yl]-7-[hydroxy(phenyl)methyl]quinoline-2-carboxamide Chemical compound C1[C@@H](N)CCCN1C1=CC=NC=C1NC(=O)C1=NC2=CC(C(O)C=3C=CC=CC=3)=CC=C2C=C1N ZRNUNAHKAVZXIQ-DQUNLGLBSA-N 0.000 claims 1
- IUWQFPCBLRECFE-AWEZNQCLSA-N 3-amino-n-[4-[(3s)-3-aminopiperidin-1-yl]pyridin-3-yl]-7-ethoxy-1,8-naphthyridine-2-carboxamide Chemical compound N=1C2=NC(OCC)=CC=C2C=C(N)C=1C(=O)NC1=CN=CC=C1N1CCC[C@H](N)C1 IUWQFPCBLRECFE-AWEZNQCLSA-N 0.000 claims 1
- CTKJRRFLVNYGTD-AWEZNQCLSA-N 3-amino-n-[4-[(3s)-3-aminopiperidin-1-yl]pyridin-3-yl]-7-ethyl-1,6-naphthyridine-2-carboxamide Chemical compound NC=1C=C2C=NC(CC)=CC2=NC=1C(=O)NC1=CN=CC=C1N1CCC[C@H](N)C1 CTKJRRFLVNYGTD-AWEZNQCLSA-N 0.000 claims 1
- VPQMMXPQFSHBJT-HNNXBMFYSA-N 3-amino-n-[4-[(3s)-3-aminopiperidin-1-yl]pyridin-3-yl]-7-ethyl-6-fluoroquinoline-2-carboxamide Chemical compound NC=1C=C2C=C(F)C(CC)=CC2=NC=1C(=O)NC1=CN=CC=C1N1CCC[C@H](N)C1 VPQMMXPQFSHBJT-HNNXBMFYSA-N 0.000 claims 1
- HHGGKGRBPVOWBO-INIZCTEOSA-N 3-amino-n-[4-[(3s)-3-aminopiperidin-1-yl]pyridin-3-yl]-7-ethylquinoline-2-carboxamide Chemical compound N=1C2=CC(CC)=CC=C2C=C(N)C=1C(=O)NC1=CN=CC=C1N1CCC[C@H](N)C1 HHGGKGRBPVOWBO-INIZCTEOSA-N 0.000 claims 1
- AMNYMLVTVLXRTN-IBGZPJMESA-N 3-amino-n-[4-[(3s)-3-aminopiperidin-1-yl]pyridin-3-yl]-7-piperidin-4-ylquinoline-2-carboxamide Chemical compound C1[C@@H](N)CCCN1C1=CC=NC=C1NC(=O)C1=NC2=CC(C3CCNCC3)=CC=C2C=C1N AMNYMLVTVLXRTN-IBGZPJMESA-N 0.000 claims 1
- FJYFIHVJKOMXRN-KRWDZBQOSA-N 3-amino-n-[4-[(3s)-3-aminopiperidin-1-yl]pyridin-3-yl]-7-propan-2-ylquinoline-2-carboxamide Chemical compound N=1C2=CC(C(C)C)=CC=C2C=C(N)C=1C(=O)NC1=CN=CC=C1N1CCC[C@H](N)C1 FJYFIHVJKOMXRN-KRWDZBQOSA-N 0.000 claims 1
- YPSXFMHXRZAGTG-UHFFFAOYSA-N 4-methoxy-2-[2-(5-methoxy-2-nitrosophenyl)ethyl]-1-nitrosobenzene Chemical compound COC1=CC=C(N=O)C(CCC=2C(=CC=C(OC)C=2)N=O)=C1 YPSXFMHXRZAGTG-UHFFFAOYSA-N 0.000 claims 1
- 208000024893 Acute lymphoblastic leukemia Diseases 0.000 claims 1
- 208000014697 Acute lymphocytic leukaemia Diseases 0.000 claims 1
- 208000031261 Acute myeloid leukaemia Diseases 0.000 claims 1
- 206010002556 Ankylosing Spondylitis Diseases 0.000 claims 1
- 102100021569 Apoptosis regulator Bcl-2 Human genes 0.000 claims 1
- 201000001320 Atherosclerosis Diseases 0.000 claims 1
- 208000023275 Autoimmune disease Diseases 0.000 claims 1
- 208000010839 B-cell chronic lymphocytic leukemia Diseases 0.000 claims 1
- 208000023328 Basedow 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
- 125000000041 C6-C10 aryl group Chemical group 0.000 claims 1
- 206010009900 Colitis ulcerative Diseases 0.000 claims 1
- 206010009944 Colon cancer Diseases 0.000 claims 1
- 208000011231 Crohn disease Diseases 0.000 claims 1
- 201000004624 Dermatitis Diseases 0.000 claims 1
- 206010013554 Diverticulum Diseases 0.000 claims 1
- 206010014733 Endometrial cancer Diseases 0.000 claims 1
- 206010014759 Endometrial neoplasm Diseases 0.000 claims 1
- 102000004190 Enzymes Human genes 0.000 claims 1
- 108090000790 Enzymes Proteins 0.000 claims 1
- 208000000461 Esophageal Neoplasms Diseases 0.000 claims 1
- 208000032027 Essential Thrombocythemia Diseases 0.000 claims 1
- 208000004262 Food Hypersensitivity Diseases 0.000 claims 1
- 206010016946 Food allergy Diseases 0.000 claims 1
- 206010018364 Glomerulonephritis Diseases 0.000 claims 1
- 208000015023 Graves' disease Diseases 0.000 claims 1
- 208000030836 Hashimoto thyroiditis Diseases 0.000 claims 1
- 208000017604 Hodgkin disease Diseases 0.000 claims 1
- 208000021519 Hodgkin lymphoma Diseases 0.000 claims 1
- 208000010747 Hodgkins lymphoma Diseases 0.000 claims 1
- 101000971171 Homo sapiens Apoptosis regulator Bcl-2 Proteins 0.000 claims 1
- 206010020751 Hypersensitivity Diseases 0.000 claims 1
- 208000022559 Inflammatory bowel disease Diseases 0.000 claims 1
- 208000008839 Kidney Neoplasms Diseases 0.000 claims 1
- 208000031671 Large B-Cell Diffuse Lymphoma Diseases 0.000 claims 1
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims 1
- 208000031422 Lymphocytic Chronic B-Cell Leukemia Diseases 0.000 claims 1
- 206010025323 Lymphomas Diseases 0.000 claims 1
- 208000025205 Mantle-Cell Lymphoma Diseases 0.000 claims 1
- 206010027476 Metastases Diseases 0.000 claims 1
- 208000034578 Multiple myelomas Diseases 0.000 claims 1
- 208000033776 Myeloid Acute Leukemia Diseases 0.000 claims 1
- 208000014767 Myeloproliferative disease Diseases 0.000 claims 1
- 208000015914 Non-Hodgkin lymphomas Diseases 0.000 claims 1
- 206010030155 Oesophageal carcinoma Diseases 0.000 claims 1
- 108700020796 Oncogene Proteins 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
- 206010033645 Pancreatitis Diseases 0.000 claims 1
- 206010035226 Plasma cell myeloma Diseases 0.000 claims 1
- 208000008601 Polycythemia Diseases 0.000 claims 1
- 208000006664 Precursor Cell Lymphoblastic Leukemia-Lymphoma Diseases 0.000 claims 1
- 206010036790 Productive cough Diseases 0.000 claims 1
- 206010060862 Prostate cancer Diseases 0.000 claims 1
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims 1
- 201000004681 Psoriasis Diseases 0.000 claims 1
- 201000001263 Psoriatic Arthritis Diseases 0.000 claims 1
- 208000036824 Psoriatic arthropathy Diseases 0.000 claims 1
- 206010038389 Renal cancer Diseases 0.000 claims 1
- 206010039491 Sarcoma Diseases 0.000 claims 1
- 206010039710 Scleroderma Diseases 0.000 claims 1
- 208000021386 Sjogren Syndrome Diseases 0.000 claims 1
- 208000005718 Stomach Neoplasms Diseases 0.000 claims 1
- 201000009594 Systemic Scleroderma Diseases 0.000 claims 1
- 206010042953 Systemic sclerosis Diseases 0.000 claims 1
- 208000005485 Thrombocytosis Diseases 0.000 claims 1
- 206010067584 Type 1 diabetes mellitus Diseases 0.000 claims 1
- 208000007097 Urinary Bladder Neoplasms Diseases 0.000 claims 1
- 208000002495 Uterine Neoplasms Diseases 0.000 claims 1
- 206010047115 Vasculitis Diseases 0.000 claims 1
- 206010047642 Vitiligo Diseases 0.000 claims 1
- 208000026935 allergic disease Diseases 0.000 claims 1
- 230000007815 allergy Effects 0.000 claims 1
- 125000003277 amino group Chemical group 0.000 claims 1
- 230000033115 angiogenesis Effects 0.000 claims 1
- 208000006673 asthma Diseases 0.000 claims 1
- ZSIQJIWKELUFRJ-UHFFFAOYSA-N azepane Chemical class C1CCCNCC1 ZSIQJIWKELUFRJ-UHFFFAOYSA-N 0.000 claims 1
- 125000002837 carbocyclic group Chemical group 0.000 claims 1
- 208000032852 chronic lymphocytic leukemia Diseases 0.000 claims 1
- 208000029742 colonic neoplasm Diseases 0.000 claims 1
- 125000000753 cycloalkyl group Chemical group 0.000 claims 1
- 206010012818 diffuse large B-cell lymphoma Diseases 0.000 claims 1
- 229940079593 drug Drugs 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 201000004101 esophageal cancer Diseases 0.000 claims 1
- 125000001301 ethoxy group Chemical group [H]C([H])([H])C([H])([H])O* 0.000 claims 1
- 235000020932 food allergy Nutrition 0.000 claims 1
- 206010017758 gastric cancer Diseases 0.000 claims 1
- 208000005017 glioblastoma Diseases 0.000 claims 1
- 125000001188 haloalkyl group Chemical group 0.000 claims 1
- 230000002489 hematologic effect Effects 0.000 claims 1
- 230000001771 impaired effect Effects 0.000 claims 1
- 230000002401 inhibitory effect Effects 0.000 claims 1
- 208000002551 irritable bowel syndrome Diseases 0.000 claims 1
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 1
- 230000000366 juvenile effect Effects 0.000 claims 1
- 201000010982 kidney cancer Diseases 0.000 claims 1
- 208000032839 leukemia Diseases 0.000 claims 1
- 201000007270 liver cancer Diseases 0.000 claims 1
- 208000014018 liver neoplasm Diseases 0.000 claims 1
- 201000005202 lung cancer Diseases 0.000 claims 1
- 208000020816 lung neoplasm Diseases 0.000 claims 1
- 206010025135 lupus erythematosus Diseases 0.000 claims 1
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims 1
- 230000009401 metastasis Effects 0.000 claims 1
- 238000000034 method Methods 0.000 claims 1
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims 1
- 125000004573 morpholin-4-yl group Chemical group N1(CCOCC1)* 0.000 claims 1
- 125000002757 morpholinyl group Chemical group 0.000 claims 1
- 201000006417 multiple sclerosis Diseases 0.000 claims 1
- 206010028417 myasthenia gravis Diseases 0.000 claims 1
- 230000002071 myeloproliferative effect Effects 0.000 claims 1
- 201000008482 osteoarthritis Diseases 0.000 claims 1
- 201000002528 pancreatic cancer Diseases 0.000 claims 1
- 208000008443 pancreatic carcinoma Diseases 0.000 claims 1
- 125000004482 piperidin-4-yl group Chemical group N1CCC(CC1)* 0.000 claims 1
- 125000003386 piperidinyl group Chemical group 0.000 claims 1
- 150000003235 pyrrolidines Chemical class 0.000 claims 1
- 125000000719 pyrrolidinyl group Chemical group 0.000 claims 1
- 206010039073 rheumatoid arthritis Diseases 0.000 claims 1
- 229920006395 saturated elastomer Polymers 0.000 claims 1
- 210000003802 sputum Anatomy 0.000 claims 1
- 208000024794 sputum Diseases 0.000 claims 1
- 201000011549 stomach cancer Diseases 0.000 claims 1
- 125000001412 tetrahydropyranyl group Chemical group 0.000 claims 1
- 238000002560 therapeutic procedure Methods 0.000 claims 1
- 208000013077 thyroid gland carcinoma Diseases 0.000 claims 1
- 201000005112 urinary bladder cancer Diseases 0.000 claims 1
- 206010046766 uterine cancer Diseases 0.000 claims 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201361752249P | 2013-01-14 | 2013-01-14 | |
| US61/752,249 | 2013-01-14 | ||
| US201361791275P | 2013-03-15 | 2013-03-15 | |
| US61/791,275 | 2013-03-15 | ||
| PCT/US2014/011487 WO2014110574A1 (en) | 2013-01-14 | 2014-01-14 | Bicyclic aromatic carboxamide compounds useful as pim kinase inhibitors |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2016505021A JP2016505021A (ja) | 2016-02-18 |
| JP2016505021A5 true JP2016505021A5 (enExample) | 2017-02-02 |
| JP6437452B2 JP6437452B2 (ja) | 2018-12-12 |
Family
ID=50030545
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2015552897A Active JP6437452B2 (ja) | 2013-01-14 | 2014-01-14 | Ｐｉｍキナーゼ阻害剤として有用な二環式芳香族カルボキサミド化合物 |
Country Status (6)
| Country | Link |
|---|---|
| US (2) | US9278950B2 (enExample) |
| EP (1) | EP2943485B1 (enExample) |
| JP (1) | JP6437452B2 (enExample) |
| CA (1) | CA2897200C (enExample) |
| ES (1) | ES2649156T3 (enExample) |
| WO (1) | WO2014110574A1 (enExample) |
Families Citing this family (18)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US9453003B2 (en) * | 2011-08-11 | 2016-09-27 | Jikai Biosciences, Inc. | Pyrimidine derivatives as PIM kinase inhibitors and preparation methods and use in medicinal manufacture thereof |
| US9458151B2 (en) * | 2011-08-11 | 2016-10-04 | Jikai Biosciences, Inc. | Isothiazole derivatives as PIM kinase inhibitors and preparation methods and use in medicinal manufacture thereof |
| JP6437452B2 (ja) | 2013-01-14 | 2018-12-12 | インサイト・ホールディングス・コーポレイションＩｎｃｙｔｅ Ｈｏｌｄｉｎｇｓ Ｃｏｒｐｏｒａｔｉｏｎ | Ｐｉｍキナーゼ阻害剤として有用な二環式芳香族カルボキサミド化合物 |
| LT2945939T (lt) | 2013-01-15 | 2020-07-27 | Incyte Holdings Corporation | Triazolkarboksamidai ir piridinkarboksamido junginiai, naudotini kaip pim kinazės inhibitoriai |
| EP3036238A1 (en) | 2013-08-23 | 2016-06-29 | Incyte Corporation | Furo- and thieno-pyridine carboxamide compounds useful as pim kinase inhibitors |
| US9580418B2 (en) | 2014-07-14 | 2017-02-28 | Incyte Corporation | Bicyclic aromatic carboxamide compounds useful as Pim kinase inhibitors |
| US9822124B2 (en) | 2014-07-14 | 2017-11-21 | Incyte Corporation | Bicyclic heteroaromatic carboxamide compounds useful as Pim kinase inhibitors |
| WO2016161248A1 (en) * | 2015-04-02 | 2016-10-06 | Tolero Pharmaceuticals, Inc. | Targeting pim kinases in combination with btk inhibition |
| US9540347B2 (en) | 2015-05-29 | 2017-01-10 | Incyte Corporation | Pyridineamine compounds useful as Pim kinase inhibitors |
| AR105967A1 (es) * | 2015-09-09 | 2017-11-29 | Incyte Corp | Sales de un inhibidor de pim quinasa |
| WO2017059251A1 (en) * | 2015-10-02 | 2017-04-06 | Incyte Corporation | Heterocyclic compounds useful as pim kinase inhibitors |
| US9771366B2 (en) * | 2016-02-19 | 2017-09-26 | Phoenix Molecular Design | Substituted tetrahydropyrido[3′,2′:4,5]pyrrolo[1,2-a]pyrazine-2-carboxamides as RSK inhibitors |
| CN106336371A (zh) * | 2016-08-16 | 2017-01-18 | 成都百事兴科技实业有限公司 | 叔丁氧羰基‑l‑焦谷氨酸甲酯的合成方法 |
| EP3535273A1 (en) * | 2016-11-02 | 2019-09-11 | H. Hoffnabb-La Roche Ag | PYRAZOLO[1,5a]PYRIMIDINE DERIVATIVES AS IRAK4 MODULATORS |
| WO2019090205A1 (en) | 2017-11-06 | 2019-05-09 | Snap Bio, Inc. | Pim kinase inhibitor compositions, methods, and uses thereof |
| TW201924683A (zh) | 2017-12-08 | 2019-07-01 | 美商英塞特公司 | 用於治療骨髓增生性贅瘤的低劑量組合療法 |
| GEP20227359B (en) | 2017-12-13 | 2022-03-10 | Lupin Ltd | Substituted bicyclic heterocyclic compounds as prmt5 inhibitors |
| CN118852123A (zh) * | 2023-04-27 | 2024-10-29 | 株式会社大熊制药 | 用于治疗和预防癌症的作为Polθ抑制剂的新型杂环化合物及含该化合物的药物组合物 |
Family Cites Families (190)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP1294358B1 (en) | 2000-06-28 | 2004-08-18 | Smithkline Beecham Plc | Wet milling process |
| AU2002246864A1 (en) | 2000-12-27 | 2002-07-24 | The Trustees Of Columbia University In The City Of New York | Pim kinase-related methods |
| DE10123055A1 (de) | 2001-05-11 | 2003-03-20 | Gruenenthal Gmbh | Screeningverfahren mit PIM1-Kinase oder PIM3-Kinase |
| DE10226702A1 (de) | 2002-06-14 | 2004-09-09 | Grünenthal GmbH | Antisense Oligonukleotide gegen PIM1 |
| WO2006078228A1 (en) | 2002-09-16 | 2006-07-27 | Plexxikon, Inc. | Methods for the design of molecular scaffolds and ligands |
| US20040142864A1 (en) | 2002-09-16 | 2004-07-22 | Plexxikon, Inc. | Crystal structure of PIM-1 kinase |
| WO2004090106A2 (en) | 2003-04-04 | 2004-10-21 | Vertex Pharmaceuticals Incorporated | Crystal structures of human pim-1 kinase protein complexes and binding pockets thereof, and uses thereof in drug design |
| WO2005028624A2 (en) | 2003-09-15 | 2005-03-31 | Plexxikon, Inc. | Molecular scaffolds for kinase ligand development |
| WO2005033310A1 (de) | 2003-10-01 | 2005-04-14 | Grünenthal GmbH | Pim-1-spezifische dsrna-verbindungen |
| WO2006006569A1 (ja) | 2004-07-12 | 2006-01-19 | Nihon Nohyaku Co., Ltd. | フェニルピリジン類又はその塩類、これらを有効成分とする除草剤及びその使用方法 |
| AU2005321966B2 (en) | 2004-12-28 | 2011-11-17 | Atnx Spv, Llc | Compositions and methods of treating cell proliferation disorders |
| WO2007002433A1 (en) | 2005-06-22 | 2007-01-04 | Plexxikon, Inc. | Pyrrolo [2, 3-b] pyridine derivatives as protein kinase inhibitors |
| WO2007011760A2 (en) | 2005-07-15 | 2007-01-25 | Kalypsys, Inc. | Inhibitors of mitotic kinesin |
| ATE533770T1 (de) | 2005-10-06 | 2011-12-15 | Schering Corp | Pyrazolopyrimidine als proteinkinaseinhibitoren |
| AU2006302174B2 (en) | 2005-10-06 | 2013-06-20 | Exelixis, Inc. | Pyridopyrimidinone Inhibitors of PIM-1 and/or PIM-3 |
| EP1948663B1 (en) | 2005-10-21 | 2011-09-14 | Exelixis, Inc. | Pyrazolo-pyrimidines as casein kinase ii (ck2) modulators |
| WO2007052843A1 (ja) | 2005-11-04 | 2007-05-10 | Takeda Pharmaceutical Company Limited | 複素環アミド化合物およびその用途 |
| WO2007084857A2 (en) | 2006-01-13 | 2007-07-26 | President And Fellows Of Harvard College | Methods and compositions for treating cell proliferative disorders |
| US20090253156A1 (en) | 2006-05-05 | 2009-10-08 | Perkinelmer Las, Inc. | Mass spectrometry methods for multiplexed quantification of protein kinases and phosphatases |
| JP5564251B2 (ja) | 2006-06-29 | 2014-07-30 | キネックス ファーマシューティカルズ， エルエルシー | キナーゼカスケードを調節するためのビアリール組成物および方法 |
| ES2500165T3 (es) | 2006-06-29 | 2014-09-30 | Kinex Pharmaceuticals, Llc | Composiciones de biarilo y métodos para modular una cascada de quinasas |
| US8318723B2 (en) | 2006-08-16 | 2012-11-27 | Boehringer Ingelheim International Gmbh | Pyrazine compounds, their use and methods of preparation |
| WO2008045252A2 (en) | 2006-10-04 | 2008-04-17 | The Board Of Trustees Of The Leland Stanford Junior University | Engineered integrin binding peptides |
| AU2007314305B2 (en) | 2006-10-31 | 2013-01-24 | Merck Sharp & Dohme Corp. | 2-aminothiazole-4-carboxylic amides as protein kinase inhibitors |
| CA2667487C (en) | 2006-11-06 | 2017-04-04 | Supergen, Inc. | Imidazo[1,2-b]pyridazine and pyrazolo[1,5-a]pyrimidine derivatives and their use as protein kinase inhibitors |
| WO2008082840A1 (en) | 2006-12-29 | 2008-07-10 | Abbott Laboratories | Pim kinase inhibitors as cancer chemotherapeutics |
| WO2008082839A2 (en) | 2006-12-29 | 2008-07-10 | Abbott Laboratories | Pim kinase inhibitors as cancer chemotherapeutics |
| EA019951B1 (ru) * | 2007-03-01 | 2014-07-30 | Новартис Аг | Ингибиторы киназы pim и способы их применения |
| CA2682231A1 (en) | 2007-03-28 | 2008-10-09 | Array Biopharma Inc. | Imidazo[1,2-a]pyridine compounds as receptor tyrosine kinase inhibitors |
| UA101611C2 (ru) | 2007-04-03 | 2013-04-25 | Аррей Байофарма Инк. | СОЕДИНЕНИЯ ИМИДАЗО[1,2-а]ПИРИДИНА КАК ИНГИБИТОРЫ ТИРОЗИНКИНАЗЫ РЕЦЕПТОРОВ |
| CA2685106A1 (en) | 2007-04-25 | 2008-11-06 | Exelixis, Inc. | 6-phenylpyrimidinones as pim modulators |
| US8324231B2 (en) | 2007-04-25 | 2012-12-04 | Exelixis, Inc. | Pyrimidinones as casein kinase II (CK2) modulators |
| CN101801958B (zh) * | 2007-07-19 | 2014-01-29 | 默沙东公司 | 作为蛋白质激酶抑制剂的杂环酰胺化合物 |
| KR20100042287A (ko) | 2007-07-31 | 2010-04-23 | 쉐링 코포레이션 | 항암요법으로서의 항-유사분열제 및 아우로라 키나제 억제제 조합물 |
| WO2009064486A2 (en) | 2007-11-15 | 2009-05-22 | Musc Foundation For Research Development | Inhibitors of pim protein kinases, compositions, and methods for treating cancer |
| JP2011503207A (ja) | 2007-11-16 | 2011-01-27 | サン ディエゴ ステート ユニバーシティ リサーチ ファウンデーション | 循環系細胞におけるｐｉｍ−１活性を操作するための組成物および方法 |
| CN102036561A (zh) | 2008-02-29 | 2011-04-27 | 赛林药物股份有限公司 | 蛋白激酶调节剂 |
| AR070531A1 (es) | 2008-03-03 | 2010-04-14 | Novartis Ag | Inhibidores de cinasa pim y metodos para su uso |
| US8168794B2 (en) * | 2008-03-03 | 2012-05-01 | Novartis Ag | Pim kinase inhibitors and methods of their use |
| US20110294789A1 (en) | 2008-05-12 | 2011-12-01 | Amnestix, Inc. | Compounds for rho kinase inhibition and for improving learning and memory |
| AU2009267048A1 (en) | 2008-06-30 | 2010-01-07 | Cylene Pharmaceuticals, Inc. | Oxindole compounds |
| UY31952A (es) | 2008-07-02 | 2010-01-29 | Astrazeneca Ab | 5-metilideno-1,3-tiazolidina-2,4-dionas sustituidas como inhibidores de quinasa pim |
| FR2933409B1 (fr) | 2008-07-03 | 2010-08-27 | Centre Nat Rech Scient | NOUVEAUX PYRROLO °2,3-a! CARBAZOLES ET LEUR UTILISATION COMME INHIBITEURS DES KINASES PIM |
| US8557809B2 (en) | 2008-08-19 | 2013-10-15 | Array Biopharma Inc. | Triazolopyridine compounds as PIM kinase inhibitors |
| TWI496779B (zh) | 2008-08-19 | 2015-08-21 | Array Biopharma Inc | 作為ｐｉｍ激酶抑制劑之三唑吡啶化合物 |
| US8759338B2 (en) | 2008-09-02 | 2014-06-24 | Novartis Ag | Heterocyclic kinase inhibitors |
| BRPI0918268B1 (pt) | 2008-09-02 | 2021-08-03 | Novartis Ag | Derivados de picolinamida, seu uso, e composição farmacêutica |
| MX2011002367A (es) | 2008-09-02 | 2011-04-04 | Novartis Ag | Inhibidores de cinasa biciclicos. |
| SG10201914059WA (en) | 2008-10-22 | 2020-03-30 | Array Biopharma Inc | Substituted pyrazolo[1,5-a]pyrimidine compounds as trk kinase inhibitors |
| GB0821307D0 (en) | 2008-11-21 | 2008-12-31 | Summit Corp Plc | Compounds for treatment of duchenne muscular dystrophy |
| TW201035100A (en) | 2008-12-19 | 2010-10-01 | Cephalon Inc | Pyrrolotriazines as ALK and JAK2 inhibitors |
| US20120128631A1 (en) | 2009-05-19 | 2012-05-24 | San Diego State University (SDSU) Foundation, dba San Diego State University (SDSU) Research | Compositions and methods for kinase-mediated cytoprotection and enhanced cellular engraftment and persistence |
| NZ596571A (en) | 2009-05-20 | 2013-03-28 | Cylene Pharmaceuticals Inc | Pyrazolopyrimidines and related heterocycles as kinase inhibitors |
| WO2010135571A1 (en) | 2009-05-20 | 2010-11-25 | Cylene Pharmaceuticals, Inc. | Novel protein kinase modulators |
| TW201100429A (en) | 2009-05-22 | 2011-01-01 | Incyte Corp | N-(hetero)aryl-pyrrolidine derivatives of pyrazol-4-yl-pyrrolo[2,3-d]pyrimidines and pyrrol-3-yl-pyrrolo[2,3-d]pyrimidines as janus kinase inhibitors |
| US20100331315A1 (en) | 2009-06-18 | 2010-12-30 | Mustapha Haddach | Rhodanines and related heterocycles as kinase inhibitors |
| HRP20140754T2 (hr) | 2009-06-29 | 2015-07-17 | Incyte Corporation | Pirimidinoni kao inhibitori pi3k |
| IN2012DN02596A (enExample) | 2009-08-26 | 2015-08-28 | Cylene Pharmaceuticals Inc | |
| TW201113285A (en) | 2009-09-01 | 2011-04-16 | Incyte Corp | Heterocyclic derivatives of pyrazol-4-yl-pyrrolo[2,3-d]pyrimidines as janus kinase inhibitors |
| EP2475659B1 (en) | 2009-09-08 | 2015-10-28 | F.Hoffmann-La Roche Ag | 4-substituted pyridin-3-yl-carboxamide compounds and methods of use |
| US8435976B2 (en) | 2009-09-08 | 2013-05-07 | F. Hoffmann-La Roche | 4-substituted pyridin-3-yl-carboxamide compounds and methods of use |
| CN102625803A (zh) | 2009-09-11 | 2012-08-01 | 赛林药物股份有限公司 | 药学上有用的杂环-取代的内酰胺 |
| AU2010295622A1 (en) | 2009-09-16 | 2012-05-10 | Cylene Pharmaceuticals, Inc. | Tricyclic compounds and pharmaceutical uses thereof |
| BR112012005970A2 (pt) | 2009-09-16 | 2015-09-08 | Cylene Pharmaceuticals Inc | moduladores tricíclicos de proteína quinase |
| US8404677B2 (en) | 2009-10-29 | 2013-03-26 | Genosco | Kinase inhibitors |
| EP2332917B1 (en) | 2009-11-11 | 2012-08-01 | Sygnis Bioscience GmbH & Co. KG | Compounds for PIM kinase inhibition and for treating malignancy |
| CN102712601A (zh) | 2009-11-12 | 2012-10-03 | 赛尔维他股份公司 | 化合物、其制备方法、药物组合物、化合物的用途、用于调节或调控丝氨酸/苏氨酸激酶的方法以及丝氨酸/苏氨酸激酶调节剂 |
| US8304172B2 (en) | 2009-11-12 | 2012-11-06 | Advanced Micro Devices, Inc. | Semiconductor device fabrication using a multiple exposure and block mask approach to reduce design rule violations |
| WO2011060295A1 (en) | 2009-11-13 | 2011-05-19 | Genosco | Kinase inhibitors |
| US8853235B2 (en) | 2009-11-23 | 2014-10-07 | Senhwa Biosciences, Inc. | Polymorphs and salts of a kinase inhibitor |
| JP5802676B2 (ja) | 2009-12-04 | 2015-10-28 | センワ バイオサイエンシズ インコーポレイテッド | Ｃｋ２阻害剤としてのピラゾロピリミジンおよび関連複素環化合物 |
| WO2011075613A1 (en) | 2009-12-18 | 2011-06-23 | Sanofi | Azaindole derivatives, their preparation and their therapeutic application |
| US8759359B2 (en) | 2009-12-18 | 2014-06-24 | Incyte Corporation | Substituted heteroaryl fused derivatives as PI3K inhibitors |
| AR079529A1 (es) | 2009-12-18 | 2012-02-01 | Incyte Corp | Derivados arilo y heteroarilo sustituidos y fundidos como inhibidores de la pi3k |
| CN102884062B (zh) | 2009-12-23 | 2016-08-03 | 嘉世高制药公司 | 氨基嘧啶激酶抑制剂 |
| GB201002861D0 (en) | 2010-02-19 | 2010-04-07 | Cxr Biosciences Ltd | Compositions |
| PH12015502575A1 (en) | 2010-03-10 | 2017-04-24 | Incyte Corp | Piperidin-4-yl azetidine derivatives as jak1 inhibitors |
| CA2794801C (en) | 2010-04-07 | 2019-01-15 | F. Hoffmann-La Roche Ag | Pyrazol-4-yl-heterocyclyl-carboxamide compounds and methods of use |
| WO2011130342A1 (en) | 2010-04-14 | 2011-10-20 | Incyte Corporation | FUSED DERIVATIVES AS ΡI3Κδ INHIBITORS |
| US9062055B2 (en) | 2010-06-21 | 2015-06-23 | Incyte Corporation | Fused pyrrole derivatives as PI3K inhibitors |
| WO2012004217A1 (en) | 2010-07-06 | 2012-01-12 | Novartis Ag | Cyclic ether compounds useful as kinase inhibitors |
| KR101995013B1 (ko) | 2010-07-13 | 2019-07-02 | 에프. 호프만-라 로슈 아게 | Irak4 조절제로서 피라졸로[1,5a]피리미딘 및 티에노[3,2b]피리미딘 유도체 |
| US8227773B2 (en) | 2010-07-29 | 2012-07-24 | Axcelis Technologies, Inc. | Versatile beam glitch detection system |
| PT2598483T (pt) | 2010-07-29 | 2020-10-12 | Rigel Pharmaceuticals Inc | Compostos heterocíclicos de ativação de ampk e métodos de utilização dos mesmos |
| US8802099B2 (en) | 2010-11-10 | 2014-08-12 | National Jewish Health | Methods to treat allergic conditions |
| WO2012065297A1 (en) | 2010-11-16 | 2012-05-24 | Impact Therapeutics, Inc. | 3-ARYL-6-ARYL-[1,2,4]TRIAZOLO[4,3-a]PYRIDINES AS INHIBITORS OF CELL PROLIFERATION AND THE USE THEREOF |
| CA2818545C (en) | 2010-11-19 | 2019-04-16 | Incyte Corporation | Heterocyclic-substituted pyrrolopyridines and pyrrolopyrimidines as jak inhibitors |
| CN103415515B (zh) | 2010-11-19 | 2015-08-26 | 因塞特公司 | 作为jak抑制剂的环丁基取代的吡咯并吡啶和吡咯并嘧啶衍生物 |
| AU2011338389A1 (en) | 2010-12-09 | 2013-06-13 | Amgen Inc. | Bicyclic compounds as Pim inhibitors |
| CA2812223C (en) | 2010-12-17 | 2019-03-12 | Nerviano Medical Sciences S.R.L. | Substituted pyrazolo-quinazoline derivatives as kinase inhibitors |
| WO2012087881A1 (en) | 2010-12-20 | 2012-06-28 | Incyte Corporation | N-(1-(substituted-phenyl)ethyl)-9h-purin-6-amines as pi3k inhibitors |
| EP2668190B1 (en) | 2011-01-26 | 2016-08-17 | Nerviano Medical Sciences S.r.l. | Tricyclic pyrrolo derivatives, process for their preparation and their use as kinase inhibitors |
| WO2012101029A1 (en) | 2011-01-26 | 2012-08-02 | Nerviano Medical Sciences S.R.L. | Tricyclic derivatives, process for their preparation and their use as kinase inhibitors |
| JP6039585B2 (ja) | 2011-02-25 | 2016-12-07 | アレイ バイオファーマ、インコーポレイテッド | Ｐｉｍキナーゼ阻害剤としてのトリアゾロピリジン化合物 |
| EP2681197A1 (en) | 2011-03-04 | 2014-01-08 | Novartis AG | Tetrasubstituted cyclohexyl compounds as kinase inhibitors |
| UY33930A (es) * | 2011-03-04 | 2012-10-31 | Novartis Ag | Inhibidores novedosos de quinasas |
| WO2012125629A1 (en) | 2011-03-14 | 2012-09-20 | Incyte Corporation | Substituted diamino-pyrimidine and diamino-pyridine derivatives as pi3k inhibitors |
| CA2830780A1 (en) | 2011-03-22 | 2012-09-27 | Amgen Inc. | Azole compounds as pim inhibitors |
| WO2012135009A1 (en) | 2011-03-25 | 2012-10-04 | Incyte Corporation | Pyrimidine-4,6-diamine derivatives as pi3k inhibitors |
| AP2013007159A0 (en) | 2011-04-05 | 2013-10-31 | Pfizer Ltd | Pyrrolo [2,3-D] pyrimidine derivatives as inhibitors of tropomyosin-related kinase |
| US9284298B2 (en) | 2011-04-11 | 2016-03-15 | Nerviano Medical Sciences S.R.L. | Pyrazolyl-pyrimidine derivatives as kinase inhibitors |
| AU2012245344B2 (en) | 2011-04-22 | 2017-11-09 | Jasco Pharmaceuticals, LLC | Aminopyrimidine kinase inhibitors |
| GB201107176D0 (en) | 2011-04-28 | 2011-06-15 | Cxr Biosciences Ltd | Pyrrolnitrin derivatives |
| GB201107197D0 (en) | 2011-04-28 | 2011-06-15 | Cxr Biosciences Ltd | Compounds |
| CA2834166A1 (en) | 2011-04-29 | 2012-11-01 | Amgen Inc. | Bicyclic pyridazine compounds as pim inhibitors |
| CN103687858B (zh) | 2011-05-17 | 2017-11-21 | 拜耳知识产权有限责任公司 | 作为mknk1激酶抑制剂的氨基取代的咪唑并哒嗪 |
| CA2872979C (en) | 2011-05-19 | 2020-02-18 | Joaquin Pastor Fernandez | Macrocyclic compounds as protein kinase inhibitors |
| KR20140048891A (ko) | 2011-05-27 | 2014-04-24 | 템플 유니버시티-오브 더 커먼웰쓰 시스템 오브 하이어 에듀케이션 | 치환된 2-벤질리덴-2H-벤조[b][1,4]티아진-3(4H)-온, 이의 유도체, 및 이의 치료적 용도 |
| US9730929B2 (en) | 2011-06-01 | 2017-08-15 | Bayer Intellectual Property Gmbh | Substituted aminoimidazopyridazines |
| WO2012170827A2 (en) | 2011-06-08 | 2012-12-13 | Cylene Pharmaceuticals, Inc. | Pyrazolopyrimidines and related heterocycles as ck2 inhibitors |
| US8691807B2 (en) | 2011-06-20 | 2014-04-08 | Incyte Corporation | Azetidinyl phenyl, pyridyl or pyrazinyl carboxamide derivatives as JAK inhibitors |
| HK1197063A1 (en) | 2011-06-22 | 2015-01-02 | 拜耳知识产权有限责任公司 | Heterocyclyl aminoimidazopyridazines |
| US9416132B2 (en) | 2011-07-21 | 2016-08-16 | Tolero Pharmaceuticals, Inc. | Substituted imidazo[1,2-b]pyridazines as protein kinase inhibitors |
| CN102924446B (zh) | 2011-08-11 | 2015-08-26 | 上海吉铠医药科技有限公司 | Pim激酶抑制剂及其制备方法与在制药中的应用 |
| CN103874700B (zh) | 2011-08-12 | 2018-03-30 | 霍夫曼-拉罗奇有限公司 | 吡唑并[3,4‑c]吡啶化合物和使用方法 |
| TW201313721A (zh) | 2011-08-18 | 2013-04-01 | Incyte Corp | 作為ｊａｋ抑制劑之環己基氮雜環丁烷衍生物 |
| JP5843524B2 (ja) | 2011-09-02 | 2016-01-13 | キヤノン株式会社 | 有機無機複合組成物、有機無機複合材料、光学素子および積層型回折光学素子 |
| LT3196202T (lt) | 2011-09-02 | 2019-07-10 | Incyte Holdings Corporation | Heterociklilaminai, kaip pi3k slopikliai |
| UA117092C2 (uk) | 2011-09-06 | 2018-06-25 | Байєр Інтеллектуал Проперті Гмбх | Амінозаміщені імідазопіридазини |
| UA111854C2 (uk) | 2011-09-07 | 2016-06-24 | Інсайт Холдінгс Корпорейшн | Способи і проміжні сполуки для отримання інгібіторів jak |
| CN103814029B (zh) | 2011-09-23 | 2016-10-12 | 拜耳知识产权有限责任公司 | 取代的咪唑并哒嗪 |
| KR20140074964A (ko) | 2011-09-27 | 2014-06-18 | 에프. 호프만-라 로슈 아게 | 피라졸-4-일-헤테로사이클릴-카복사마이드 화합물 및 사용 방법 |
| ES2639064T3 (es) | 2011-10-07 | 2017-10-25 | Nerviano Medical Sciences S.R.L. | Derivados de 3,4-dihidropirrolo[1,2-a]pirazin-1(2h)-ona sustituidos como inhibidores de cinasa |
| EP2788350B1 (en) | 2011-10-07 | 2017-12-06 | Nerviano Medical Sciences S.r.l. | 4-ALKYL SUBSTITUTED 3,4-DIHYDROPYRROLO[1,2-a]PYRAZIN-1(2H)-ONE DERIVATIVES AS KINASES INHIBITORS |
| CN104011046B (zh) | 2011-11-04 | 2017-05-03 | 嘉世高制药公司 | 氨基嘧啶激酶抑制剂 |
| US9394297B2 (en) | 2012-02-28 | 2016-07-19 | Amgen Inc. | Amides as pim inhibitors |
| WO2013134079A1 (en) | 2012-03-05 | 2013-09-12 | Amgen Inc. | Oxazolidinone compounds and derivatives thereof |
| US9777004B2 (en) | 2012-03-29 | 2017-10-03 | Bayer Intellectual Property Gmbh | Amino-substituted imidazopyridazines |
| AR090548A1 (es) | 2012-04-02 | 2014-11-19 | Incyte Corp | Azaheterociclobencilaminas biciclicas como inhibidores de pi3k |
| CN104321326B (zh) | 2012-04-04 | 2017-05-31 | 拜耳医药股份有限公司 | 氨基取代的咪唑并哒嗪 |
| TWI572605B (zh) | 2012-04-26 | 2017-03-01 | 必治妥美雅史谷比公司 | 血小板聚集之抑制劑 |
| JP6042529B2 (ja) | 2012-04-27 | 2016-12-14 | ノバルティス アーゲー | 環式橋頭エーテルｄｇａｔ１阻害剤 |
| RS58058B1 (sr) | 2012-05-09 | 2019-02-28 | Biogen Ma Inc | Modulatori nukleusnog transporta i njihove upotrebe |
| CN104302638B (zh) | 2012-05-15 | 2016-08-24 | 诺华股份有限公司 | 用于抑制abl1、abl2和bcr-abl1的活性的苯甲酰胺衍生物 |
| TW201406761A (zh) | 2012-05-18 | 2014-02-16 | Incyte Corp | 做爲ｊａｋ抑制劑之哌啶基環丁基取代之吡咯并吡啶及吡咯并嘧啶衍生物 |
| WO2013175388A1 (en) | 2012-05-21 | 2013-11-28 | Novartis Ag | Novel ring-substituted n-pyridinyl amides as kinase inhibitors |
| BR112014029115A8 (pt) | 2012-05-22 | 2018-04-03 | Idenix Pharmaceuticals Inc | Composto, composição farmacêutica, e, uso de um composto ou composição |
| TWI568722B (zh) | 2012-06-15 | 2017-02-01 | 葛蘭馬克製藥公司 | 作爲ｍＰＧＥＳ－１抑制劑之三唑酮化合物 |
| CN104428299B (zh) | 2012-06-27 | 2018-05-11 | 霍夫曼-拉罗奇有限公司 | 5-氮杂吲唑化合物及其使用方法 |
| TW201408652A (zh) | 2012-07-11 | 2014-03-01 | Hoffmann La Roche | 作爲ＲＯＲｃ調節劑之芳基磺內醯胺衍生物 |
| TW201414737A (zh) | 2012-07-13 | 2014-04-16 | 必治妥美雅史谷比公司 | 作爲激酶抑制劑之咪唑并三□甲腈 |
| WO2014022752A1 (en) | 2012-08-03 | 2014-02-06 | Amgen Inc. | Macrocycles as pim inhibitors |
| WO2014033631A1 (en) | 2012-08-31 | 2014-03-06 | Novartis Ag | N-(3-pyridyl) biarylamides as kinase inhibitors |
| WO2014033630A1 (en) | 2012-08-31 | 2014-03-06 | Novartis Ag | Novel aminothiazole carboxamides as kinase inhibitors |
| CN103664878A (zh) | 2012-09-12 | 2014-03-26 | 山东亨利医药科技有限责任公司 | 杂芳环及其衍生物类酪氨酸激酶抑制剂 |
| BR112015005743A2 (pt) | 2012-09-14 | 2017-07-04 | Abbvie Deutschland | derivados tricíclicos de quinoxalina e quinolina |
| SI2900657T1 (sl) | 2012-09-26 | 2020-07-31 | F. Hoffmann-La Roche Ag | Ciklični eter pirazol-4-il-heterociklil-karboksamidne spojine in načini uporabe |
| WO2014053568A1 (en) | 2012-10-02 | 2014-04-10 | Sanofi | Indolyldihydroimidazopyrimidinone derivatives, preparation thereof and therapeutic use thereof |
| BR112015008325B1 (pt) | 2012-10-16 | 2022-01-25 | Janssen Sciences Ireland Uc | Compostos antivirais contra o rsv, seu uso e composição farmacêutica que os compreende |
| CA2888816A1 (en) | 2012-11-01 | 2014-05-08 | Incyte Corporation | Tricyclic fused thiophene derivatives as jak inhibitors |
| EP2920176B1 (en) | 2012-11-19 | 2017-09-13 | Bayer Pharma Aktiengesellschaft | Aminoimidazopyridazines as mknk1 kinase inhibitors |
| WO2014079011A1 (en) | 2012-11-22 | 2014-05-30 | Agios Pharmaceuticals, Inc. | Heterocyclic compounds for inhibiting glutaminase and their methods of use |
| US9550463B2 (en) | 2012-12-07 | 2017-01-24 | Toyota Jidosha Kabushiki Kaisha | Vehicle body end section structure |
| PT4190786T (pt) | 2012-12-07 | 2025-05-29 | Vertex Pharma | Compostos úteis como inibidores da quinase atr |
| KR102075885B1 (ko) | 2012-12-18 | 2020-02-11 | 버텍스 파마슈티칼스 인코포레이티드 | 세균 감염 치료용 만노스 유도체 |
| US20150336960A1 (en) | 2012-12-19 | 2015-11-26 | Novartis Ag | Aryl-substituted fused bicyclic pyridazine compounds |
| CN104968656B (zh) | 2012-12-19 | 2017-08-11 | 诺华股份有限公司 | 自分泌运动因子抑制剂 |
| DK3067358T3 (da) | 2012-12-21 | 2019-11-04 | Gilead Sciences Inc | Polycykliske carbamoylpyridon-forbindelser og deres farmaceutiske anvendelse |
| EP3498701B1 (en) | 2012-12-21 | 2023-02-22 | Epizyme Inc | Prmt5 inhibitors and uses thereof |
| FR3000569B1 (fr) | 2013-01-03 | 2015-02-13 | Peugeot Citroen Automobiles Sa | Dispositif d'eclairage a ecran a bord(s) lumineux |
| JP6437452B2 (ja) | 2013-01-14 | 2018-12-12 | インサイト・ホールディングス・コーポレイションＩｎｃｙｔｅ Ｈｏｌｄｉｎｇｓ Ｃｏｒｐｏｒａｔｉｏｎ | Ｐｉｍキナーゼ阻害剤として有用な二環式芳香族カルボキサミド化合物 |
| LT2945939T (lt) | 2013-01-15 | 2020-07-27 | Incyte Holdings Corporation | Triazolkarboksamidai ir piridinkarboksamido junginiai, naudotini kaip pim kinazės inhibitoriai |
| TWI657090B (zh) | 2013-03-01 | 2019-04-21 | 英塞特控股公司 | 吡唑并嘧啶衍生物治療PI3Kδ 相關病症之用途 |
| BR112015021458B1 (pt) | 2013-03-06 | 2022-06-07 | Incyte Holdings Corporation | "processos e intermediários para preparar {1-{1-[3-flúor2-(trifluormetil)isonicotinoil] piperidin-4-il}-3-[4-(7hpirrolo[2,3-d]pirimidin-4-il)-1h-pirazol-1-il]azetidin-3-il}acetonitrila, útil no tratamento de doenças relacionadas com a atividade de janus quinases |
| JO3383B1 (ar) | 2013-03-14 | 2019-03-13 | Lilly Co Eli | مثبطات cdc7 |
| UY35421A (es) | 2013-03-15 | 2014-10-31 | Nihon Nohyaku Co Ltd | Compuesto heterocíclico condensado o su sal, insecticida agrícola u hortícola que comprende el comp uesto y método de uso del insecticida |
| TWI689490B (zh) | 2013-03-15 | 2020-04-01 | 英商邊緣生物科技有限公司 | 用於治療纖維化之經取代之芳族化合物及相關方法 |
| PE20151900A1 (es) | 2013-03-15 | 2016-01-20 | Global Blood Therapeutics Inc | Compuestos y sus usos para modular la hemoglobina |
| EA029309B1 (ru) | 2013-03-15 | 2018-03-30 | Идорсиа Фармасьютиклз Лтд | Производные пиридин-4-ила в качестве агонистов s1p/edg1 |
| US20160052926A1 (en) | 2013-03-15 | 2016-02-25 | Hutchison Medipharma Limited | Novel pyrimidine and pyridine compounds and usage thereof |
| CN105051015B (zh) | 2013-03-15 | 2018-09-25 | 日本烟草产业株式会社 | 吡唑-酰胺化合物和其医药用途 |
| TWI719464B (zh) | 2013-03-15 | 2021-02-21 | 美商英塞特控股公司 | 作為bet蛋白抑制劑之三環雜環 |
| US20140275108A1 (en) | 2013-03-15 | 2014-09-18 | Galderma Research & Development | Novel benzenesulfonamide compounds, method for synthesizing same, and use thereof in medicine as well as in cosmetics |
| RU2680100C9 (ru) | 2013-03-15 | 2019-04-18 | Плексксикон Инк. | Гетероциклические соединения и их применения |
| JO3279B1 (ar) | 2013-03-15 | 2018-09-16 | Respivert Ltd | مشتقات 2-((4- امينو -3- (3- فلورو-5- هيدروكسي فينيل)-h1- بيرازولو [d-3,4] بيرمدين-1-يل )ميثيل )- 3- (2- تراي فلورو ميثيل ) بينزيل ) كوينازولين -4 (h3)- واحد واستخدامها كمثبطات فوسفواينوسيتايد 3- كاينيز |
| AP2015008718A0 (en) | 2013-03-15 | 2015-09-30 | Global Blood Therapeutics Inc | Compounds and uses thereof for the modulation of hemoglobin |
| TWI742541B (zh) | 2013-03-15 | 2021-10-11 | 英商邊緣生物科技有限公司 | 用於治療肺纖維化、肝纖維化、皮膚纖維化及心臟纖維化之經取代之芳族化合物 |
| AR095443A1 (es) | 2013-03-15 | 2015-10-14 | Fundación Centro Nac De Investig Oncológicas Carlos Iii | Heterociclos condensados con acción sobre atr |
| US9308236B2 (en) | 2013-03-15 | 2016-04-12 | Bristol-Myers Squibb Company | Macrocyclic inhibitors of the PD-1/PD-L1 and CD80(B7-1)/PD-L1 protein/protein interactions |
| CN109134440A (zh) | 2013-03-15 | 2019-01-04 | 美国陶氏益农公司 | 除草化合物及其作为除草剂的用途 |
| WO2015021153A1 (en) | 2013-08-07 | 2015-02-12 | Incyte Corporation | Sustained release dosage forms for a jak1 inhibitor |
| EP3036238A1 (en) | 2013-08-23 | 2016-06-29 | Incyte Corporation | Furo- and thieno-pyridine carboxamide compounds useful as pim kinase inhibitors |
| SI3110409T1 (sl) | 2014-02-28 | 2018-11-30 | Incyte Corporation | Inhibitorji JAK1 za zdravljenje mielodisplastičnih sindromov |
| NZ763326A (en) | 2014-04-08 | 2023-04-28 | Incyte Holdings Corp | Treatment of b-cell malignancies by a combination jak and pi3k inhibitor |
| CR20160553A (es) | 2014-04-30 | 2017-04-25 | Incyte Corp | Procesos para preparar un inhibidor de jak1 y nuevas formas de este |
| WO2015184305A1 (en) | 2014-05-30 | 2015-12-03 | Incyte Corporation | TREATMENT OF CHRONIC NEUTROPHILIC LEUKEMIA (CNL) AND ATYPICAL CHRONIC MYELOID LEUKEMIA (aCML) BY INHIBITORS OF JAK1 |
| US10077277B2 (en) | 2014-06-11 | 2018-09-18 | Incyte Corporation | Bicyclic heteroarylaminoalkyl phenyl derivatives as PI3K inhibitors |
| US9580418B2 (en) | 2014-07-14 | 2017-02-28 | Incyte Corporation | Bicyclic aromatic carboxamide compounds useful as Pim kinase inhibitors |
| US9822124B2 (en) | 2014-07-14 | 2017-11-21 | Incyte Corporation | Bicyclic heteroaromatic carboxamide compounds useful as Pim kinase inhibitors |
| US9540347B2 (en) | 2015-05-29 | 2017-01-10 | Incyte Corporation | Pyridineamine compounds useful as Pim kinase inhibitors |
-
2014
- 2014-01-14 JP JP2015552897A patent/JP6437452B2/ja active Active
- 2014-01-14 EP EP14702167.9A patent/EP2943485B1/en active Active
- 2014-01-14 US US14/155,134 patent/US9278950B2/en active Active
- 2014-01-14 CA CA2897200A patent/CA2897200C/en active Active
- 2014-01-14 ES ES14702167T patent/ES2649156T3/es active Active
- 2014-01-14 WO PCT/US2014/011487 patent/WO2014110574A1/en not_active Ceased
-
2016
- 2016-01-20 US US15/001,826 patent/US9676750B2/en active Active
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| JP2016505021A5 (enExample) | ||
| JP7505023B2 (ja) | 疾患の治療用のホスホイノシチド３－キナーゼ（ｐｉ３ｋ）のアロステリッククロメノン阻害剤 | |
| KR101727211B1 (ko) | 신규한 피리도피리미딘 유도체 및 이의 용도 | |
| JP7068295B2 (ja) | Ｂ型肝炎ウイルス感染症の処置及び予防のための新規なテトラヒドロピリドピリミジン | |
| US20250263394A1 (en) | Compounds, preparation methods and uses thereof | |
| JP6437452B2 (ja) | Ｐｉｍキナーゼ阻害剤として有用な二環式芳香族カルボキサミド化合物 | |
| JP6377081B2 (ja) | 新規ピリミジン化合物 | |
| CN111467346B (zh) | 具有四氢吡喃基甲基的吡啶酮衍生物 | |
| JP2013528204A5 (enExample) | ||
| JP2010525023A5 (enExample) | ||
| EP3393472B1 (en) | 3-(1h-pyrazol-4-yl)pyridine allosteric modulators of the m4 muscarinic acetylcholine receptor | |
| PH12015502055B1 (en) | Compounds and pharmaceutical compositions thereof for the treatment of inflammatory disorders | |
| JP2022510689A (ja) | Ｒｅｔ阻害剤、医薬組成物およびその使用 | |
| AU2016219183B2 (en) | Substituted pyrazole compounds as RORgammaT inhibitors and uses thereof | |
| EP3197884A1 (en) | Aminotriazine derivatives useful as tank-binding kinase inhibitor compounds | |
| CN118055933B (zh) | 选择性parp1抑制剂及其应用 | |
| JP6057907B2 (ja) | チアゾリジン誘導体又はその塩を有効成分とする医薬品 | |
| IL257392A (en) | The troarils are converted to pyrazolil and their use as drugs | |
| ES2598830T3 (es) | Compuestos bicíclicos o sales de los mismos para el uso en el tratamiento del cáncer | |
| EA035739B1 (ru) | Конденсированные бициклические гетероарильные производные с активностью ингибиторов пролилгидроксилазы | |
| KR20170113629A (ko) | 포유류 티로신 키나제 ROR1 활성의 저해제로서 유용한 2-페닐-3H-이미다조[4,5-b]피리딘 유도체 | |
| KR20140025326A (ko) | 신규 인돌, 인다졸 유도체 또는 그 염 | |
| US20200024272A1 (en) | 2-phenylimidazo[4,5-b]pyridin-7-amine derivates useful as inhibitors of mammalian tyrosine kinase ror1 activity | |
| US11149036B2 (en) | 3-(1H-pyrazol-4-yl)pyridine allosteric modulators of the M4 muscarinic acetylcholine receptor | |
| US11339156B2 (en) | 3-(1H-pyrazol-4-yl)pyridine allosteric modulators of the M4 muscarinic acetylcholine receptor |