JP2012501312A5 - - Google Patents
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- Publication number
- JP2012501312A5 JP2012501312A5 JP2011524403A JP2011524403A JP2012501312A5 JP 2012501312 A5 JP2012501312 A5 JP 2012501312A5 JP 2011524403 A JP2011524403 A JP 2011524403A JP 2011524403 A JP2011524403 A JP 2011524403A JP 2012501312 A5 JP2012501312 A5 JP 2012501312A5
- Authority
- JP
- Japan
- Prior art keywords
- pyridin
- naphthyridin
- amino
- amine
- aminopiperidin
- 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
- -1 aminocarbonyloxy, aminosulfonyl Chemical group 0.000 claims 50
- 125000000753 cycloalkyl group Chemical group 0.000 claims 29
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims 17
- 150000001875 compounds Chemical class 0.000 claims 16
- 239000001257 hydrogen Substances 0.000 claims 16
- 229910052739 hydrogen Inorganic materials 0.000 claims 16
- 125000000217 alkyl group Chemical group 0.000 claims 15
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 15
- 125000001475 halogen functional group Chemical group 0.000 claims 14
- 125000001072 heteroaryl group Chemical group 0.000 claims 13
- 150000002431 hydrogen Chemical class 0.000 claims 11
- 125000003118 aryl group Chemical group 0.000 claims 10
- 125000002252 acyl group Chemical group 0.000 claims 8
- 125000003545 alkoxy group Chemical group 0.000 claims 7
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 7
- 125000004423 acyloxy group Chemical group 0.000 claims 6
- 125000003342 alkenyl group Chemical group 0.000 claims 6
- 125000004414 alkyl thio group Chemical group 0.000 claims 6
- 125000000304 alkynyl group Chemical group 0.000 claims 6
- 125000004104 aryloxy group Chemical group 0.000 claims 6
- 125000004093 cyano group Chemical group *C#N 0.000 claims 6
- 125000000000 cycloalkoxy group Chemical group 0.000 claims 6
- 125000005553 heteroaryloxy group Chemical group 0.000 claims 6
- 125000005844 heterocyclyloxy group Chemical group 0.000 claims 6
- 125000003386 piperidinyl group Chemical group 0.000 claims 6
- 125000003441 thioacyl group Chemical group 0.000 claims 6
- 150000003573 thiols Chemical class 0.000 claims 6
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 5
- 125000004193 piperazinyl group Chemical group 0.000 claims 5
- 125000000596 cyclohexenyl group Chemical group C1(=CCCCC1)* 0.000 claims 4
- 239000003814 drug Substances 0.000 claims 4
- 150000003839 salts Chemical class 0.000 claims 4
- 229920006395 saturated elastomer Polymers 0.000 claims 4
- 125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 claims 3
- 230000000694 effects Effects 0.000 claims 3
- 238000004519 manufacturing process Methods 0.000 claims 3
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 3
- 125000001424 substituent group Chemical group 0.000 claims 3
- 125000003107 substituted aryl group Chemical group 0.000 claims 3
- GOZBXWPQUSCSOL-YLJYHZDGSA-N (3r,4r)-1-[6-[6-(2,6-difluorophenyl)pyridin-2-yl]quinolin-4-yl]-4-fluoropiperidin-3-amine Chemical compound C1C[C@@H](F)[C@H](N)CN1C1=CC=NC2=CC=C(C=3N=C(C=CC=3)C=3C(=CC=CC=3F)F)C=C12 GOZBXWPQUSCSOL-YLJYHZDGSA-N 0.000 claims 2
- MVHATFDKNQITLT-IIBYNOLFSA-N (3r,4r)-3-amino-1-[6-[6-(1,3-thiazol-2-yl)pyridin-2-yl]quinolin-4-yl]piperidin-4-ol Chemical compound C1C[C@@H](O)[C@H](N)CN1C1=CC=NC2=CC=C(C=3N=C(C=CC=3)C=3SC=CN=3)C=C12 MVHATFDKNQITLT-IIBYNOLFSA-N 0.000 claims 2
- ATIMFZCPBCTHFM-NTKDMRAZSA-N (3r,4r)-3-amino-1-[6-[6-(2,6-difluorophenyl)pyridin-2-yl]quinolin-4-yl]piperidin-4-ol Chemical compound C1C[C@@H](O)[C@H](N)CN1C1=CC=NC2=CC=C(C=3N=C(C=CC=3)C=3C(=CC=CC=3F)F)C=C12 ATIMFZCPBCTHFM-NTKDMRAZSA-N 0.000 claims 2
- HRJZGPILOHKMOC-INIZCTEOSA-N (3s)-1-[6-[4-(2,6-difluorophenyl)pyrimidin-2-yl]quinolin-4-yl]piperidin-3-amine Chemical compound C1[C@@H](N)CCCN1C1=CC=NC2=CC=C(C=3N=C(C=CN=3)C=3C(=CC=CC=3F)F)C=C12 HRJZGPILOHKMOC-INIZCTEOSA-N 0.000 claims 2
- HUSFRIKYCASQCP-WBVHZDCISA-N (3s,5r)-5-methyl-1-[6-[6-(1,3-thiazol-2-yl)pyridin-2-yl]quinolin-4-yl]piperidin-3-amine Chemical compound C1[C@H](C)C[C@H](N)CN1C1=CC=NC2=CC=C(C=3N=C(C=CC=3)C=3SC=CN=3)C=C12 HUSFRIKYCASQCP-WBVHZDCISA-N 0.000 claims 2
- 125000006645 (C3-C4) cycloalkyl group Chemical group 0.000 claims 2
- ZSWOHSKPVUUOAX-UHFFFAOYSA-N 2-[4-(2-amino-6-methylpyridin-4-yl)-1,7-naphthyridin-6-yl]-6-(2,6-difluorophenyl)pyridin-3-amine Chemical compound NC1=NC(C)=CC(C=2C3=CC(=NC=C3N=CC=2)C=2C(=CC=C(N=2)C=2C(=CC=CC=2F)F)N)=C1 ZSWOHSKPVUUOAX-UHFFFAOYSA-N 0.000 claims 2
- OYJREFHZQJZOJS-CQSZACIVSA-N 2-[4-[(3r)-3-aminopiperidin-1-yl]-1,7-naphthyridin-6-yl]-6-(2,6-difluorophenyl)pyridin-3-amine Chemical compound C1[C@H](N)CCCN1C1=CC=NC2=CN=C(C=3C(=CC=C(N=3)C=3C(=CC=CC=3F)F)N)C=C12 OYJREFHZQJZOJS-CQSZACIVSA-N 0.000 claims 2
- YUORUIOLJWUERY-ZDUSSCGKSA-N 2-[4-[(3s)-3-aminopiperidin-1-yl]-1,7-naphthyridin-6-yl]-6-(1,3-thiazol-2-yl)pyridin-3-amine Chemical compound C1[C@@H](N)CCCN1C1=CC=NC2=CN=C(C=3C(=CC=C(N=3)C=3SC=CN=3)N)C=C12 YUORUIOLJWUERY-ZDUSSCGKSA-N 0.000 claims 2
- DEUGTHPDIWIBNL-AWEZNQCLSA-N 2-[4-[(3s)-3-aminopiperidin-1-yl]-1,7-naphthyridin-6-yl]-6-(2,3-difluorophenyl)pyridin-3-amine Chemical compound C1[C@@H](N)CCCN1C1=CC=NC2=CN=C(C=3C(=CC=C(N=3)C=3C(=C(F)C=CC=3)F)N)C=C12 DEUGTHPDIWIBNL-AWEZNQCLSA-N 0.000 claims 2
- UVWWZIDGIDLXSG-HNNXBMFYSA-N 2-[4-[(3s)-3-aminopiperidin-1-yl]-1,7-naphthyridin-6-yl]-6-(2,4-difluorophenyl)pyridin-3-amine Chemical compound C1[C@@H](N)CCCN1C1=CC=NC2=CN=C(C=3C(=CC=C(N=3)C=3C(=CC(F)=CC=3)F)N)C=C12 UVWWZIDGIDLXSG-HNNXBMFYSA-N 0.000 claims 2
- OYJREFHZQJZOJS-AWEZNQCLSA-N 2-[4-[(3s)-3-aminopiperidin-1-yl]-1,7-naphthyridin-6-yl]-6-(2,6-difluorophenyl)pyridin-3-amine Chemical compound C1[C@@H](N)CCCN1C1=CC=NC2=CN=C(C=3C(=CC=C(N=3)C=3C(=CC=CC=3F)F)N)C=C12 OYJREFHZQJZOJS-AWEZNQCLSA-N 0.000 claims 2
- LPLKMKMFBBFYQP-HNNXBMFYSA-N 2-[4-[(3s)-3-aminopiperidin-1-yl]-1,7-naphthyridin-6-yl]-6-(2-fluorophenyl)pyridin-3-amine Chemical compound C1[C@@H](N)CCCN1C1=CC=NC2=CN=C(C=3C(=CC=C(N=3)C=3C(=CC=CC=3)F)N)C=C12 LPLKMKMFBBFYQP-HNNXBMFYSA-N 0.000 claims 2
- WVZUHFMFJOSMPG-KRWDZBQOSA-N 2-[4-[(3s)-3-aminopiperidin-1-yl]-1,7-naphthyridin-6-yl]-6-(3-methylsulfonylphenyl)pyridin-3-amine Chemical compound CS(=O)(=O)C1=CC=CC(C=2N=C(C(N)=CC=2)C=2N=CC3=NC=CC(=C3C=2)N2C[C@@H](N)CCC2)=C1 WVZUHFMFJOSMPG-KRWDZBQOSA-N 0.000 claims 2
- HREPMROSVIOQON-KRWDZBQOSA-N 2-[4-[(3s)-3-aminopiperidin-1-yl]-1,7-naphthyridin-6-yl]-6-(4-fluorophenyl)pyridin-3-amine Chemical compound C1[C@@H](N)CCCN1C1=CC=NC2=CN=C(C=3C(=CC=C(N=3)C=3C=CC(F)=CC=3)N)C=C12 HREPMROSVIOQON-KRWDZBQOSA-N 0.000 claims 2
- CTIFOGRUVOEDFK-KRWDZBQOSA-N 2-[4-[(3s)-3-aminopiperidin-1-yl]-1,7-naphthyridin-6-yl]-6-(4-methylsulfonylphenyl)pyridin-3-amine Chemical compound C1=CC(S(=O)(=O)C)=CC=C1C1=CC=C(N)C(C=2N=CC3=NC=CC(=C3C=2)N2C[C@@H](N)CCC2)=N1 CTIFOGRUVOEDFK-KRWDZBQOSA-N 0.000 claims 2
- FDBXKVKVXBEYCA-HNNXBMFYSA-N 2-[4-[(3s)-3-aminopiperidin-1-yl]-1,7-naphthyridin-6-yl]-6-(6-methoxypyridin-2-yl)pyridin-3-amine Chemical compound COC1=CC=CC(C=2N=C(C(N)=CC=2)C=2N=CC3=NC=CC(=C3C=2)N2C[C@@H](N)CCC2)=N1 FDBXKVKVXBEYCA-HNNXBMFYSA-N 0.000 claims 2
- UPWAQZXGUQYYTH-KRWDZBQOSA-N 2-[4-[(3s)-3-aminopiperidin-1-yl]-1,7-naphthyridin-6-yl]-6-phenylpyridin-3-amine Chemical compound C1[C@@H](N)CCCN1C1=CC=NC2=CN=C(C=3C(=CC=C(N=3)C=3C=CC=CC=3)N)C=C12 UPWAQZXGUQYYTH-KRWDZBQOSA-N 0.000 claims 2
- HVLSMSVGNNNZJZ-AWEZNQCLSA-N 2-[4-[(3s)-3-aminopiperidin-1-yl]-1,7-naphthyridin-6-yl]-6-thiophen-2-ylpyridin-3-amine Chemical compound C1[C@@H](N)CCCN1C1=CC=NC2=CN=C(C=3C(=CC=C(N=3)C=3SC=CC=3)N)C=C12 HVLSMSVGNNNZJZ-AWEZNQCLSA-N 0.000 claims 2
- SETCJYIDTBJZQT-LBPRGKRZSA-N 2-[4-[(3s)-3-aminopiperidin-1-yl]-3-fluoro-1,7-naphthyridin-6-yl]-6-(1,3-thiazol-2-yl)pyridin-3-amine Chemical compound C1[C@@H](N)CCCN1C1=C(F)C=NC2=CN=C(C=3C(=CC=C(N=3)C=3SC=CN=3)N)C=C12 SETCJYIDTBJZQT-LBPRGKRZSA-N 0.000 claims 2
- YKSJVFFKFZUNCD-UHFFFAOYSA-N 3-[5-amino-6-[4-(2-amino-6-methylpyridin-4-yl)-1,7-naphthyridin-6-yl]pyridin-2-yl]-4-fluoro-n-propan-2-ylbenzamide Chemical compound CC(C)NC(=O)C1=CC=C(F)C(C=2N=C(C(N)=CC=2)C=2N=CC3=NC=CC(=C3C=2)C=2C=C(N)N=C(C)C=2)=C1 YKSJVFFKFZUNCD-UHFFFAOYSA-N 0.000 claims 2
- KWEQYIYARKVRPE-GOSISDBHSA-N 3-[5-amino-6-[4-[(3r)-3-aminopiperidin-1-yl]-1,7-naphthyridin-6-yl]pyridin-2-yl]-4-fluoro-n-propan-2-ylbenzamide Chemical compound CC(C)NC(=O)C1=CC=C(F)C(C=2N=C(C(N)=CC=2)C=2N=CC3=NC=CC(=C3C=2)N2C[C@H](N)CCC2)=C1 KWEQYIYARKVRPE-GOSISDBHSA-N 0.000 claims 2
- GGOVNNBQWDKAJJ-KRWDZBQOSA-N 3-[5-amino-6-[4-[(3s)-3-aminopiperidin-1-yl]-1,7-naphthyridin-6-yl]pyridin-2-yl]-4-fluoro-n,n-dimethylbenzamide Chemical compound CN(C)C(=O)C1=CC=C(F)C(C=2N=C(C(N)=CC=2)C=2N=CC3=NC=CC(=C3C=2)N2C[C@@H](N)CCC2)=C1 GGOVNNBQWDKAJJ-KRWDZBQOSA-N 0.000 claims 2
- FUDKTSYUNRLCTD-FQEVSTJZSA-N 3-[5-amino-6-[4-[(3s)-3-aminopiperidin-1-yl]-1,7-naphthyridin-6-yl]pyridin-2-yl]-4-fluoro-n-phenylbenzamide Chemical compound C1[C@@H](N)CCCN1C1=CC=NC2=CN=C(C=3C(=CC=C(N=3)C=3C(=CC=C(C=3)C(=O)NC=3C=CC=CC=3)F)N)C=C12 FUDKTSYUNRLCTD-FQEVSTJZSA-N 0.000 claims 2
- KWEQYIYARKVRPE-SFHVURJKSA-N 3-[5-amino-6-[4-[(3s)-3-aminopiperidin-1-yl]-1,7-naphthyridin-6-yl]pyridin-2-yl]-4-fluoro-n-propan-2-ylbenzamide Chemical compound CC(C)NC(=O)C1=CC=C(F)C(C=2N=C(C(N)=CC=2)C=2N=CC3=NC=CC(=C3C=2)N2C[C@@H](N)CCC2)=C1 KWEQYIYARKVRPE-SFHVURJKSA-N 0.000 claims 2
- HMTIPZSXXLHSMP-FQEVSTJZSA-N 3-[5-amino-6-[4-[(3s)-3-aminopiperidin-1-yl]-1,7-naphthyridin-6-yl]pyridin-2-yl]-n-cyclohexyl-4-fluorobenzamide Chemical compound C1[C@@H](N)CCCN1C1=CC=NC2=CN=C(C=3C(=CC=C(N=3)C=3C(=CC=C(C=3)C(=O)NC3CCCCC3)F)N)C=C12 HMTIPZSXXLHSMP-FQEVSTJZSA-N 0.000 claims 2
- BKZKUNVXXLXOJM-KRWDZBQOSA-N 3-[5-amino-6-[4-[(3s)-3-aminopiperidin-1-yl]-3-fluoro-1,7-naphthyridin-6-yl]pyridin-2-yl]-4-fluoro-n-propan-2-ylbenzamide Chemical compound CC(C)NC(=O)C1=CC=C(F)C(C=2N=C(C(N)=CC=2)C=2N=CC3=NC=C(F)C(N4C[C@@H](N)CCC4)=C3C=2)=C1 BKZKUNVXXLXOJM-KRWDZBQOSA-N 0.000 claims 2
- XLQOSTSZIBAZPH-AWEZNQCLSA-N 4-[4-[(3s)-3-aminopiperidin-1-yl]-1,7-naphthyridin-6-yl]-2-(2-fluorophenyl)pyrimidin-5-amine Chemical compound C1[C@@H](N)CCCN1C1=CC=NC2=CN=C(C=3C(=CN=C(N=3)C=3C(=CC=CC=3)F)N)C=C12 XLQOSTSZIBAZPH-AWEZNQCLSA-N 0.000 claims 2
- XNJBFWQURVDFJO-UHFFFAOYSA-N S1C(=NC=C1)C1=CC=CC(=N1)C=1C=C2C(=CC=NC2=CC1)C1CCC(CN1)N Chemical compound S1C(=NC=C1)C1=CC=CC(=N1)C=1C=C2C(=CC=NC2=CC1)C1CCC(CN1)N XNJBFWQURVDFJO-UHFFFAOYSA-N 0.000 claims 2
- QQDJGJUETVITCD-UHFFFAOYSA-N S1C(=NC=C1)C1=CC=CC(=N1)C=1C=C2C(=CC=NC2=CN1)C1CCC(CN1)N Chemical compound S1C(=NC=C1)C1=CC=CC(=N1)C=1C=C2C(=CC=NC2=CN1)C1CCC(CN1)N QQDJGJUETVITCD-UHFFFAOYSA-N 0.000 claims 2
- 125000004442 acylamino group Chemical group 0.000 claims 2
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 2
- 125000006310 cycloalkyl amino group Chemical group 0.000 claims 2
- 230000002401 inhibitory effect Effects 0.000 claims 2
- 229910052757 nitrogen Inorganic materials 0.000 claims 2
- 239000008194 pharmaceutical composition Substances 0.000 claims 2
- 125000004549 quinolin-4-yl group Chemical group N1=CC=C(C2=CC=CC=C12)* 0.000 claims 2
- PFDKGWBVVPMQGY-IAGOWNOFSA-N (3r,4r)-4-fluoro-1-[6-[6-(1,3-thiazol-2-yl)pyridin-2-yl]quinolin-4-yl]piperidin-3-amine Chemical compound C1C[C@@H](F)[C@H](N)CN1C1=CC=NC2=CC=C(C=3N=C(C=CC=3)C=3SC=CN=3)C=C12 PFDKGWBVVPMQGY-IAGOWNOFSA-N 0.000 claims 1
- KRZJRNZICWNMOA-GXSJLCMTSA-N (3s,4r)-4,8-dihydroxy-3-methoxy-3,4-dihydro-2h-naphthalen-1-one Chemical compound C1=CC=C2[C@@H](O)[C@@H](OC)CC(=O)C2=C1O KRZJRNZICWNMOA-GXSJLCMTSA-N 0.000 claims 1
- OHUYDZVINKITJA-AEFFLSMTSA-N (3s,5r)-1-[6-[6-(2,6-difluorophenyl)pyridin-2-yl]quinolin-4-yl]-5-methylpiperidin-3-amine Chemical compound C1[C@H](C)C[C@H](N)CN1C1=CC=NC2=CC=C(C=3N=C(C=CC=3)C=3C(=CC=CC=3F)F)C=C12 OHUYDZVINKITJA-AEFFLSMTSA-N 0.000 claims 1
- 206010028980 Neoplasm Diseases 0.000 claims 1
- 108091000080 Phosphotransferase Proteins 0.000 claims 1
- GTGFEYLGSCNMKQ-UHFFFAOYSA-N S1C(=NC=C1)C1=NC(=NC=C1)C1(CC=NC2=CC=CC=C12)C1CCC(CN1)N Chemical compound S1C(=NC=C1)C1=NC(=NC=C1)C1(CC=NC2=CC=CC=C12)C1CCC(CN1)N GTGFEYLGSCNMKQ-UHFFFAOYSA-N 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- 239000003795 chemical substances by application Substances 0.000 claims 1
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 1
- 230000010354 integration Effects 0.000 claims 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 1
- 239000000203 mixture Substances 0.000 claims 1
- 229910017464 nitrogen compound Inorganic materials 0.000 claims 1
- 150000002830 nitrogen compounds Chemical class 0.000 claims 1
- 102000020233 phosphotransferase Human genes 0.000 claims 1
- PEUGKEHLRUVPAN-UHFFFAOYSA-N piperidin-3-amine Chemical compound NC1CCCNC1 PEUGKEHLRUVPAN-UHFFFAOYSA-N 0.000 claims 1
- 230000001566 pro-viral effect Effects 0.000 claims 1
- 125000003373 pyrazinyl 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
- 229940124597 therapeutic agent Drugs 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US9366908P | 2008-09-02 | 2008-09-02 | |
| US61/093,669 | 2008-09-02 | ||
| PCT/EP2009/061182 WO2010026121A1 (en) | 2008-09-02 | 2009-08-31 | Bicyclic kinase inhibitors |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2012501312A JP2012501312A (ja) | 2012-01-19 |
| JP2012501312A5 true JP2012501312A5 (enExample) | 2012-10-11 |
| JP5564045B2 JP5564045B2 (ja) | 2014-07-30 |
Family
ID=41211220
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2011524403A Expired - Fee Related JP5564045B2 (ja) | 2008-09-02 | 2009-08-31 | 二環式キナーゼ阻害剤 |
Country Status (11)
| Country | Link |
|---|---|
| US (1) | US8735424B2 (enExample) |
| EP (1) | EP2342190A1 (enExample) |
| JP (1) | JP5564045B2 (enExample) |
| KR (1) | KR20110058866A (enExample) |
| CN (1) | CN102203075B (enExample) |
| AU (1) | AU2009289316A1 (enExample) |
| BR (1) | BRPI0918496A2 (enExample) |
| CA (1) | CA2735779A1 (enExample) |
| EA (1) | EA201100426A1 (enExample) |
| MX (1) | MX2011002367A (enExample) |
| WO (1) | WO2010026121A1 (enExample) |
Families Citing this family (49)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DK3184526T3 (en) | 2005-12-13 | 2019-01-14 | Incyte Holdings Corp | PYRROLO [2,3-D] PYRIMIDINE DERIVATIVES AS A JANUS-KINASE INHIBITOR |
| EP2740731B1 (en) | 2007-06-13 | 2016-03-23 | Incyte Holdings Corporation | Crystalline salts of the janus kinase inhibitor (r)-3-(4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)-1h-pyrazol-1-yl)-3-cyclopentylpropanenitrile |
| ES2487542T3 (es) | 2009-05-22 | 2014-08-21 | Incyte Corporation | Derivados de N-(hetero)aril-pirrolidina de pirazol-4-il-pirrolo[2,3-d]pirimidinas y pirrol-3-il-pirrolo[2,3-d]pirimidinas como inhibidores de cinasas Janus |
| WO2010135621A1 (en) | 2009-05-22 | 2010-11-25 | Incyte Corporation | 3-[4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)-1h-pyrazol-1-yl]octane- or heptane-nitrile as jak inhibitors |
| WO2011028685A1 (en) | 2009-09-01 | 2011-03-10 | Incyte Corporation | Heterocyclic derivatives of pyrazol-4-yl-pyrrolo[2,3-d]pyrimidines as janus kinase inhibitors |
| SMT201800137T1 (it) | 2010-03-10 | 2018-07-17 | Incyte Holdings Corp | Derivati di piperidin-4-il azetidina come inibitori di jak1 |
| PH12012502296B1 (en) | 2010-05-21 | 2017-10-06 | Incyte Holdings Corp | Topical formulation for a jak inhibitor |
| ES2536415T3 (es) | 2010-11-19 | 2015-05-25 | Incyte Corporation | Pirrolopiridinas y pirrolopirimidinas sustituidas heterocíclicas como inhibidores de JAK |
| SG190839A1 (en) | 2010-11-19 | 2013-07-31 | Incyte Corp | Cyclobutyl substituted pyrrolopyridine and pyrrolopyrimidine derivatives as jak inhibitors |
| WO2012177606A1 (en) | 2011-06-20 | 2012-12-27 | Incyte Corporation | Azetidinyl phenyl, pyridyl or pyrazinyl carboxamide derivatives as jak inhibitors |
| ES2834093T3 (es) | 2011-07-21 | 2021-06-16 | Sumitomo Dainippon Pharma Oncology Inc | Inhibidores de proteína quinasa heterocíclicos |
| 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 |
| UA111854C2 (uk) | 2011-09-07 | 2016-06-24 | Інсайт Холдінгс Корпорейшн | Способи і проміжні сполуки для отримання інгібіторів jak |
| WO2013173720A1 (en) | 2012-05-18 | 2013-11-21 | Incyte Corporation | Piperidinylcyclobutyl substituted pyrrolopyridine and pyrrolopyrimidine derivatives as jak inhibitors |
| PE20151157A1 (es) | 2012-11-15 | 2015-08-19 | Incyte Corp | Formas de dosificacion de ruxolitinib de liberacion sostenida |
| EP2943485B1 (en) | 2013-01-14 | 2017-09-20 | Incyte Holdings Corporation | Bicyclic aromatic carboxamide compounds useful as pim kinase inhibitors |
| HUE050215T2 (hu) | 2013-01-15 | 2020-11-30 | Incyte Holdings Corp | Pim kináz inhibitorokként hasznos tiazolkarboxamid és piridinkarboxamid vegyületek |
| MA38287B1 (fr) | 2013-01-23 | 2018-08-31 | Astrazeneca Ab | Nouveaux dérivés aminopyrazine pour le traitement ou la prévention du cancer |
| LT3489239T (lt) | 2013-03-06 | 2022-03-10 | Incyte Holdings Corporation | Jak inhibitoriaus gamybos būdai ir tarpiniai junginiai |
| UA120499C2 (uk) | 2013-08-07 | 2019-12-26 | Інсайт Корпорейшн | Лікування захворювань із застосуванням лікарських форм з уповільненим вивільненням для інгібітора jak1 |
| TW201605866A (zh) | 2013-08-23 | 2016-02-16 | 英塞特公司 | 可用作ｐｉｍ激酶抑制劑之呋喃并－及噻吩并－吡啶甲醯胺化合物 |
| 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 |
| WO2016010897A1 (en) | 2014-07-14 | 2016-01-21 | Incyte Corporation | Bicyclic heteroaromatic 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 |
| TWI656121B (zh) * | 2014-08-04 | 2019-04-11 | 德商拜耳製藥公司 | ２－（嗎啉－４－基）－１，７－萘啶 |
| CL2015001657S1 (es) | 2014-12-15 | 2016-09-02 | Jjgc Indústria E Comércio De Materiais Dentários S A | Configuracion aplicada a implante oseo. |
| US9540347B2 (en) | 2015-05-29 | 2017-01-10 | Incyte Corporation | Pyridineamine compounds useful as Pim kinase inhibitors |
| US10376504B2 (en) | 2015-07-29 | 2019-08-13 | Merck, Sharp & Dohme Corp. | Substituted quinolinones as PDE9 inhibitors |
| WO2017019724A1 (en) | 2015-07-29 | 2017-02-02 | Merck Sharp & Dohme Corp. | Phenyl-cyanoquinolinone pde9 inhibitors |
| WO2017019726A1 (en) | 2015-07-29 | 2017-02-02 | Merck Sharp & Dohme Corp. | Oxy-cyanoquinolinone pde9 inhibitors |
| TWI734699B (zh) | 2015-09-09 | 2021-08-01 | 美商英塞特公司 | Ｐｉｍ激酶抑制劑之鹽 |
| WO2017059251A1 (en) | 2015-10-02 | 2017-04-06 | Incyte Corporation | Heterocyclic compounds useful as pim kinase inhibitors |
| MX2021006804A (es) | 2015-12-17 | 2023-01-13 | Merck Patent Gmbh | Antagonistas policiclicos del receptor 7/8 tipo toll (tlr7/8) y uso de los mismos en el tratamiento de trastornos inmunitarios. |
| RS63776B1 (sr) | 2016-07-14 | 2022-12-30 | Crinetics Pharmaceuticals Inc | Modulatori somatostatina i njihove upotrebe |
| CN105974036A (zh) * | 2016-07-31 | 2016-09-28 | 合肥远志医药科技开发有限公司 | 一种氨基吡啶异构体的检测方法 |
| RU2758686C2 (ru) | 2016-08-08 | 2021-11-01 | Мерк Патент Гмбх | Антагонисты tlr7/8 и их применение |
| WO2019113487A1 (en) | 2017-12-08 | 2019-06-13 | Incyte Corporation | Low dose combination therapy for treatment of myeloproliferative neoplasms |
| IL276302B2 (en) | 2018-01-30 | 2023-11-01 | Incyte Corp | Procedures for preparing [1-(3-fluoro-2-(trifluoromethyl(isonicotinyl}piperidine-4-one) |
| SMT202400306T1 (it) | 2018-03-30 | 2024-09-16 | Incyte Corp | Trattamento dell'idrosadenite suppurativa utilizzando inibitori di jak. |
| CA3095580A1 (en) | 2018-04-13 | 2019-10-17 | Sumitomo Dainippon Pharma Oncology, Inc. | Pim kinase inhibitors for treatment of myeloproliferative neoplasms and fibrosis associated with cancer |
| ES2950825T3 (es) * | 2018-08-24 | 2023-10-13 | Bayer Ag | Procedimiento para preparar 2-[(3R)-3--metilmofolin--4-il]-4-(1-metil-1H-pirazol-5-il)-8-(1H-pirazol-5-il)-1,7-naftiridina |
| HUE072069T2 (hu) | 2019-02-12 | 2025-10-28 | Sumitomo Pharma America Inc | 2-((1R,4R)-4-((3-(3-(trifluormetil)fenil)imidazo[1,2- b]piridazin-6-il)amino)ciklohexil)propán-2-ol sósavas sójának kristályos formája |
| US11833155B2 (en) | 2020-06-03 | 2023-12-05 | Incyte Corporation | Combination therapy for treatment of myeloproliferative neoplasms |
| CA3191084A1 (en) | 2020-09-09 | 2022-03-17 | Gerald Burke | Formulations of a somatostatin modulator |
| WO2022090101A1 (en) | 2020-10-26 | 2022-05-05 | Boehringer Ingelheim International Gmbh | Process for synthesis of 2,4-dichloro-5-aminopyrimidine |
| EP4277626A4 (en) * | 2021-01-14 | 2024-12-11 | Georgetown University | USP13 INHIBITORS AND METHODS OF USE THEREOF |
| CN113648294B (zh) * | 2021-08-26 | 2024-01-23 | 山东领海生物科技有限公司 | β-双磺酰亚胺取代酮类化合物在治疗癌症中的应用 |
| AU2023372386A1 (en) | 2022-10-31 | 2025-05-08 | Sumitomo Pharma America, Inc. | Pim1 inhibitor for treating myeloproliferative neoplasms |
| WO2024186839A1 (en) * | 2023-03-05 | 2024-09-12 | University Of Vermont And State Agricultural College | Bicyclic aryl sulfonamides, sulfones, and sulfonate esters as anti-parasitic agents |
Family Cites Families (18)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4017500A (en) * | 1973-07-16 | 1977-04-12 | Schering Corporation | Certain 8-amino-1,7-naphthyridines |
| DE3815617A1 (de) * | 1988-05-07 | 1989-11-16 | Bayer Ag | 4-aza-1,10-phenanthrolin-derivate, verfahren zu ihrer herstellung sowie ihre verwendung in schaedlingsbekaempfungsmitteln |
| DE4011105A1 (de) * | 1990-04-06 | 1991-10-10 | Bayer Ag | Neue 4-chinolyl-dihydropyridine, verfahren zu ihrer herstellung und ihre verwendung in arzneimitteln |
| US5204472A (en) * | 1990-04-06 | 1993-04-20 | Bayer Aktiengesellschaft | Quinoline and isoquinoline intermediates |
| GB9603095D0 (en) | 1996-02-14 | 1996-04-10 | Zeneca Ltd | Quinazoline derivatives |
| AR007857A1 (es) * | 1996-07-13 | 1999-11-24 | Glaxo Group Ltd | Compuestos heterociclicos fusionados como inhibidores de proteina tirosina quinasa, sus metodos de preparacion, intermediarios uso en medicina ycomposiciones farmaceuticas que los contienen. |
| EP0837063A1 (en) * | 1996-10-17 | 1998-04-22 | Pfizer Inc. | 4-Aminoquinazoline derivatives |
| GB9708917D0 (en) * | 1997-05-01 | 1997-06-25 | Pfizer Ltd | Compounds useful in therapy |
| CA2496164C (en) * | 2002-08-23 | 2010-11-09 | Chiron Corporation | Benzimidazole quinolinones and uses thereof |
| EP1558585B1 (en) * | 2002-10-04 | 2013-09-25 | Prana Biotechnology Limited | Neurologically-active compounds |
| JP4794446B2 (ja) * | 2003-09-23 | 2011-10-19 | メルク・シャープ・エンド・ドーム・コーポレイション | イソキノリン系カリウムチャンネル阻害薬 |
| EP1781293A1 (en) * | 2004-06-04 | 2007-05-09 | Amphora Discovery Corporation | Quinoline- and isoquinoline-based compounds exhibiting atp-utilizing enzyme inhibitory activity, and compositions, and uses thereof |
| JP2006219453A (ja) * | 2005-02-14 | 2006-08-24 | Tokyo Univ Of Pharmacy & Life Science | キノリン環を母核とする金属識別型二波長性蛍光分子 |
| EP1899332A1 (en) * | 2005-06-24 | 2008-03-19 | Gilead Sciences, Inc. | Pyrido(3,2-d)pyrimidines and pharmaceutical compositions useful for treating hepatitis c. |
| WO2008009078A2 (en) * | 2006-07-20 | 2008-01-24 | Gilead Sciences, Inc. | 4,6-dl- and 2,4,6-trisubstituted quinazoline derivatives useful for treating viral infections |
| PE20090717A1 (es) | 2007-05-18 | 2009-07-18 | Smithkline Beecham Corp | Derivados de quinolina como inhibidores de la pi3 quinasa |
| AR066660A1 (es) * | 2007-05-23 | 2009-09-02 | Genentech Inc | Prevencion y tratamiento de condiciones del ojo asociadas con su complemento |
| PT2344474E (pt) * | 2008-09-02 | 2015-12-28 | Novartis Ag | Derivados de picolinamida como inibidores de cinase |
-
2009
- 2009-08-31 US US13/060,971 patent/US8735424B2/en active Active
- 2009-08-31 WO PCT/EP2009/061182 patent/WO2010026121A1/en not_active Ceased
- 2009-08-31 CN CN200980143219.4A patent/CN102203075B/zh not_active Expired - Fee Related
- 2009-08-31 EA EA201100426A patent/EA201100426A1/ru unknown
- 2009-08-31 EP EP09782373A patent/EP2342190A1/en not_active Withdrawn
- 2009-08-31 AU AU2009289316A patent/AU2009289316A1/en not_active Abandoned
- 2009-08-31 KR KR1020117007560A patent/KR20110058866A/ko not_active Withdrawn
- 2009-08-31 BR BRPI0918496A patent/BRPI0918496A2/pt not_active IP Right Cessation
- 2009-08-31 CA CA2735779A patent/CA2735779A1/en not_active Abandoned
- 2009-08-31 MX MX2011002367A patent/MX2011002367A/es not_active Application Discontinuation
- 2009-08-31 JP JP2011524403A patent/JP5564045B2/ja not_active Expired - Fee Related
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