JP2014514322A5 - - Google Patents
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- JP2014514322A5 JP2014514322A5 JP2014506559A JP2014506559A JP2014514322A5 JP 2014514322 A5 JP2014514322 A5 JP 2014514322A5 JP 2014506559 A JP2014506559 A JP 2014506559A JP 2014506559 A JP2014506559 A JP 2014506559A JP 2014514322 A5 JP2014514322 A5 JP 2014514322A5
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- JP
- Japan
- Prior art keywords
- alkyl
- substituted
- compound
- cycloalkyl
- unsubstituted
- 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.)
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- 125000000217 alkyl group Chemical group 0.000 claims 68
- 150000001875 compounds Chemical class 0.000 claims 67
- -1 1-aminocyclohexyl Chemical group 0.000 claims 31
- 125000000753 cycloalkyl group Chemical group 0.000 claims 29
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 15
- 208000019425 cirrhosis of liver Diseases 0.000 claims 12
- 125000001995 cyclobutyl group Chemical group [H]C1([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims 8
- 239000000203 mixture Substances 0.000 claims 8
- 150000003839 salts Chemical class 0.000 claims 8
- 229940002612 prodrug Drugs 0.000 claims 7
- 239000000651 prodrug Substances 0.000 claims 7
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 6
- 125000001972 isopentyl group Chemical group [H]C([H])([H])C([H])(C([H])([H])[H])C([H])([H])C([H])([H])* 0.000 claims 6
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 6
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 6
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 claims 6
- 125000005119 alkyl cycloalkyl group Chemical group 0.000 claims 5
- 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 5
- 125000005936 piperidyl group Chemical group 0.000 claims 5
- 125000005916 2-methylpentyl group Chemical group 0.000 claims 4
- 125000005917 3-methylpentyl group Chemical group 0.000 claims 4
- 206010016654 Fibrosis Diseases 0.000 claims 4
- 108091000080 Phosphotransferase Proteins 0.000 claims 4
- 230000007882 cirrhosis Effects 0.000 claims 4
- 125000000582 cycloheptyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 claims 4
- 125000000640 cyclooctyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C([H])([H])C1([H])[H] 0.000 claims 4
- 125000001511 cyclopentyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims 4
- 229910052736 halogen Inorganic materials 0.000 claims 4
- 150000002367 halogens Chemical class 0.000 claims 4
- 208000006454 hepatitis Diseases 0.000 claims 4
- 231100000283 hepatitis Toxicity 0.000 claims 4
- 125000000959 isobutyl group Chemical group [H]C([H])([H])C([H])(C([H])([H])[H])C([H])([H])* 0.000 claims 4
- 208000008338 non-alcoholic fatty liver disease Diseases 0.000 claims 4
- 206010053219 non-alcoholic steatohepatitis Diseases 0.000 claims 4
- 125000003566 oxetanyl group Chemical group 0.000 claims 4
- 102000020233 phosphotransferase Human genes 0.000 claims 4
- 125000002914 sec-butyl group Chemical group [H]C([H])([H])C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 4
- 230000007863 steatosis Effects 0.000 claims 4
- 231100000240 steatosis hepatitis Toxicity 0.000 claims 4
- 125000001973 tert-pentyl group Chemical group [H]C([H])([H])C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 claims 4
- 125000003718 tetrahydrofuranyl group Chemical group 0.000 claims 4
- 125000001412 tetrahydropyranyl group Chemical group 0.000 claims 4
- 101000950695 Homo sapiens Mitogen-activated protein kinase 8 Proteins 0.000 claims 3
- 102100037808 Mitogen-activated protein kinase 8 Human genes 0.000 claims 3
- 239000008194 pharmaceutical composition Substances 0.000 claims 3
- 125000003764 2,4-dimethylpentyl group Chemical group [H]C([H])([H])C([H])(C([H])([H])[H])C([H])([H])C([H])(C([H])([H])[H])C([H])([H])* 0.000 claims 2
- 208000008439 Biliary Liver Cirrhosis Diseases 0.000 claims 2
- 208000033222 Biliary cirrhosis primary Diseases 0.000 claims 2
- 208000008964 Chemical and Drug Induced Liver Injury Diseases 0.000 claims 2
- 206010008609 Cholangitis sclerosing Diseases 0.000 claims 2
- 206010072268 Drug-induced liver injury Diseases 0.000 claims 2
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims 2
- 101000950669 Homo sapiens Mitogen-activated protein kinase 9 Proteins 0.000 claims 2
- 208000001145 Metabolic Syndrome Diseases 0.000 claims 2
- 102100037809 Mitogen-activated protein kinase 9 Human genes 0.000 claims 2
- 208000012654 Primary biliary cholangitis Diseases 0.000 claims 2
- 102000001253 Protein Kinase Human genes 0.000 claims 2
- 201000000690 abdominal obesity-metabolic syndrome Diseases 0.000 claims 2
- 230000001684 chronic effect Effects 0.000 claims 2
- 206010012601 diabetes mellitus Diseases 0.000 claims 2
- 206010073071 hepatocellular carcinoma Diseases 0.000 claims 2
- 231100000844 hepatocellular carcinoma Toxicity 0.000 claims 2
- 125000000623 heterocyclic group Chemical group 0.000 claims 2
- 208000015181 infectious disease Diseases 0.000 claims 2
- 230000002401 inhibitory effect Effects 0.000 claims 2
- 210000004185 liver Anatomy 0.000 claims 2
- 125000004108 n-butyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])C([H])([H])* 0.000 claims 2
- 125000004123 n-propyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])* 0.000 claims 2
- 125000001971 neopentyl group Chemical group [H]C([*])([H])C(C([H])([H])[H])(C([H])([H])[H])C([H])([H])[H] 0.000 claims 2
- 125000003538 pentan-3-yl group Chemical group [H]C([H])([H])C([H])([H])C([H])(*)C([H])([H])C([H])([H])[H] 0.000 claims 2
- 201000000742 primary sclerosing cholangitis Diseases 0.000 claims 2
- 108060006633 protein kinase Proteins 0.000 claims 2
- 208000010157 sclerosing cholangitis Diseases 0.000 claims 2
- 238000002054 transplantation Methods 0.000 claims 2
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims 1
- VSDOJRUZJYPUSK-UHFFFAOYSA-N 2-(2-aminoethylamino)-4-(cyclohexylamino)pyrimidine-5-carboxamide Chemical compound NCCNC1=NC=C(C(N)=O)C(NC2CCCCC2)=N1 VSDOJRUZJYPUSK-UHFFFAOYSA-N 0.000 claims 1
- ALYYEJSTMRTGLB-UHFFFAOYSA-N 2-(2-aminoethylamino)-4-(methylamino)pyrimidine-5-carboxamide Chemical compound CNC1=NC(NCCN)=NC=C1C(N)=O ALYYEJSTMRTGLB-UHFFFAOYSA-N 0.000 claims 1
- UAYBCKVPLZGCSH-UHFFFAOYSA-N 2-(2-aminopropylamino)-4-(cyclohexylamino)pyrimidine-5-carboxamide Chemical compound CC(N)CNC1=NC=C(C(N)=O)C(NC2CCCCC2)=N1 UAYBCKVPLZGCSH-UHFFFAOYSA-N 0.000 claims 1
- PRVXZIQLVKRULX-UHFFFAOYSA-N 4-(3-methylbutylamino)-2-[3-(2-methylpiperidin-1-yl)propylamino]pyrimidine-5-carbonitrile Chemical compound C1=C(C#N)C(NCCC(C)C)=NC(NCCCN2C(CCCC2)C)=N1 PRVXZIQLVKRULX-UHFFFAOYSA-N 0.000 claims 1
- GBKXVXDNYFHIKP-UHFFFAOYSA-N 4-(cycloheptylamino)-2-[3-(2-methylpiperidin-1-yl)propylamino]pyrimidine-5-carbonitrile Chemical compound CC1CCCCN1CCCNC1=NC=C(C#N)C(NC2CCCCCC2)=N1 GBKXVXDNYFHIKP-UHFFFAOYSA-N 0.000 claims 1
- ISISJCJHYKHXPT-UHFFFAOYSA-N 4-(cyclopentylamino)-2-(methylamino)pyrimidine-5-carboxamide Chemical compound CNC1=NC=C(C(N)=O)C(NC2CCCC2)=N1 ISISJCJHYKHXPT-UHFFFAOYSA-N 0.000 claims 1
- OBRZLFUDLHNMRP-UHFFFAOYSA-N 4-[(4-methylcyclohexyl)amino]-2-[3-(2-methylpiperidin-1-yl)propylamino]pyrimidine-5-carbonitrile Chemical compound C1CC(C)CCC1NC1=NC(NCCCN2C(CCCC2)C)=NC=C1C#N OBRZLFUDLHNMRP-UHFFFAOYSA-N 0.000 claims 1
- NXCAXRYHCPZKEI-UHFFFAOYSA-N CC(CC(=O)ONOC(CC(C)C)=O)C Chemical compound CC(CC(=O)ONOC(CC(C)C)=O)C NXCAXRYHCPZKEI-UHFFFAOYSA-N 0.000 claims 1
- BRSWQCNLEUCCPD-UHFFFAOYSA-N CC(CCC(=O)ONOC(CCC(C)C)=O)C Chemical compound CC(CCC(=O)ONOC(CCC(C)C)=O)C BRSWQCNLEUCCPD-UHFFFAOYSA-N 0.000 claims 1
- HVHCSIIAFMYLLX-UHFFFAOYSA-N CC1CCC(CC1)NC1=NC=C(C=N1)C#N Chemical compound CC1CCC(CC1)NC1=NC=C(C=N1)C#N HVHCSIIAFMYLLX-UHFFFAOYSA-N 0.000 claims 1
- 125000005879 dioxolanyl group Chemical group 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 125000002541 furyl group Chemical group 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 125000004076 pyridyl group Chemical group 0.000 claims 1
- 125000000719 pyrrolidinyl group Chemical group 0.000 claims 1
- 239000003981 vehicle Substances 0.000 claims 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201161478076P | 2011-04-22 | 2011-04-22 | |
| US61/478,076 | 2011-04-22 | ||
| US201161555339P | 2011-11-03 | 2011-11-03 | |
| US61/555,339 | 2011-11-03 | ||
| PCT/US2012/034349 WO2012145569A1 (en) | 2011-04-22 | 2012-04-20 | Substituted diaminocarboxamide and diaminocarbonitrile pyrimidines, compositions thereof, and methods of treatment therewith |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016202099A Division JP6502302B2 (ja) | 2011-04-22 | 2016-10-13 | 置換されたジアミノカルボキサミドおよびジアミノカルボニトリルピリミジン、その組成物、ならびに、それを用いた治療方法 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2014514322A JP2014514322A (ja) | 2014-06-19 |
| JP2014514322A5 true JP2014514322A5 (enExample) | 2015-12-24 |
| JP6027095B2 JP6027095B2 (ja) | 2016-11-16 |
Family
ID=46025954
Family Applications (5)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2014506559A Active JP6027095B2 (ja) | 2011-04-22 | 2012-04-20 | 置換されたジアミノカルボキサミドおよびジアミノカルボニトリルピリミジン、その組成物、ならびに、それを用いた治療方法 |
| JP2016202099A Active JP6502302B2 (ja) | 2011-04-22 | 2016-10-13 | 置換されたジアミノカルボキサミドおよびジアミノカルボニトリルピリミジン、その組成物、ならびに、それを用いた治療方法 |
| JP2019052826A Active JP6898961B2 (ja) | 2011-04-22 | 2019-03-20 | 置換されたジアミノカルボキサミドおよびジアミノカルボニトリルピリミジン、その組成物、ならびに、それを用いた治療方法 |
| JP2021098226A Active JP7374955B2 (ja) | 2011-04-22 | 2021-06-11 | 置換されたジアミノカルボキサミドおよびジアミノカルボニトリルピリミジン、その組成物、ならびに、それを用いた治療方法 |
| JP2023183330A Pending JP2023179797A (ja) | 2011-04-22 | 2023-10-25 | 置換されたジアミノカルボキサミドおよびジアミノカルボニトリルピリミジン、その組成物、ならびに、それを用いた治療方法 |
Family Applications After (4)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016202099A Active JP6502302B2 (ja) | 2011-04-22 | 2016-10-13 | 置換されたジアミノカルボキサミドおよびジアミノカルボニトリルピリミジン、その組成物、ならびに、それを用いた治療方法 |
| JP2019052826A Active JP6898961B2 (ja) | 2011-04-22 | 2019-03-20 | 置換されたジアミノカルボキサミドおよびジアミノカルボニトリルピリミジン、その組成物、ならびに、それを用いた治療方法 |
| JP2021098226A Active JP7374955B2 (ja) | 2011-04-22 | 2021-06-11 | 置換されたジアミノカルボキサミドおよびジアミノカルボニトリルピリミジン、その組成物、ならびに、それを用いた治療方法 |
| JP2023183330A Pending JP2023179797A (ja) | 2011-04-22 | 2023-10-25 | 置換されたジアミノカルボキサミドおよびジアミノカルボニトリルピリミジン、その組成物、ならびに、それを用いた治療方法 |
Country Status (35)
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| MX375752B (es) | 2013-12-05 | 2025-03-06 | Pharmacyclics Llc | Inhibidores de tirosina quinasa de bruton. |
| CN108947867A (zh) | 2013-12-12 | 2018-12-07 | 卡利拉制药公司 | 双环烷基化合物及合成 |
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| IL301709B2 (en) * | 2017-08-09 | 2025-07-01 | Denali Therapeutics Inc | Compounds, compositions and methods |
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| CN107573249B (zh) * | 2017-09-25 | 2018-12-25 | 上海馨远医药科技有限公司 | 一种反式4-烷氧基环己胺的制备方法 |
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