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
- Authority
- 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.)
- Granted
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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 (OSRAM) | 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)
| Country | Link |
|---|---|
| US (7) | US9139534B2 (OSRAM) |
| EP (2) | EP4328223A3 (OSRAM) |
| JP (5) | JP6027095B2 (OSRAM) |
| KR (2) | KR101962488B1 (OSRAM) |
| CN (5) | CN111499580A (OSRAM) |
| AR (1) | AR087151A1 (OSRAM) |
| AU (1) | AU2012245387C1 (OSRAM) |
| BR (1) | BR112013022813B1 (OSRAM) |
| CA (1) | CA2829264C (OSRAM) |
| CL (1) | CL2013003025A1 (OSRAM) |
| CO (1) | CO6821941A2 (OSRAM) |
| CR (1) | CR20130490A (OSRAM) |
| DK (1) | DK2699553T3 (OSRAM) |
| EC (1) | ECSP13012985A (OSRAM) |
| ES (1) | ES2968700T3 (OSRAM) |
| FI (1) | FI2699553T3 (OSRAM) |
| HR (1) | HRP20240097T1 (OSRAM) |
| HU (1) | HUE064883T2 (OSRAM) |
| IL (3) | IL228721A (OSRAM) |
| LT (1) | LT2699553T (OSRAM) |
| MX (1) | MX351754B (OSRAM) |
| NI (1) | NI201300113A (OSRAM) |
| PE (1) | PE20140502A1 (OSRAM) |
| PH (2) | PH12013501921A1 (OSRAM) |
| PL (1) | PL2699553T3 (OSRAM) |
| PT (1) | PT2699553T (OSRAM) |
| RS (1) | RS65202B1 (OSRAM) |
| RU (2) | RU2697712C2 (OSRAM) |
| SG (2) | SG194086A1 (OSRAM) |
| SI (1) | SI2699553T1 (OSRAM) |
| SM (1) | SMT202400031T1 (OSRAM) |
| TW (3) | TWI599563B (OSRAM) |
| UA (1) | UA120740C2 (OSRAM) |
| WO (1) | WO2012145569A1 (OSRAM) |
| ZA (1) | ZA201306471B (OSRAM) |
Families Citing this family (39)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| SG194086A1 (en) | 2011-04-22 | 2013-11-29 | Signal Pharm Llc | Substituted diaminocarboxamide and diaminocarbonitrile pyrimidines, compositions thereof, and methods of treatment therewith |
| ES2648226T3 (es) * | 2012-11-08 | 2017-12-29 | Bristol-Myers Squibb Company | Compuestos de pirimidina sustituidos con alquilamida útiles en la modulación de IL-12, IL-23 y/o IFN |
| AR095036A1 (es) | 2013-03-14 | 2015-09-16 | Kalyra Pharmaceuticals Inc | Compuestos analgésicos bicíclicos |
| CN104262328B (zh) * | 2013-09-18 | 2016-09-07 | 北京韩美药品有限公司 | 抑制btk和/或jak3激酶活性的化合物 |
| AU2014360446A1 (en) | 2013-12-05 | 2016-06-09 | Pharmacyclics, Llc | Inhibitors of Bruton's tyrosine kinase |
| WO2015089170A1 (en) | 2013-12-12 | 2015-06-18 | Kalyra Pharmaceuticals, Inc. | Bicyclic alkyl compounds and synthesis |
| MX2016007898A (es) * | 2013-12-20 | 2016-10-07 | Signal Pharm Llc | Compuestos diaminopirimidilo sustituidos, las composiciones de estos y los metodos de tratamiento con estos. |
| NZ715903A (en) * | 2014-01-30 | 2017-06-30 | Signal Pharm Llc | Solid forms of 2-(tert-butylamino)-4-((1r,3r,4r)-3-hydroxy-4-methylcyclohexylamino)-pyrimidine-5-carboxamide, compositions thereof and methods of their use |
| CN113336653A (zh) | 2014-03-07 | 2021-09-03 | 里科瑞尔姆Ip控股有限责任公司 | 螺桨烷衍生物及合成 |
| CN106999451B (zh) | 2014-09-17 | 2021-04-02 | 里科瑞尔姆Ip控股有限责任公司 | 双环化合物 |
| SG11201704827UA (en) * | 2014-12-16 | 2017-07-28 | Signal Pharm Llc | Formulations of 2-(tert-butylamino)-4-((1r,3r,4r)-3-hydroxy-4-methycyclohexylamino)-pyrimidine-5-carboxamide |
| WO2016100308A1 (en) | 2014-12-16 | 2016-06-23 | Signal Pharmaceuticals, Llc | Methods for measurement of inhibition of c-jun n-terminal kinase in skin |
| EP3250557B1 (en) * | 2015-01-29 | 2024-11-20 | Signal Pharmaceuticals, LLC | Isotopologues of 2-(tert-butylamino)-4-((1r,3r,4r)-3-hydroxy-4-methylcyclohexylamino)-pyrimidine-5-carboxamide |
| CN107922287B (zh) | 2015-07-24 | 2021-04-09 | 细胞基因公司 | 合成(1r,2r,5r)-5-氨基-2-甲基环己醇盐酸盐的方法和其中可用的中间体 |
| WO2018019244A1 (zh) * | 2016-07-27 | 2018-02-01 | 广东东阳光药业有限公司 | 2,6-二甲基嘧啶酮衍生物的盐及其用途 |
| WO2018029336A1 (en) | 2016-08-12 | 2018-02-15 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Methods for determining whether a subject was administered with an activator of the ppar beta/delta pathway. |
| WO2018049353A1 (en) * | 2016-09-12 | 2018-03-15 | Imago Pharmaceuticals, Inc. | Treatment of fibrotic disorders with jun n-terminal kinase inhibitors |
| EP3551180B1 (en) | 2016-12-09 | 2021-09-29 | Cadila Healthcare Limited | Treatment for primary biliary cholangitis |
| BR112019024155A2 (pt) | 2017-05-15 | 2020-06-02 | Recurium Ip Holdings, Llc | Compostos analgésicos |
| MY201438A (en) | 2017-08-09 | 2024-02-22 | Denali Therapeutics Inc | Compounds, compositions and methods |
| PT3676297T (pt) | 2017-09-01 | 2023-08-29 | Denali Therapeutics Inc | Compostos, composições e métodos |
| 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 |
| EP3704113B1 (en) | 2017-11-01 | 2023-10-11 | Bristol-Myers Squibb Company | Bridged bicyclic compounds as farnesoid x receptor modulators |
| WO2020168011A1 (en) | 2019-02-13 | 2020-08-20 | Denali Therapeutics Inc. | Compounds, compositions and methods |
| MA54959A (fr) | 2019-02-13 | 2021-12-22 | Denali Therapeutics Inc | Composés, compositions et procédés |
| WO2020187292A1 (zh) * | 2019-03-19 | 2020-09-24 | 北京赛特明强医药科技有限公司 | 2-取代吡唑氨基-4-取代氨基-5-嘧啶甲酰胺类化合物、组合物及其应用 |
| WO2021003417A1 (en) | 2019-07-03 | 2021-01-07 | Sumitomo Dainippon Pharma Oncology, Inc. | Tyrosine kinase non-receptor 1 (tnk1) inhibitors and uses thereof |
| MX2022001413A (es) * | 2019-08-06 | 2022-03-29 | Lilly Co Eli | Compuesto de pirimidina-5-carboxamida. |
| CN112574123B (zh) * | 2019-09-30 | 2024-06-11 | 武汉朗来科技发展有限公司 | Jnk抑制剂、其药物组合物和用途 |
| AU2021230288A1 (en) * | 2020-03-06 | 2022-09-01 | National Health Research Institutes | Pyrimidine compounds and their pharmaceutical uses |
| CN113698408B (zh) * | 2020-05-22 | 2025-07-25 | 武汉朗来科技发展有限公司 | Jnk抑制剂、其药物组合物和用途 |
| WO2022048684A1 (zh) * | 2020-09-07 | 2022-03-10 | 武汉朗来科技发展有限公司 | Jnk抑制剂、其药物组合物和用途 |
| EP4240362A4 (en) * | 2020-11-09 | 2024-10-23 | Merck Sharp & Dohme LLC | Diaminopyrimidine carboxamide inhibitors of hpk1 |
| US20240360125A9 (en) * | 2021-02-22 | 2024-10-31 | The Trustees Of Princeton University | 2-substituted bicyclo[1.1.1]pentanes |
| WO2023108536A1 (en) * | 2021-12-16 | 2023-06-22 | Lynk Pharmaceuticals Co. Ltd. | Tyk2 inhibitors and compositions and methods thereof |
| JP2025503448A (ja) | 2021-12-16 | 2025-02-04 | リンク ファーマシューティカルズ シーオー．エルティーディー． | Ｔｙｋ２阻害剤および組成物ならびにその方法 |
| CN114315738B (zh) * | 2022-01-15 | 2023-08-18 | 重庆东寰科技开发有限公司 | 一种2,4-二氨基嘧啶-3-氧化物的制备方法 |
| TW202434251A (zh) | 2022-11-04 | 2024-09-01 | 美商必治妥美雅史谷比公司 | 治療癌症之療法 |
| CN120457121A (zh) * | 2022-12-30 | 2025-08-08 | 杭州矩阵生物药业有限公司 | 具有jnk抑制活性的嘧啶类衍生物及其应用 |
Family Cites Families (84)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CH549339A (de) | 1971-05-12 | 1974-05-31 | Ciba Geigy Ag | Herbizides mittel. |
| US4301281A (en) * | 1979-04-18 | 1981-11-17 | American Home Products Corporation | 7,8-Dihydro-2,5,8-trisubstituted-7-oxo-pyrido[2,3-d]-pyrimidine-6-carboxylic acid amides |
| DE3338859A1 (de) * | 1983-10-26 | 1985-05-09 | Bayer Ag, 5090 Leverkusen | Substituierte pyrimidine |
| ES2301194T3 (es) * | 1997-02-05 | 2008-06-16 | Warner-Lambert Company Llc | Pirido 2,3-d pirimidinas y 4-aminopirimidinas como inhibidores de la proliferacion celular. |
| WO1999031073A1 (en) * | 1997-12-15 | 1999-06-24 | Yamanouchi Pharmaceutical Co., Ltd. | Novel pyrimidine-5-carboxamide derivatives |
| CN1138778C (zh) | 1998-05-26 | 2004-02-18 | 沃尼尔·朗伯公司 | 用作细胞增殖抑制剂的二环嘧啶及二环3,4-二氢嘧啶化合物及用途 |
| EP1107957B1 (en) | 1998-08-29 | 2006-10-18 | AstraZeneca AB | Pyrimidine compounds |
| JP4622047B2 (ja) | 1999-06-09 | 2011-02-02 | アステラス製薬株式会社 | 新規なヘテロ環カルボキサミド誘導体 |
| EP1184376B1 (en) * | 1999-06-09 | 2005-02-02 | Yamanouchi Pharmaceutical Co. Ltd. | Novel heterocyclic carboxamide derivatives |
| WO2000076980A1 (en) | 1999-06-10 | 2000-12-21 | Yamanouchi Pharmaceutical Co., Ltd. | Novel nitrogen-contaiing heterocyclic derivatives or salts thereof |
| CA2383546A1 (en) | 1999-06-30 | 2001-01-04 | William H. Parsons | Src kinase inhibitor compounds |
| GB0016877D0 (en) * | 2000-07-11 | 2000-08-30 | Astrazeneca Ab | Chemical compounds |
| JP4329290B2 (ja) * | 2000-10-06 | 2009-09-09 | 田辺三菱製薬株式会社 | 脂肪族含窒素五員環化合物 |
| TWI329105B (en) * | 2002-02-01 | 2010-08-21 | Rigel Pharmaceuticals Inc | 2,4-pyrimidinediamine compounds and their uses |
| GB0206215D0 (en) | 2002-03-15 | 2002-05-01 | Novartis Ag | Organic compounds |
| JPWO2003082855A1 (ja) * | 2002-03-28 | 2005-08-04 | 協和醗酵工業株式会社 | 抗炎症剤 |
| JPWO2004000841A1 (ja) | 2002-06-25 | 2005-10-20 | 協和醗酵工業株式会社 | 二環性複素環化合物 |
| CN1665789A (zh) | 2002-06-28 | 2005-09-07 | 山之内制药株式会社 | 二氨基嘧啶酰胺衍生物 |
| ATE451104T1 (de) | 2002-07-29 | 2009-12-15 | Rigel Pharmaceuticals Inc | Verfahren zur behandlung oder pruvention von autoimmunkrankheiten mit 2,4-pyrimidindiamin- verbindungen |
| MXPA05004670A (es) * | 2002-11-01 | 2005-08-18 | Abbott Lab | Agentes anti-infecciones. |
| US7902203B2 (en) | 2002-11-01 | 2011-03-08 | Abbott Laboratories, Inc. | Anti-infective agents |
| WO2004054617A1 (ja) | 2002-12-13 | 2004-07-01 | Kyowa Hakko Kogyo Co., Ltd. | 中枢疾患の予防および／または治療剤 |
| JP2006516561A (ja) | 2003-01-17 | 2006-07-06 | ワーナー−ランバート・カンパニー、リミテッド、ライアビリティ、カンパニー | 細胞増殖の阻害剤としての２−アミノピリジン置換ヘテロ環類 |
| EP1590334B1 (en) * | 2003-01-30 | 2009-08-19 | Boehringer Ingelheim Pharmaceuticals Inc. | 2,4-diaminopyrimidine derivatives useful as inhibitors of pkc-theta |
| KR100864393B1 (ko) * | 2003-04-10 | 2008-10-20 | 에프. 호프만-라 로슈 아게 | 피리미도 화합물 |
| EP1518655A1 (en) * | 2003-07-24 | 2005-03-30 | John Palmer Corp. | Apparatus for and process of gas-assisted injection molding of plastics material |
| DK2287156T3 (da) | 2003-08-15 | 2013-08-26 | Novartis Ag | 2,4-Di(phenylamino)-pyrimidiner egnede i behandling af neoplastiske sygdomme, inflammatoriske lidelser og lidelser i immunsystemet |
| EP1663241B1 (en) | 2003-09-24 | 2009-05-27 | Wyeth Holdings Corporation | 5-arylpyrimidines as anticancer agents |
| US7253204B2 (en) * | 2004-03-26 | 2007-08-07 | Methylgene Inc. | Inhibitors of histone deacetylase |
| EP1749827A4 (en) | 2004-03-30 | 2010-04-21 | Kyowa Hakko Kirin Co Ltd | ANTITUMOR AGENTS |
| JP2008505910A (ja) * | 2004-07-08 | 2008-02-28 | ベーリンガー インゲルハイム ファーマシューティカルズ インコーポレイテッド | Ｐｋｃ−シータのインヒビターとして有用なピリミジン誘導体 |
| CA2579007A1 (en) | 2004-09-10 | 2006-03-16 | Altana Pharma Ag | Ciclesonide and syk inhibitor combination and methods of use thereof |
| JP2008512429A (ja) | 2004-09-10 | 2008-04-24 | ニコメッド ゲゼルシャフト ミット ベシュレンクテル ハフツング | ロフルミラストとｓｙｋインヒビターとの組合せ物並びにその使用方法 |
| JP2006124387A (ja) | 2004-09-30 | 2006-05-18 | Taisho Pharmaceut Co Ltd | 新規なキノリン、テトラヒドロキナゾリン、及びピリミジン誘導体と、これらを使用することに関連した治療方法 |
| EP1797047B1 (en) | 2004-09-30 | 2012-01-25 | Tibotec Pharmaceuticals | Hiv inhibiting 5-substituted pyrimidines |
| WO2006091737A1 (en) | 2005-02-24 | 2006-08-31 | Kemia, Inc. | Modulators of gsk-3 activity |
| GT200600105A (es) | 2005-03-10 | 2007-02-14 | Derivados de pirimidina para el tratamiento de trastornos hiperproliferativos. | |
| KR101011957B1 (ko) * | 2005-08-25 | 2011-01-31 | 에프. 호프만-라 로슈 아게 | Ｐ３８ ｍαｐ 키나아제 저해제 및 이의 사용 방법 |
| WO2007032445A1 (ja) | 2005-09-16 | 2007-03-22 | Kyowa Hakko Kogyo Co., Ltd. | タンパク質キナーゼ阻害剤 |
| US20090221600A1 (en) * | 2005-09-28 | 2009-09-03 | Ashwani Kumar Verma | Pyrido-pyridimidine derivatives useful as antiinflammatory agents |
| CA2633992A1 (en) | 2005-12-21 | 2007-07-05 | Boehringer Ingelheim International Gmbh | Pyrimidine derivatives useful as inhibitors of pkc-theta |
| WO2008009458A1 (en) * | 2006-07-21 | 2008-01-24 | Novartis Ag | 2, 4 -di (arylaminio) -pyrimidine-5-carboxamide compounds as jak kinases inhibitors |
| US8188113B2 (en) | 2006-09-14 | 2012-05-29 | Deciphera Pharmaceuticals, Inc. | Dihydropyridopyrimidinyl, dihydronaphthyidinyl and related compounds useful as kinase inhibitors for the treatment of proliferative diseases |
| US20080139531A1 (en) | 2006-12-04 | 2008-06-12 | Alcon Manufacturing Ltd. | Use of connective tissue mast cell stabilizers to facilitate ocular surface re-epithelization and wound repair |
| WO2008129380A1 (en) | 2007-04-18 | 2008-10-30 | Pfizer Products Inc. | Sulfonyl amide derivatives for the treatment of abnormal cell growth |
| NZ581397A (en) | 2007-04-27 | 2012-02-24 | Astrazeneca Ab | Pyrimidine compounds for the inhibition of Eph receptors and for the treatment of cancer |
| CN101796046A (zh) | 2007-07-16 | 2010-08-04 | 阿斯利康(瑞典)有限公司 | 嘧啶衍生物934 |
| WO2009012421A1 (en) | 2007-07-17 | 2009-01-22 | Rigel Pharmaceuticals, Inc. | Cyclic amine substituted pyrimidinediamines as pkc inhibitors |
| CA2960692C (en) * | 2008-04-16 | 2019-09-24 | Portola Pharmaceuticals, Inc. | 2,6-diamino-pyrimidin-5-yl-carboxamides as syk or jak kinase inhibitors |
| CN102066339B (zh) * | 2008-04-16 | 2014-09-24 | 波托拉医药品公司 | 作为syk或jak蛋白激酶抑制剂的2，6-二氨基-嘧啶-5-基甲酰胺类化合物 |
| NZ589315A (en) * | 2008-04-16 | 2012-11-30 | Portola Pharm Inc | 2,6-diamino-pyrimidin-5-yl-carboxamides as Spleen tryosine kinase (syk) or Janus kinase (JAK) inhibitors |
| MX2010011591A (es) | 2008-04-22 | 2010-11-09 | Astrazeneca Ab | Pirimidin-5-carboxamidas sustituidas 281. |
| NZ588830A (en) | 2008-04-22 | 2012-11-30 | Portola Pharm Inc | Inhibitors of protein kinases |
| CA2719868A1 (en) | 2008-04-29 | 2009-11-05 | F. Hoffmann-La Roche Ag | Pyrimidinyl pyridone inhibitors of jnk. |
| PL2300013T5 (pl) | 2008-05-21 | 2025-04-28 | Takeda Pharmaceutical Company Limited | Pochodne fosforu jako inhibitor kinazy |
| UY31929A (es) | 2008-06-25 | 2010-01-05 | Irm Llc | Compuestos y composiciones como inhibidores de cinasa |
| US8338439B2 (en) | 2008-06-27 | 2012-12-25 | Celgene Avilomics Research, Inc. | 2,4-disubstituted pyrimidines useful as kinase inhibitors |
| TWI458721B (zh) | 2008-06-27 | 2014-11-01 | Celgene Avilomics Res Inc | 雜芳基化合物及其用途 |
| CN102137848A (zh) * | 2008-09-01 | 2011-07-27 | 安斯泰来制药株式会社 | 2,4-二氨基嘧啶化合物 |
| TWI453207B (zh) | 2008-09-08 | 2014-09-21 | Signal Pharm Llc | 胺基三唑并吡啶，其組合物及使用其之治療方法 |
| EP2331507A2 (en) | 2008-09-18 | 2011-06-15 | Astellas Pharma Inc. | Heterocyclic carboxamide compounds |
| TW201016676A (en) | 2008-10-03 | 2010-05-01 | Astrazeneca Ab | Heterocyclic derivatives and methods of use thereof |
| EP2344502A2 (en) * | 2008-10-22 | 2011-07-20 | F. Hoffmann-La Roche AG | Pyrimidinyl pyridone inhibitors of jnk |
| RU2522001C2 (ru) | 2008-10-31 | 2014-07-10 | Сентокор Орто Байотек Инк. | Дифференцирование человеческих эмбриональных стволовых клеток в линию панкреатических эндокринных клеток |
| AU2009325398A1 (en) * | 2008-12-12 | 2010-06-17 | Msd K.K. | Dihydropyrimidopyrimidine derivative |
| WO2010080864A1 (en) | 2009-01-12 | 2010-07-15 | Array Biopharma Inc. | Piperidine-containing compounds and use thereof |
| CA2749403A1 (en) | 2009-01-13 | 2010-09-02 | Glaxo Group Limited | Pyrimidinecarboxamide derivatives as inhibitors of syk kinase |
| US8377924B2 (en) * | 2009-01-21 | 2013-02-19 | Rigel Pharmaceuticals Inc. | Protein kinase C inhibitors and uses thereof |
| US8367689B2 (en) * | 2009-05-06 | 2013-02-05 | Portola Pharmaceuticals, Inc. | Inhibitors of JAK |
| JP2012148977A (ja) * | 2009-05-20 | 2012-08-09 | Astellas Pharma Inc | アミノシクロヘキシルアルキル基を有する２，４−ジアミノピリミジン化合物 |
| CA2764513A1 (en) * | 2009-06-08 | 2010-12-16 | Reduction Technologies Inc. | Systems, methods and devices for correcting spinal deformities |
| MX2011013325A (es) | 2009-06-10 | 2012-04-30 | Abbott Lab | 2-(lh-pirazol-4-ilamino)-pirimidina como inhibidores de cinasa. |
| JP2012197231A (ja) | 2009-08-06 | 2012-10-18 | Oncotherapy Science Ltd | Ｔｔｋ阻害作用を有するピリジンおよびピリミジン誘導体 |
| WO2011065800A2 (ko) * | 2009-11-30 | 2011-06-03 | 주식회사 오스코텍 | 피리미딘 유도체, 이의 제조방법 및 이를 함유하는 약학적 조성물 |
| CA2780759A1 (en) | 2009-12-01 | 2011-06-09 | Rigel Pharmaceuticals, Inc. | Protein kinase c inhibitors and uses thereof |
| JP2011173853A (ja) | 2010-02-26 | 2011-09-08 | Astellas Pharma Inc | 置換アミノアダマンチルアルキル基を有する２，４−ジアミノピリミジン化合物 |
| CA2801781C (en) | 2010-07-21 | 2018-02-27 | Rigel Pharmaceuticals, Inc. | Protein kinase c inhibitors and uses thereof |
| WO2012045010A1 (en) | 2010-09-30 | 2012-04-05 | Portola Pharmaceuticals, Inc. | Combinations of 4-(3-(2h-1,2,3-triazo-2-yl) phenylamino)-2-((1r,2s)-2-aminocyclohexylamino) pyrimidine-5-carboxamide and fludarabine |
| US20130244963A1 (en) | 2010-09-30 | 2013-09-19 | Portola Pharmaceuticals, Inc. | Combination therapy with 4-(3-(2h-1,2,3-triazol-2-yl)phenylamino)-2-((1r,2s)-2-aminocyclohexylamino)pyrimidine-5-carboxamide |
| SG194086A1 (en) * | 2011-04-22 | 2013-11-29 | Signal Pharm Llc | Substituted diaminocarboxamide and diaminocarbonitrile pyrimidines, compositions thereof, and methods of treatment therewith |
| MX2016007898A (es) * | 2013-12-20 | 2016-10-07 | Signal Pharm Llc | Compuestos diaminopirimidilo sustituidos, las composiciones de estos y los metodos de tratamiento con estos. |
| NZ715903A (en) * | 2014-01-30 | 2017-06-30 | Signal Pharm Llc | Solid forms of 2-(tert-butylamino)-4-((1r,3r,4r)-3-hydroxy-4-methylcyclohexylamino)-pyrimidine-5-carboxamide, compositions thereof and methods of their use |
| SG11201704827UA (en) * | 2014-12-16 | 2017-07-28 | Signal Pharm Llc | Formulations of 2-(tert-butylamino)-4-((1r,3r,4r)-3-hydroxy-4-methycyclohexylamino)-pyrimidine-5-carboxamide |
| WO2016100308A1 (en) * | 2014-12-16 | 2016-06-23 | Signal Pharmaceuticals, Llc | Methods for measurement of inhibition of c-jun n-terminal kinase in skin |
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