JP2014514322A5 - - Google Patents
Download PDFInfo
- Publication number
- 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
Links
- 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)
Families Citing this family (40)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TWI548621B (zh) | 2011-04-22 | 2016-09-11 | 標誌製藥公司 | 經取代之二胺基甲醯胺及二胺基甲腈嘧啶、其組合物、及以該等治療之方法 |
| CA2890935A1 (en) * | 2012-11-08 | 2014-05-15 | Bristol-Myers Squibb Company | Alkyl amide-substituted pyrimidine compounds useful in the modulation of il-12, il-23 and/or ifn.alpha. |
| US9447025B2 (en) | 2013-03-14 | 2016-09-20 | Kalyra Pharmaceuticals, Inc. | Bicyclic analgesic compounds |
| WO2015039613A1 (zh) * | 2013-09-18 | 2015-03-26 | 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 |
| US10189780B2 (en) | 2013-12-12 | 2019-01-29 | Zeno Royalties & Milestones, LLC | Bicyclic alkyl compounds and synthesis |
| RU2016129380A (ru) * | 2013-12-20 | 2018-01-25 | СИГНАЛ ФАРМАСЬЮТИКАЛЗ, ЭлЭлСи | Замещенные диаминопиримидильные соединения, их композиции и способы лечения с их участием |
| 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 |
| CN106232567B (zh) | 2014-03-07 | 2021-11-02 | 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 |
| US9513297B2 (en) | 2014-12-16 | 2016-12-06 | Signal Pharmaceuticals, Llc | Methods for measurement of inhibition of c-Jun N-terminal kinase in skin |
| EP3712134B1 (en) * | 2014-12-16 | 2023-11-29 | Signal Pharmaceuticals, LLC | Salts of 2-(tert-butylamino)-4-((1r,3r,4r)-3-hydroxy-4-methycyclohexylamino)-pyrimidine-5-carboxamide |
| 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 |
| EP3325432B1 (en) | 2015-07-24 | 2020-09-02 | Celgene Corporation | Methods of synthesis of (1r,2r,5r)-5-amino-2-methylcyclohexanol hydrochloride and intermediates useful therein |
| CN109311820B (zh) * | 2016-07-27 | 2022-09-27 | 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. |
| US20190231751A1 (en) * | 2016-09-12 | 2019-08-01 | 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 |
| EP3628043A4 (en) | 2017-05-15 | 2021-04-28 | Recurium IP Holdings, LLC | ANALGESIC COMPOUNDS |
| IL301709B2 (en) | 2017-08-09 | 2025-07-01 | Denali Therapeutics Inc | Compounds, compositions and methods |
| TW201920129A (zh) | 2017-09-01 | 2019-06-01 | 美商戴納立製藥公司 | 化合物、組合物及方法 |
| 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 |
| JP7212693B2 (ja) | 2017-11-01 | 2023-01-25 | ブリストル－マイヤーズ スクイブ カンパニー | ファルネソイドｘ受容体モジュレーターとしての架橋二環化合物 |
| CR20210426A (es) | 2019-02-13 | 2021-09-30 | Denali Therapeutics Inc | Compuestos, composiciones y métodos |
| EP3924341A4 (en) | 2019-02-13 | 2022-11-02 | Denali Therapeutics Inc. | Compounds, compositions and methods |
| CN111718332B (zh) * | 2019-03-19 | 2021-08-17 | 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 |
| AU2020300619A1 (en) | 2019-07-03 | 2022-01-27 | Sumitomo Pharma Oncology, Inc. | Tyrosine kinase non-receptor 1 (TNK1) inhibitors and uses thereof |
| ES2963560T3 (es) * | 2019-08-06 | 2024-03-27 | Lilly Co Eli | Compuesto piramidin-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 |
| JP7691991B2 (ja) * | 2020-03-06 | 2025-06-12 | ナショナル・ヘルス・リサーチ・インスティテューツ | ピリミジン化合物及びその薬学的使用 |
| 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 |
| CN115003671B (zh) * | 2020-09-07 | 2024-08-06 | 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 |
| US20230416225A1 (en) * | 2020-11-09 | 2023-12-28 | Merck Sharp & Dohme Llc | Diaminopyrimidine carboxamide inhibitors of hpk1 |
| TW202241857A (zh) | 2020-12-18 | 2022-11-01 | 美商戴納立製藥公司 | 化合物之固體形式 |
| US20240360125A9 (en) * | 2021-02-22 | 2024-10-31 | The Trustees Of Princeton University | 2-substituted bicyclo[1.1.1]pentanes |
| TW202339749A (zh) | 2021-12-16 | 2023-10-16 | 大陸商凌科藥業有限公司 | Ｔｙｋ２抑制劑及其組合物和方法 |
| WO2023108536A1 (en) * | 2021-12-16 | 2023-06-22 | Lynk Pharmaceuticals Co. Ltd. | Tyk2 inhibitors and compositions and methods thereof |
| 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 |
| CN120463687A (zh) * | 2022-12-30 | 2025-08-12 | 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. |
| ATE401312T1 (de) * | 1997-12-15 | 2008-08-15 | Astellas Pharma Inc | Pyrimidin-5-carboxamid-derivate |
| DE69939168D1 (de) | 1998-05-26 | 2008-09-04 | Warner Lambert Co | Bicyclische pyrimidine und bicyclische 3,4-dihydropyrimidine als inhibitoren der zellvermehrung |
| AU5438299A (en) | 1998-08-29 | 2000-03-21 | Astrazeneca Ab | Pyrimidine compounds |
| EP1184376B1 (en) * | 1999-06-09 | 2005-02-02 | Yamanouchi Pharmaceutical Co. Ltd. | Novel heterocyclic carboxamide derivatives |
| 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 |
| AU5108000A (en) | 1999-06-10 | 2001-01-02 | Yamanouchi Pharmaceutical Co., Ltd. | Novel nitrogen-contaiing heterocyclic derivatives or salts thereof |
| EP1206265B1 (en) | 1999-06-30 | 2003-11-12 | Merck & Co., Inc. | 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 |
| WO2003082855A1 (en) * | 2002-03-28 | 2003-10-09 | Kyowa Hakko Kogyo Co., Ltd. | Anti-inflammatory agent |
| CN1310916C (zh) | 2002-06-25 | 2007-04-18 | 协和发酵工业株式会社 | 双环类杂环化合物 |
| ES2373226T3 (es) | 2002-06-28 | 2012-02-01 | Astellas Pharma Inc. | Derivado de diaminopirimidincarboxamida. |
| IL166241A0 (en) | 2002-07-29 | 2006-01-15 | Rigel Pharmaceuticals Inc | Method of treating or preventing autoimmune diseases with 2,4-pyrimidinedinediamine compounds |
| US7902203B2 (en) | 2002-11-01 | 2011-03-08 | Abbott Laboratories, Inc. | Anti-infective agents |
| BR0315897A (pt) * | 2002-11-01 | 2008-05-13 | Abbott Lab | agentes antiinfecciosos |
| JPWO2004054617A1 (ja) | 2002-12-13 | 2006-04-20 | 協和醗酵工業株式会社 | 中枢疾患の予防および／または治療剤 |
| EP1590341B1 (en) | 2003-01-17 | 2009-06-17 | Warner-Lambert Company LLC | 2-aminopyridine substituted heterocycles as inhibitors of cellular proliferation |
| EP1590334B1 (en) * | 2003-01-30 | 2009-08-19 | Boehringer Ingelheim Pharmaceuticals Inc. | 2,4-diaminopyrimidine derivatives useful as inhibitors of pkc-theta |
| CA2521124A1 (en) * | 2003-04-10 | 2004-10-21 | F. Hoffmann-La Roche Ag | Pyrimido compounds |
| EP1518655A1 (en) * | 2003-07-24 | 2005-03-30 | John Palmer Corp. | Apparatus for and process of gas-assisted injection molding of plastics material |
| ATE542801T1 (de) | 2003-08-15 | 2012-02-15 | Novartis Ag | Zur behandlung von neoplastischen krankheiten, entzündlichen erkrankungen und erkrankungen des immunsystems geeignete 2,4-pyrimidindiamine |
| JP2007506746A (ja) | 2003-09-24 | 2007-03-22 | ワイス・ホールディングズ・コーポレイション | 抗癌剤としての５−アリールピリミジン類 |
| US7253204B2 (en) * | 2004-03-26 | 2007-08-07 | Methylgene Inc. | Inhibitors of histone deacetylase |
| WO2005095382A1 (ja) | 2004-03-30 | 2005-10-13 | Kyowa Hakko Kogyo Co., Ltd. | 抗腫瘍剤 |
| US7601714B2 (en) * | 2004-07-08 | 2009-10-13 | Boehringer Ingelheim Pharmaceuticals, Inc. | Pyrimidine derivatives useful as inhibitors of PKC-theta |
| 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 |
| CA2579007A1 (en) | 2004-09-10 | 2006-03-16 | Altana Pharma Ag | Ciclesonide and syk inhibitor combination and methods of use thereof |
| 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 |
| ATE542802T1 (de) | 2004-09-30 | 2012-02-15 | Tibotec Pharm Ltd | Hiv-inhibierende 5-substituierte pyrimidine |
| WO2006091737A1 (en) | 2005-02-24 | 2006-08-31 | Kemia, Inc. | Modulators of gsk-3 activity |
| EP1858882A1 (en) | 2005-03-10 | 2007-11-28 | Bayer Pharmaceuticals Corporation | Pyrimidine derivatives for treatment of hyperproliferative disorders |
| EP1919913A2 (en) * | 2005-08-25 | 2008-05-14 | F.Hoffmann-La Roche Ag | P38 map kinase inhibitors and methods for using the same |
| 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 |
| EP1931667A1 (en) * | 2005-09-28 | 2008-06-18 | Ranbaxy Laboratories Limited | Pyrido-pyridimidine derivatives useful as antiinflammatory agents |
| JP2009521488A (ja) * | 2005-12-21 | 2009-06-04 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | Ｐｋｃ−シータのインヒビターとして有益なピリミジン誘導体 |
| 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 |
| DK2146779T3 (en) | 2007-04-18 | 2016-11-28 | Pfizer Prod Inc | Sulfonylamid derivatives to treat abnormal cell growth. |
| JP2010525047A (ja) | 2007-04-27 | 2010-07-22 | アストラゼネカ アクチボラグ | 増殖状態の処置のためのＥｐｈＢ４キナーゼ阻害剤としてのＮ’−（フェニル）−Ｎ−（モルホリン−４−イル−ピリジン−２−イル）−ピリミジン−２，４−ジアミン誘導体 |
| CN101796046A (zh) | 2007-07-16 | 2010-08-04 | 阿斯利康(瑞典)有限公司 | 嘧啶衍生物934 |
| CN101903357A (zh) | 2007-07-17 | 2010-12-01 | 里格尔药品股份有限公司 | 作为pkc抑制剂的环状胺取代的嘧啶二胺 |
| KR20100132550A (ko) * | 2008-04-16 | 2010-12-17 | 포톨라 파마슈티컬스, 인코포레이티드 | ｓｙｋ 또는 ＪＡＫ 키나제 억제제로서의 ２,６－디아미노-피리미딘－５－일－카르복스아미드 |
| CA2723205C (en) * | 2008-04-16 | 2017-03-14 | Portola Pharmaceuticals, Inc. | 2,6-diamino-pyrimidin-5-yl-carboxamides as syk or jak kinase inhibitors |
| US8063058B2 (en) * | 2008-04-16 | 2011-11-22 | Portola Pharmaceuticals, Inc. | Inhibitors of syk and JAK protein kinases |
| MX2010011591A (es) | 2008-04-22 | 2010-11-09 | Astrazeneca Ab | Pirimidin-5-carboxamidas sustituidas 281. |
| BRPI0910668A2 (pt) | 2008-04-22 | 2019-09-24 | Portola Pharmaceutiacals Inc | inibidores de proteína quinases |
| WO2009132980A1 (en) * | 2008-04-29 | 2009-11-05 | F. Hoffmann-La Roche Ag | Pyrimidinyl pyridone inhibitors of jnk. |
| JP2011523646A (ja) | 2008-05-21 | 2011-08-18 | アリアド・ファーマシューティカルズ・インコーポレイテッド | キナーゼ阻害剤としてのリン誘導体 |
| PE20100087A1 (es) | 2008-06-25 | 2010-02-08 | 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 |
| AU2009262068C1 (en) | 2008-06-27 | 2015-07-02 | Celgene Car Llc | Heteroaryl compounds and uses thereof |
| EP2325175A4 (en) * | 2008-09-01 | 2012-03-21 | Astellas Pharma Inc | 2,4-DIAMINOPYRIMIDINVERBINDUNG |
| 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 |
| BRPI0918045A2 (pt) | 2008-09-18 | 2015-12-01 | Astellas Pharma Inc | compostos de carboxamida heterocíclicos |
| TW201016676A (en) | 2008-10-03 | 2010-05-01 | Astrazeneca Ab | Heterocyclic derivatives and methods of use thereof |
| CN102177161A (zh) * | 2008-10-22 | 2011-09-07 | 霍夫曼-拉罗奇有限公司 | Jnk的嘧啶基吡啶酮抑制剂 |
| EP2346988B1 (en) | 2008-10-31 | 2017-05-31 | Janssen Biotech, Inc. | Differentiation of human embryonic stem cells to the pancreatic endocrine lineage |
| CA2745970A1 (en) * | 2008-12-12 | 2010-06-17 | Msd K.K. | Dihydropyrimidopyrimidine derivative |
| JP5683489B2 (ja) | 2009-01-12 | 2015-03-11 | アレイ バイオファーマ、インコーポレイテッド | ピペリジン含有化合物およびその用途 |
| CA2749403A1 (en) | 2009-01-13 | 2010-09-02 | Glaxo Group Limited | Pyrimidinecarboxamide derivatives as inhibitors of syk kinase |
| WO2010090875A1 (en) * | 2009-01-21 | 2010-08-12 | Rigel Pharmaceuticals, Inc. | Derivatives of n2-(3-pyridil or phenyl)-n4-(4-piperidyl)-2,4-pyrimidinediamine useful in the treatment of inflammatory, autoimmune or proliferative diseases |
| WO2010129802A1 (en) * | 2009-05-06 | 2010-11-11 | 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 |
| WO2010144458A1 (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 |
| US20110130415A1 (en) | 2009-12-01 | 2011-06-02 | Rajinder Singh | 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 |
| WO2012045020A1 (en) | 2010-09-30 | 2012-04-05 | Portola Pharmaceuticals, Inc. | Combinations of 4-(cyclopropylamino)-2-(4-(4-(ethylsulfonyl)piperazin-1-yl)phenylamino)pyrimidine-5-carboxamide and fludarabine |
| WO2012044936A1 (en) | 2010-09-30 | 2012-04-05 | Portola Pharmaceuticals, Inc. | Combination therapy with 4-(3-(2h-1,2,3-triazol-2-yl)phenylamino)-2-((1r,2s)-2-aminocyclohexylamino)pyrimidine-5-carboxamide |
| TWI548621B (zh) * | 2011-04-22 | 2016-09-11 | 標誌製藥公司 | 經取代之二胺基甲醯胺及二胺基甲腈嘧啶、其組合物、及以該等治療之方法 |
| RU2016129380A (ru) * | 2013-12-20 | 2018-01-25 | СИГНАЛ ФАРМАСЬЮТИКАЛЗ, ЭлЭлСи | Замещенные диаминопиримидильные соединения, их композиции и способы лечения с их участием |
| 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 |
| US9513297B2 (en) * | 2014-12-16 | 2016-12-06 | Signal Pharmaceuticals, Llc | Methods for measurement of inhibition of c-Jun N-terminal kinase in skin |
| EP3712134B1 (en) * | 2014-12-16 | 2023-11-29 | Signal Pharmaceuticals, LLC | Salts of 2-(tert-butylamino)-4-((1r,3r,4r)-3-hydroxy-4-methycyclohexylamino)-pyrimidine-5-carboxamide |
-
2012
- 2012-04-20 TW TW101114317A patent/TWI548621B/zh active
- 2012-04-20 RS RS20240075A patent/RS65202B1/sr unknown
- 2012-04-20 CN CN201510389071.XA patent/CN105001165B/zh active Active
- 2012-04-20 EP EP12718524.7A patent/EP2699553B1/en active Active
- 2012-04-20 SG SG10201702654VA patent/SG10201702654VA/en unknown
- 2012-04-20 CN CN201610882236.1A patent/CN106946795B/zh active Active
- 2012-04-20 PT PT127185247T patent/PT2699553T/pt unknown
- 2012-04-20 CA CA2829264A patent/CA2829264C/en active Active
- 2012-04-20 US US13/451,574 patent/US9139534B2/en active Active
- 2012-04-20 AU AU2012245387A patent/AU2012245387C1/en active Active
- 2012-04-20 PH PH1/2013/501921A patent/PH12013501921A1/en unknown
- 2012-04-20 RU RU2017121958A patent/RU2697712C2/ru active
- 2012-04-20 SI SI201232053T patent/SI2699553T1/sl unknown
- 2012-04-20 RU RU2013152021A patent/RU2625309C2/ru active
- 2012-04-20 BR BR112013022813A patent/BR112013022813B1/pt active IP Right Grant
- 2012-04-20 WO PCT/US2012/034349 patent/WO2012145569A1/en not_active Ceased
- 2012-04-20 LT LTEPPCT/US2012/034349T patent/LT2699553T/lt unknown
- 2012-04-20 DK DK12718524.7T patent/DK2699553T3/da active
- 2012-04-20 FI FIEP12718524.7T patent/FI2699553T3/fi active
- 2012-04-20 PL PL12718524.7T patent/PL2699553T3/pl unknown
- 2012-04-20 HU HUE12718524A patent/HUE064883T2/hu unknown
- 2012-04-20 CN CN201280019861.3A patent/CN103492370B/zh active Active
- 2012-04-20 EP EP23205984.0A patent/EP4328223A3/en not_active Withdrawn
- 2012-04-20 MX MX2013010946A patent/MX351754B/es active IP Right Grant
- 2012-04-20 TW TW105112041A patent/TWI599563B/zh active
- 2012-04-20 ES ES12718524T patent/ES2968700T3/es active Active
- 2012-04-20 TW TW106120278A patent/TWI681952B/zh active
- 2012-04-20 SG SG2013074273A patent/SG194086A1/en unknown
- 2012-04-20 KR KR1020197007112A patent/KR102055532B1/ko active Active
- 2012-04-20 JP JP2014506559A patent/JP6027095B2/ja active Active
- 2012-04-20 SM SM20240031T patent/SMT202400031T1/it unknown
- 2012-04-20 KR KR1020137027371A patent/KR101962488B1/ko active Active
- 2012-04-20 CN CN202010398710.XA patent/CN111471021B/zh active Active
- 2012-04-20 PE PE2013002388A patent/PE20140502A1/es active IP Right Grant
- 2012-04-20 UA UAA201313555A patent/UA120740C2/uk unknown
- 2012-04-20 HR HRP20240097TT patent/HRP20240097T1/hr unknown
- 2012-04-20 CN CN202010398589.0A patent/CN111499580A/zh active Pending
- 2012-04-23 AR ARP120101402 patent/AR087151A1/es active IP Right Grant
-
2013
- 2013-08-28 ZA ZA2013/06471A patent/ZA201306471B/en unknown
- 2013-09-26 CR CR20130490A patent/CR20130490A/es unknown
- 2013-10-03 IL IL228721A patent/IL228721A/en active IP Right Grant
- 2013-10-08 CO CO13238970A patent/CO6821941A2/es active IP Right Grant
- 2013-10-18 CL CL2013003025A patent/CL2013003025A1/es unknown
- 2013-10-21 EC ECSP13012985 patent/ECSP13012985A/es unknown
- 2013-10-21 NI NI201300113A patent/NI201300113A/es unknown
-
2015
- 2015-07-29 PH PH12015501677A patent/PH12015501677B1/en unknown
- 2015-07-31 US US14/814,633 patent/US9701643B2/en active Active
-
2016
- 2016-05-23 IL IL245792A patent/IL245792B/en active IP Right Grant
- 2016-10-13 JP JP2016202099A patent/JP6502302B2/ja active Active
-
2017
- 2017-06-07 US US15/616,039 patent/US10040770B2/en active Active
- 2017-06-15 IL IL252952A patent/IL252952B/en active IP Right Grant
-
2018
- 2018-06-28 US US16/021,415 patent/US10266500B2/en active Active
-
2019
- 2019-03-04 US US16/291,193 patent/US10919865B2/en active Active
- 2019-03-20 JP JP2019052826A patent/JP6898961B2/ja active Active
-
2020
- 2020-12-29 US US17/136,276 patent/US11325890B2/en active Active
-
2021
- 2021-06-11 JP JP2021098226A patent/JP7374955B2/ja active Active
-
2022
- 2022-03-29 US US17/707,471 patent/US12129237B2/en active Active
-
2023
- 2023-10-25 JP JP2023183330A patent/JP2023179797A/ja active Pending
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| RU2013152021A (ru) | Замещенные диаминокарбоксамидные и диаминокарбонитрильные производные пиримидинов, их композиции и способы лечения с их помощью | |
| JP2022512482A5 (enExample) | ||
| JP2014520898A5 (enExample) | ||
| JP2013523802A5 (enExample) | ||
| US20170157133A1 (en) | Novel pyridazones and triazinones for treatment and prophylaxis of hepatitis b virus infection | |
| JP2013544860A5 (enExample) | ||
| RU2018121946A (ru) | Модуляторы ror-гамма | |
| BR112020008851A2 (pt) | composto da fórmula i, processo de preparação de compostos da fórmula i, composição farmacêutica, método para o tratamento e/ou prevenção de várias doenças, uso, método para o tratamento de câncer, método de tratamento de câncer e método para o tratamento e/ou prevenção de câncer e doenças infecciosas | |
| JP2018510139A5 (enExample) | ||
| JP2020519654A5 (enExample) | ||
| RU2009127095A (ru) | Новые оксадиазольные соединения | |
| JP2018531981A5 (enExample) | ||
| EA032609B1 (ru) | Соединения аминопиримидинила в качестве ингибиторов jak | |
| JP2012502974A5 (enExample) | ||
| RU2016123382A (ru) | Твердые формы { [5-(3-хлорфенил)-3-гидроксипиридин-2-карбонил]амино} уксусной кислоты, их композиции и применения | |
| US20140275085A1 (en) | 2-aminopyrimidin-6-ones and analogs exhibiting anti-cancer and anti-proliferative activities | |
| JP2008509146A5 (enExample) | ||
| JP2013544233A5 (enExample) | ||
| WO2012039460A1 (ja) | 置換アミド化合物 | |
| JP2019518764A5 (enExample) | ||
| JP2017531013A5 (enExample) | ||
| JP2017508794A5 (enExample) | ||
| JP2020518571A5 (enExample) | ||
| JP2023532298A (ja) | 化合物、組成物及び方法 | |
| JP2017508795A5 (enExample) |