Benzyl 4-Methanesulfonylpiperazine-1-Carboxylate置于palladium 10% On Activated Carbon 氢气体系中,用 乙醇 作为反应溶剂,化学反应 2.0H,反应生成 1-甲烷磺酰哌嗪 参考文献:Phthalazine,Aza-And Diaza-Phthalazine Compounds And Methods Of Use 标题:Phthalazine,Aza-And Diaza-Phthalazine Compounds And Methods Of Use 摘要:本发明包括一类新的化合物,用于预防和治疗蛋白激酶介导的疾病,包括炎症及相关状况.这些化合物的通用公式为i 其中a 1,A 2,B,R 1,R 2,R 3 和r 4 在此定义.该发明还包括包括一个或多个i公式化合物的药物组合物,以及使用这些化合物和组合物治疗激酶介导的疾病,包括类风湿性关节炎,银屑病和其他炎症性疾病,以及用于制备i公式化合物的中间体和工艺.
专利号:WO-2024137329-A1 优先权日:2022-12-20 标 题:Methods for the synthesis of complement factor d inhibitors and intermediates thereof 发明人:HASHIMOTO AKIHIRO; TIPPARAJU SURESH KUMAR 权利人:ALEXION PHARMA INC 摘要:The present disclosure provides methods for the synthesis of complement factor D inhibitors and intermediates thereof.
专利号:US-2024199637-A1 优先权日:2021-04-21 标题 :Improved process for the preparation of 7-(morpholinyl)-2-(n-piperazinyl)methylthieno[2, 3-c]pyridine derivatives 发明人:KOMPELLA AMALA; VAGICHERLA KAMESWARA RAO; LANKI REDDY TIRUMALA REDDY; PESARU NARMADA; MUDDASANI PULLA REDDY; NANNAPANENI VENKAIAH CHOWDARY 权利人:NATCO PHARMA LTD 摘要:The present invention describes an improved second generation process for the synthesis of NRC-1111 (1,5-[2-[[4-(methylsulfonyl)-1-piperazinyl]methyl]-7-(4-morpholinyl)thieno[2,3-c] pyridine-5-yl]-2-pyrimidinamine) dimethane sulfonate and NRC-1109 (II, 5-[3-methyl-2-[(4-methylsulfonylpiperazin-1-yl)methyl]-7-morpholino-thieno[2,3-c]pyridin-5-yl]pyrimidin-2-amine) dimethane sulfonate. This process is cost effective, high yielding and industrially feasible process for the synthesis of compounds of formulae I and II with high purity. Formula (I) Formula (I): Râ•?H for NRC-1111 and Formula (II): Râ•?CH3 for NRC-1109 NRC-1111 and NRC-1109 are potential anti-cancer agents.
专利号:US-10995078-B2 优先权日:2013-03-13 标 题:Compounds and compositions for inhibition of FASN 发明人:BAIR KENNETH W; LANCIA JR DAVID R; LI HONGBIN; LOCH JAMES; LU WEI; MARTIN MATTHEW W; MILLAN DAVID S; SCHILLER SHAWN E R; TEBBE MARK J 权利人:FORMA THERAPEUTICS INC 摘要:The present invention relates to compounds and composition for inhibition of FASN, their synthesis, applications, and antidotes. An illustrative compound of the invention is shown below:
专利号:WO-2023114200-A2 优先权日:2021-12-14 标题 :Methods for the synthesis of complement factor d inhibitors and intermediates thereof
专利号:WO-0010565-A1 优先权日:1998-08-18 标 题 :Growth hormone secretagogues 发明人:DODGE JEFFREY ALAN; HAUSER KENNETH LEE; HEIMAN MARK LOUIS; JONES SCOTT ALAN; ALT CHARLES ARTHUR; BRYANT HENRY UHLMAN; COHEN JEFFREY DANIEL; COPP JAMES DENSMORE; FAHEY KENNAN JOSEPH; GRITTON WILLIAM HARLAN; JUNGHEIM LOUIS NICKOLAUS; KENNEDY JOSEPH HENRY; LUGAR CHARLES WILLIS III; MUEHL BRIAN STEPHEN; PALKOWITZ ALAN DAVID; RATZ ANDREW MICHAEL; RHODES GARY ANTHONY; ROBEY ROBERT LEWIS; SEYLER DAVID EDWARD; SHEPHERD TIMOTHY ALAN; THRASHER KENNETH JEFF; TRANKLE WILLIAM GEORGE 权利人:LILLY CO ELI; DODGE JEFFREY ALAN; HAUSER KENNETH LEE; HEIMAN MARK LOUIS; JONES SCOTT ALAN; ALT CHARLES ARTHUR; BRYANT HENRY UHLMAN; COHEN JEFFREY DANIEL; COPP JAMES DENSMORE; FAHEY KENNAN JOSEPH; GRITTON WILLIAM HARLAN; JUNGHEIM LOUIS NICKOLAUS; KENNEDY JOSEPH HENRY; LUGAR CHARLES WILLIS III; MUEHL BRIAN STEPHEN; PALKOWITZ ALAN DAVID; RATZ ANDREW MICHAEL; RHODES GARY ANTHONY; ROBEY ROBERT LEWIS; SEYLER DAVID EDWARD; SHEPHERD TIMOTHY ALAN; THRASHER KENNETH JEFF; TRANKLE WILLIAM GEORGE 摘要:This invention relates to novel compounds which are useful in the modulation of endogenous growth hormone levels in a mammal. The invention further relates to novel intermediates for use in the synthesis of said compounds, as well as novel processes employed in these syntheses. Also included are methods of treating a mammal which include the administration of said compounds.
专利号:US-9676721-B2 优先权日:2010-09-03 标题 :Compounds and compositions for the inhibition of NAMPT 发明人:BAIR KENNETH W; BUCKMELTER ALEXANDRE J; HAN BINGSONG; LIN JIAN; REYNOLDS DOMINIC J; SMITH CHASE C; WANG ZHONGGUO; ZHENG XIAOZHANG 权利人:BAIR KENNETH W; BUCKMELTER ALEXANDRE J; HAN BINGSONG; LIN JIAN; REYNOLDS DOMINIC J; SMITH CHASE C; WANG ZHONGGUO; ZHENG XIAOZHANG; FORMA TM LLC 摘要:The present invention relates to compounds and compositions for the inhibition of NAMPT, their synthesis, applications and antidotes. An illustrative compound of the invention is shown below.
参考文献:10.1007/s00044-023-03180-1 摘要:Tandel P, Upadhyay R, Patel AB. A concise review on anti-breast cancer effectiveness of s-triazines through EGFR kinase inhibition. Med Chem Res. 2023 Dec 21;33(1):47–65. doi: 10.1007/s00044-023-03180-1.