公开(公告)号：US09988348B1

公开(公告)日：2018-06-05

申请号：US15615765

申请日：2017-06-06

Applicant: KING SAUD UNIVERSITY

Inventor： Yahia Nasser Mabkhot Gabr ,  Jamal Mohammed Ali Khaled ,  Mujeeb Abdullah Saeed Sultan ,  Salim S. Al-Showiman ,  Naiyf Sultan Helial Alaloi Alharbi ,  Hazem Ahmed Ghabbour

IPC: C07C329/00 ,  A61K31/265

CPC classification number: C07C329/00 ,  A61K31/265 ,  A61K2121/00

Abstract: A method for preparing a trithiocarbonate derivative compound includes reacting ethyl cyanoacetate, carbon disulfide (CS2) and ethyl chloroacetate in the presence of potassium carbonate (K2CO3) in an organic solvent to produce 2,2′-(thiocarbonylbis(sulfanediyl))diacetate compound, represented by the structural formula:

公开(公告)号：US09125866B1

公开(公告)日：2015-09-08

申请号：US14608042

申请日：2015-01-28

Applicant: KING SAUD UNIVERSITY

Inventor： Usama Sayed Karama ,  Mujeeb Abdullah Saeed Sultan ,  Kamal Eldin Hussein El Tahir ,  Abdulrahman Ibrahim Almansour

IPC: A61K31/137 ,  C07C211/42 ,  C07C209/26 ,  A61K31/135 ,  C07C47/457

CPC classification number: A61K31/135 ,  C07C47/457 ,  C07C211/42 ,  C07C2603/88

Abstract: The antidepressant compounds are compounds of the formula: wherein R1 and R2 are either both hydrogen or both halogen (particularly chlorine), and if R1 and R2 are both hydrogen, R3 and R4 are both halogen (particularly chlorine), otherwise both R3 and R4 are hydrogen; or a pharmaceutically acceptable salt thereof. The compounds may be prepared by: (a) reducing 1,8-dihaloanthrquinone with zinc powder in aqueous ammonia, followed by acidic treatment to provide 1,8-dihaloanthracene; (b) Diels-Alder [4+2] cycloaddition reaction of the 1,8-dihaloanthracene and acrolein at room temperature in the presence of boron trifluoride etherate to obtain a mixture of the intermediate compounds 1,8-dihalo-9,10-dihydo-9,10-ethanoanthracene-11-carbaldehyde and 4,5-dihalo-9,10-dihydo-9,10-ethanoanthracene-11-carbaldehyde; (c) separating the mixture of carbaldehydes by column chromatography; and (d) direct reductive amination of the respective carbaldehydes to obtain the corresponding antidepressant compounds of the above formula.

Abstract translation: 抗抑郁剂化合物是下式的化合物：其中R 1和R 2既可以是氢也可以是卤素（特别是氯），或者如果R 1和R 2都是氢，则R3和R4都是卤素（特别是氯），否则R3和R4 是氢; 或其药学上可接受的盐。 化合物可以通过以下步骤制备：（a）用氨水中的锌粉还原1,8-二卤代蒽醌，接着进行酸性处理，得到1,8-二卤代蒽; （b）1,8-二卤代蒽和丙烯醛在三氟化硼乙醚合物的存在下在室温下的狄尔斯 - 阿尔德[4 + 2]环加成反应，得到中间体化合物1,8-二卤代-9,10- 二氢-9,10-亚磺基-11-甲醛和4,5-二卤代-9,10-二氢-9,10-乙基蒽-10-甲醛; （c）通过柱色谱分离碳醛混合物; 和（d）直接还原胺化各种碳醛，得到上述相应的抗抑郁药。

公开(公告)号：US09498460B1

公开(公告)日：2016-11-22

申请号：US15092597

申请日：2016-04-06

Applicant: KING SAUD UNIVERSITY

Inventor： Usama Sayed Eisa Karama ,  Mujeeb Abdullah Saeed Sultan ,  Abdulrahman Ibrahim Almansour ,  Kamal Eldin Hussein El Tahir ,  Yasser Abbas Elnakady ,  Talal Abdul Aziz Mohaya

IPC: A61K31/235 ,  A61K31/11 ,  A61K31/135 ,  A61K31/045 ,  C07C211/31 ,  C07C47/24

CPC classification number: A61K31/235 ,  A61K31/045 ,  A61K31/11 ,  A61K31/135 ,  A61K31/137 ,  C07C47/24 ,  C07C211/31 ,  C07C2603/88

Abstract: The anti-cancer compounds are represented by Formula I: wherein R1 and R2 are either both hydrogen or both halogen, and if R1 and R2 are both hydrogen, R3 and R4 are both halogen, otherwise both R3 and R4 are hydrogen; wherein R5 is CHO or NHCH3; and wherein n is 0 to 3; provided that n is 0 only when R5 is CHO, or a pharmaceutically acceptable salt or isomer thereof.