CAS: 157810-81-6; (S)-1-((2S,4R)-4-Benzyl-2-Hydroxy-5-(((1S,2R)-2-Hydroxy-2,3-Dihydro-1H-Inden-1-yl)Amino)-5-Oxopentyl)-N-(Tert-Butyl)-4-(Pyridin-3-Ylmethyl)Piperazine-2-Carboxamide Sulfate

(S)-1-[(2S,4R)-4-Benzyl-5-((3As,8Ar)-2,2-Dimethyl-8,8A-Dihydro-3Ah-Indeno[1,2-D]Oxazol-3-yl)-2-Hydroxy-5-Oxo-Pentyl]-4-Pyridin-3-Ylmethyl-Piperazine-2-Carboxylic Acid Tert-Butylamide 以90的收率获得硫酸茚地那韦
参考文献: Process To Make Hiv Protease Inhibitor From 2(S)-4-Picolyl-2-Piperazine-T-Butylcarboxamide[fr] Procede De Fabrication D'Un Inhibiteur De La Protease Du Virus Vih A Partir Du 2(S)-4-Picolyl-2-Piperazine-T-Butylcarboxamide
标题: Process To Make Hiv Protease Inhibitor From 2(S)-4-Picolyl-2-Piperazine-T-Butylcarboxamide[fr] Procede De Fabrication D'Un Inhibiteur De La Protease Du Virus Vih A Partir Du 2(S)-4-Picolyl-2-Piperazine-T-Butylcarboxamide
摘要:一个制作临床有效的hiv蛋白酶抑制剂的过程,通过使用2(S)-4-吡啶基-2-哌嗪基-T-丁基羧酰胺作为中间体,通过另一种汇合合成方法来消除其合成中的一步;如上所示.

专利信息

专利号:US-8987493-B2
优先权日:2010-05-20
标题 :Process for synthesis of silane dipeptide analogs
发明人：SIEBURTH SCOTT MCNEILL; BO YINGJIAN
权利人:SIEBURTH SCOTT MCNEILL; BO YINGJIAN; Temple University—Of the Commonwealth System of Higher Education
摘要:The invention provides a method of preparing silane dipeptide analogs, comprising the steps of treating a solution of a substituted 1,2-oxasilolane with lithium metal to form a solution of the dilithium salt of a substituted 3-hydroxypropylsilanol, and reacting the solution of the dilithium salt of the substituted 3-hydroxypropylsilanol with a substituted enamine.

专利号:US-2025206743-A1
优先权日:2022-03-25
标 题:Tyk2 inhibitor synthesis and intermediates thereof
发明人：MASSE CRAIG E; PHADKE AVINASH S; LAWSON JON P; LEVY STUART; YANG XIAOWEI; WU GUISHENG; FAN SHUFENG
权利人:TAKEDA PHARMACEUTICALS CO
摘要:Described herein are methods of synthesis of a tyrosine-protein kinase 2 (TYK2) inhibitor and to intermediate compounds of the synthesis and methods of making the intermediates. Also provided are pharmaceutically acceptable compositions including compounds prepared by the synthetic method and methods of treating disorders using the same.

专利号:US-8557979-B2
优先权日:2004-06-10
标题 :Carbapenem antibacterials with gram-negative activity and processes for their preparation
发明人：CHOI WOO-BAEG; KOWALIK EWA
权利人:CHOI WOO-BAEG; KOWALIK EWA; FOB SYNTHESIS INC
摘要:The present invention provides β-methyl carbapenem compounds and pharmaceutical compositions useful in the treatment of bacterial infections and methods for treating such infections using such compounds and/or compositions. The invention includes administering an effective amount of a carbapenem compound or salt and/or prodrug thereof to a host in need of such a treatment. The present invention is also in the field of synthetic organic chemistry and is specifically provides an improved method of synthesis of β-methyl carbapenems which are useful as antibacterial agents.

专利号:US-6869973-B2
优先权日:2000-06-22
标题:Nitrosated and nitrosylated taxanes, compositions and methods of use
发明人：GARVEY DAVID S; LETTS L GORDON; LIN CHIA-EN; RICHARDSON STEWART K; WANG TIANSHENG
权利人:NITROMED INC
摘要:The present invention describes novel nitrosated and/or nitrosylated taxanes, and novel compositions comprising at least one nitrosated and/or nitrosylated taxane, and, optionally, at least one compound that donates, transfers or releases nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor, stimulates endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and/or at least one therapeutic agent. The present invention also provides novel compositions comprising at least one taxane and at least one compound that donates, transfers or releases nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor, stimulates endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and/or at least one therapeutic agent. The compounds and compositions of the present invention can also be bound to a matrix. The present invention also provides methods for treating or preventing cardiovascular diseases and disorders, autoimmune diseases, pathological conditions resulting from abnormal cell proliferation, polycystic kidney disease, inflammatory disease, preserving organs and/or tissues or to inhibit wound contraction, particularly the prophylactic and/or therapeutic treatment of restenosis, by administering nitrosated and/or nitrosylated taxane or parent taxanes in combination with nitric oxide donors that are capable of releasing nitric oxide or indirectly delivering or transferring nitric oxide to targeted sites under physiological conditions.

专利号:US-2003203915-A1
优先权日:2002-04-05
标题 :Nitric oxide donors, compositions and methods of use related applications
发明人：FANG XINQIN; GARVEY DAVID S; GASTON RICKY D; LIN CHIA-EN; RANATUNGA RAMANI R; RICHARDSON STEWART K; WANG TIANSHENG; WANG WEIHENG; WEY SHIOW-JYI
权利人:FANG XINQIN; GARVEY DAVID S; GASTON RICKY D; LIN CHIA-EN; RANATUNGA RAMANI R; RICHARDSON STEWART K; WANG TIANSHENG; WANG WEIHENG; WEY SHIOW-JYI
摘要:The invention describes novel nitric oxide donors and novel compositions comprising at least one nitric oxide donor. The invention also provides novel compositions comprising at least one nitric oxide donor, and, optionally, at least one therapeutic agent. The compounds and compositions of the invention can also be bound to a matrix. The invention also provides methods for treating cardiovascular diseases, for the inhibition of platelet aggregation and platelet adhesion caused by the exposure of blood to a medical device, for treating pathological conditions resulting from abnormal cell proliferation; transplantation rejections, autoimmune, inflammatory, proliferative, hyperproliferative, vascular diseases; for reducing scar tissue or for inhibiting wound contraction, particularly the prophylactic and/or therapeutic treatment of restenosis by administering the nitric oxide donor optionally in combination with at least one therapeutic agent. The invention also provides methods for treating inflammation, pain, fever, gastrointestinal disorders, respiratory disorders and sexual dysfunctions. The nitric oxide donors donate, transfer or release nitric oxide, and/or elevate endogenous levels of endothelium-derived relaxing factor, and/or stimulate endogenous synthesis of nitric oxide and/or are substrates for nitric oxide synthase and are capable of releasing nitric oxide or indirectly delivering or transferring nitric oxide to targeted sites under physiological conditions. The therapeutic agent can optionally be substituted with at least one NO and/or NO 2 group (i.e., nitrosylated and/or nitrosated). The invention also provides novel compositions and kits comprising at least one nitric oxide donor and/or at least one therapeutic agent.

专利号:US-10933051-B2
优先权日:2017-06-09
标 题 :Carbapenem compounds and compositions for the treatment of bacterial infections
发明人：CHOI WOO-BAEG; TOMIOKA TAKASHI; JOO HYUNG-YEUL; TRUONG PHONG; MIN BRIAN
权利人:FOB SYNTHESIS INC
摘要:The present invention provides carbapenem compounds and pharmaceutical compositions useful in the treatment of bacterial infections, including drug resistant or multiple-drug resistant bacterial infections, and methods for treating such infections using such compounds and/or compositions. The invention includes administering an effective amount of a carbapenem compound or salt and/or prodrug thereof to a host in need of such a treatment.