项目整合精选

聚焦新型临床类新产品的整合与转化. 在创新药研发领域，传统的“单一产品、单打独斗”模式正在被一种更系统化的“项目整合”思维所取代。项目整合的核心，在于将散落在研发早期、中期的创新资产，通过资金、临床资源、产业生态等多维度要素的有机组合，实现从“科学发现”到“临床价值”，再到“商业成功”的跨越。研发与商业的战略整合：从“资产思维”到“组合思维”它要求我们超越单个分子的视野，拥抱一个由技术创新、临床需求、资本支持和商业洞察共同构成的复杂网络。在这个网络中，成功的标准不再是单一的“获批上市”，而是能否通过高效的整合，将科学上的突破，转化为临床上真正可及、商业上可持续、能够惠及患者的解决方案。近年来，药物发现已从传统的小分子化药拓展至更多元的分子类型，这些新型API在项目整合中呈现出独特的开发范式，项目整合的核心挑战在于递送系统的设计与肝外靶向能力的突破。
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项目整合精选

Indinavir sulfate, MK-639, L-735524, Crixivan

硫酸茚地那韦茚地那韦茚地那韦Chemical Name: 2(R)-Benzyl-5-[2(S)-(N-tert-butylcarbamoyl)-4-(3-pyridylmethyl)piperazin-1-yl]-4(S)-hydroxy-N-[2(R)-hydroxyindan-1(S)-yl]pentanamide sulfate (1:1); N-tert-Butyl-1-[2(S)-...
参考文献标题:HIV protease inhibitors useful for the treatment of AIDS
文献作者:Vacca,J.P.; Holloway,M.K.; Dorsey,B.D.; Hungate,R.W.; Guare,J.P.(Merck & Co.,Inc.)
参考来源:EP 0541168; JP 1993279337; WO 9309096

Vinblastine sulfate, 29060-LE, NSC-49842, Velbe, Velsar, Velban

硫酸长春碱长春质碱 Chemical Name: Vincaleukoblastine sulfate
CAS No. 143-67-9, 865-21-4 (free base)
项目整合开发状态: Launched
项目研究机构: Janssen (Originator), Lilly (Licensee)
合成路线:A stereocontrolled total ...
参考文献标题:Stereocontrolled total synthesis of (+)-vinblastine
文献作者:Yokoshima,S.; Ueda,T.; Kobayashi,S.; Sato,A.; Kuboyama,T.; Tokuyama,H.; Fukuyama,T.
参考来源:J Am Chem Soc 2002,124(10),2137

Abacavir sulfate, 1592U89 sulfate, Ziagen

硫酸阿巴卡韦阿巴卡韦Chemical Name: (1R,4S)-cis-2-Amino-6-(cyclopropylamino)-9-[4-(hydroxymethyl)-2-cyclopentenyl]-9H-purine sulfate (2:1); (1S,4R)-4-[2-Amino-6-(cyclopropylamino)-9H-purin-9-yl]-2-cyclopentene-1...
参考文献标题:Therapeutic nucleosides
文献作者:Daluge,S.M.(Glaxo Wellcome plc)
参考来源:AU 8937025; EP 0349242; JP 1990045486; JP 1999139976; US 5034394; US 5089500

Sulukast, LY-170680

硫鲁司特Chemical Name: (1S,2R)-5-[3-[2-(2-Carboxyethylthio)-1-hydroxypentadeca-3(E),5(Z)-dienyl]phenyl]-1H-tetrazole; 3-[[(1R,2E,4Z)-1-[(alphaS)-alpha-Hydroxy-m-1H-tetrazol-5-ylbenzyl]-2,4-tetradecadienyl...
参考文献标题:Sulukast
文献作者:Wishart,G.; Baker,S.R.; Lucas,R.; Boot,J.R.
参考来源:Drugs Fut 1991,16(5),432

Iomorinate sodium, ST-5614, Oravesin

碘吗酸Chemical Name: N-[2,4,6-Triiodo-3-[(1-morpholinoethylidene)amino]benzoyl]-2-methyl-beta-alanine sodium salt; 2-Methyl-3-[2,4,6-triiodo-3-[(1-morpholinoethylidene)amino]benzoylamino]propionic acid s...
参考文献标题:
文献作者:Obendorf,W.; Schwarzinger,E.; Krieger,J.; Lindner,I.
参考来源:DE 2235935; DE 3000215

Iopentol, Compound-5411, Ivepaque, Imagopaque

碘喷托Chemical Name: N,N'-Bis(2,3-dihydroxypropyl)-5-[N-(2-hydroxy-3-methoxypropyl)acetamido]-2,4,6-triiodoisophthalamide; 5-[Acetyl(2-hydroxy-3-methoxypropyl)amino]-N,N'-bis(2,3-dihydroxypropyl)-2,4,6-t...
参考文献标题:X-Ray contrast agents
文献作者:Wille,K.(Amersham plc)
参考来源:EP 0105752

Iopamidol, SQ-13396, Iopamyron, Niopam

碘帕醇Chemical Name: N,N'-Bis[2-hydroxy-1-(hydroxymethyl)ethyl]-5-[2(S)-hydroxypropionamido]-2,4,6-triiodoisophthalamide; N,N'-Bis[2-hydroxy-1-(hydroxymethyl)ethyl]-5-[2(S)-hydroxypropionamido]-2,4,6-tri...
参考文献标题:
文献作者:Felder,E.; Pitre,D.
参考来源:BE 836355; CA 1046082; CH 608189; DE 122475; DE 2547789; FR 2293919; GB 1472050; HU 12463; JP 7682236; NL 7512208; PT 64567; US 4001323; ZA 7507222

Ioxilan, Oxilan, Imagenil

碘昔兰Chemical Name: N-(2,3-Dihydroxypropyl)-5-[N-(2,3-dihydroxypropyl)acetamido]-N'-(2-hydroxyethyl)-2,4,6-triiodoisophthalamide
CAS No. 107793-72-6
项目整合开发状态: Launched-1996
项目研究机构: Cook Imaging...
参考文献标题:Non-ionic polyol contrast media from ionic contrast media
文献作者:Sovak,M.; Ranganathan,R.(Cook Imaging Corp.)
参考来源:WO 8700757

Idoxifene, SB-223030, CB-7432

碘昔芬Chemical Name: (E)-1-(4-Iodophenyl)-2-phenyl-1-[4-(2-pyrrolidinoethoxy)phenyl]-1-butene; (E)-1-[2-[4-[1-(4-Iodophenyl)-2-phenyl-1-butenyl]phenoxy]ethyl]pyrrolidine
CAS No. 116057-75-1
项目整合开发状...
参考文献标题:Tamoxifen derivs
文献作者:McCague,R.(National Research Development Corp.)
参考来源:EP 0260066; GB 2196003; JP 1988077845

Iobitridol, Xenetix

碘比醇Chemical Name: N,N'-Bis(2,3-dihydroxypropyl)-5-[3-hydroxy-2-(hydroxymethyl)propionamido]-2,4,6-triiodo-N,N'-dimethylisophthalamide
CAS No. 136949-58-1
项目整合开发状态: Launched-1995
项目研究机构: Guerb...
参考文献标题:Non-ionic iodinated cpds.,procedure for their preparation and contrast agents containing them
文献作者:Schaefer,M.; Dugast-Zrihen,M.; Guillemot,M.; Doucet,D.; Meyer,D.(Guerbet SA)
参考来源:EP 0437144; WO 9109836