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

L-758298

福沙匹坦二甲葡胺福沙吡坦杂质1 Chemical Name: 3-[2(R)-[1(R)-[3,5-Bis(trifluoromethyl)phenyl]ethoxy]-3(S)-(4-fluorophenyl)morpholin-4-ylmethyl]-5-oxo-4,5-dihydro-1H-1,2,4-triazole-1-phosphinic acid bis(N-methyl-D-gl...
参考文献标题:Prodrugs of morpholine tachykinin receptor antagonists
文献作者:Dorn,C.P.; Hale,J.J.; Maccoss,M.; Mills,S.G.(Merck & Co.,Inc.)
参考来源:EP 0748320; JP 1997509935; US 5691336; WO 9523798

Formidacillin, Fomidacillin sodium, BRL-36650

福米西林Chemical Name: 6beta-[D-2-[(4-Ethyl-2,3-dioxopiperazin-1-yl)carbonylamino]-2-(3,4-dihydroxyphenyl)acetamido]-6alpha-formamidopenicillinic acid sodium salt
CAS No. 98048-07-8 (free acid)
项目整合...
参考文献标题:beta -Lactam antibacterial agents
文献作者:Milner,P.H.(SmithKline Beecham plc)
参考来源:EP 0071395; GB 2107307; US 4539149; US 4609652; US 4877783

Foropafant, SR-27417

福罗帕泛Chemical Name: 2-[N-[2-(Dimethylamino)ethyl]-N-(3-pyridylmethyl)amino]-4-(2,4,6-triisopropylphenyl)thiazole
CAS No. 136468-36-5
项目整合开发状态: Phase II
项目研究机构: Sanofi-Aventis (Originator)
合...
参考文献标题:SR 27417,a highly potent,selective and long-acting antagonist of the PAF receptor
文献作者:Herbert,J.M.; Valette,G.; Bernat,A.; Savi,P.; Maffrand,J.P.; Le Fur,G.
参考来源:Drugs Fut 1992,17(11),1011

Forphenicinol, Forfenimex

福芬诺尔福酚美克 Chemical Name: L-2-(3-Hydroxy-4-hydroxymethylphenyl)glycine; (-)-(R)-alpha-Amino-3-hydroxy-4-(hydroxymethyl)benzeneacetic acid
CAS No. 71522-58-2, 72973-11-6 ((+)-enantiomer)
项目整合开发状态:...
参考文献标题:Pharmacological cpd.with immunopotentiating activity and production and uses thereof
文献作者:Aoyagi,T.; Ishizuka,M.; Matsumoto,I,.Morishima,H.; Takeuchi,T.; Umezawa,H.; Yamamoto,T.(Microbial Chemistry Research Foundation)
参考来源:US 4238507

Fotemustine, S-10036, Servier-10036, Muphoran

福莫司汀Chemical Name: (?-[1-[3-(2-Chloroethyl)-3-nitrosoureido]ethyl]phosphonic acid diethyl ester
CAS No. 92118-27-9
项目整合开发状态: Launched-1990
项目研究机构: ADIR (Originator), Servier (Originator), Ita...
参考文献标题:New nitrosourea derivs.,process for preparing them and pharmaceutical compsns.containing them
文献作者:Lavielle,G.; Cudennec,C.(ADIR et Cie.)
参考来源:FR 2536075

Arformoterol, (R,R)-Formoterol

福莫特罗酒石酸福莫特罗 Chemical Name: (-)-N-[2-Hydroxy-5-[1(R)-hydroxy-2-[2-(4-methoxyphenyl)-1(R)-methylethylamino]ethyl]phenyl]formamide
CAS No. 67346-49-0, 200815-49-2 (tartrate)
项目整合开发状态: Phase III 参考文献标题:Formoterol process
文献作者:Hett,R.; Senanayake,C.H.; Fang,K.Q.; Wald,S.A.; Redmon,M.P.; Gao,Y.(Sepracor Inc.)
参考来源:US 6040344

Fosinopril sodium, SQ-28555, Tenso-stop, Eliten, Fositen, Fozitec, Monopril HCT, Dynacil, Fosinorm, Monopril, Staril

福辛普利钠福辛普利 Chemical Name: 4(S)-Cyclohexyl-1-[2-[(R)-[2-methyl-1(S)-(1-propionyloxy)propoxy](4-phenylbutyl)phosphinyl]acetyl]-L-proline sodium salt
CAS No. 88889-14-9, 98048-97-6 (free acid)
项目整合...
参考文献标题:Process and intermediates for preparing trans-4-substd.-S-prolines
文献作者:Thottathil,J.K.(Bristol-Myers Squibb Co.)
参考来源:EP 0183390; US 4588819

Zindoxifene, NSC-341952, D-16726

秦哚昔芬Chemical Name: 5-Acetoxy-2-(4-acetoxyphenyl)-1-ethyl-3-methylindole
CAS No. 86111-26-4
项目整合开发状态: Phase II
项目研究机构: Degussa (Originator)
合成路线:4-Methoxyaniline (I) is reacted with 2'-brom...
参考文献标题:D-16726
文献作者:von Angerer,E.; Sheldrick,W.S.; Engel,J.; Schneider,M.R.
参考来源:Drugs Fut 1985,10(4),281

Tefluxitol, Lu-10-022

秦氟替索Chemical Name: 2-[4-[3-[7-Fluoro-2-(trifluoromethyl)-10H-dibenzo[b,e]thiopyran-10-yl]propyl]piperazin-1-yl]ethanol
CAS No. 55837-23-5, 53542-42-0 (diHCl)
项目整合开发状态: Not Determined
项目研究机构: ...
参考文献标题:
文献作者:Buus,J.M.L.; Lassen,N.; Bigler,A.J.
参考来源:AT 332395; AT 345826; BE 845057; CA 1010870; DE 2359359; FR 2209573; FR 2320740; GB 1453828; GB 1498394; JP 7494691; JP 7739682; NL 7316035; NL 7608822; US 4042695; US 4044024; ZA 7308990; ZA 7604544

Lysuride maleate, Lisuride maleate, Dopergin

稠环乙脲Chemical Name: 3-(6-Methyl-9,10-didehydroergolin-8alpha-yl)-1,1-diethylurea maleate
CAS No. 18016-80-3 (free base)
项目整合开发状态: Launched-1982
项目研究机构: Schering-Plough (Originator)
合成路线:The...
参考文献标题:Process for the preparation of ergoline derivs.
文献作者:Sauer,G.; Haffer,G.(Schering AG)
参考来源:EP 0074921