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

(+)-Hemipalmitoylcarnitinium, Z-15

Chemical Name: 2-[6(S)-Hydroxy-4,4-dimethyl-6-pentadecylmorpholinium-2(R)-yl]acetate; (2S,6R)-6-(Carboxymethyl)-2-hydroxy-4,4-dimethyl-2-pentadecylmorpholinium inner salt
CAS No. 145554-73-0, 14563...
参考文献标题:Acylcarnitine analogues as topical,microbicidal spermicides
文献作者:Savle,P.S.; Doncel,G.F.; Bryant,S.D.; Hubieki,M.P.; Robinette,R.G.; Gandourk,R.D.
参考来源:Bioorg Med Chem Lett 1999,9(17),2545

新产品编号:294761

Chemical Name: 2-[4-[2-[4-(6-Aminopyridin-2-yl)phenyl]ethyl]piperazin-1-yl]-1-phenylethanone
CAS No. 198211-96-0
项目整合开发状态: Preclinical
项目研究机构: Pfizer (Originator)
合成路线:2-Amino-6-bromopyrid...
参考文献标题:6-Phenylpyridyl-2-amine derivs.
文献作者:Lowe,J.A.III; Whittle,P.J.(Pfizer Inc.)
参考来源:EP 0891332; JP 1999510513; WO 9736871

新产品编号:408665

Chemical Name: 4-[2-(Benzylamino)ethoxy]-2-trifluoromethyl-1H-benzimidazole
CAS No. 212062-12-9, 212062-13-0 (mono HCl salt)
项目整合开发状态: Preclinical
项目研究机构: Wyeth Pharmaceuticals (Originator) 参考文献标题:4-Aminoalkoxy-1H-benzimidazole derivs.,their preparation and their use as dopamine autoreceptor (D2) agonists
文献作者:Nelson,J.A.; Mewshaw,R.E.(American Home Products Corp.)
参考来源:EP 0973749; WO 9835945

J-110441

Chemical Name: (1R,5S,6S)-2-(Benzothien-2-ylsulfanyl)-6-[1(R)-hydroxyethyl]-1-methylcarbapen-2-em-3-carboxylic acid sodium salt; (4R,5S,6S)-3-(1-benzothiophen-2-ylsulfanyl)-6-[1(R)-hydroxyethyl]-4-met...
参考文献标题:Benzothiazolylthio carbapenems: Potent anti-MRSA agents
文献作者:Szumiloski,S.P.; Ratcliffe,R.W.; Waddell,S.T.; et al.
参考来源:Bioorg Med Chem Lett 1995,5(13),1427

BAL-2299, Ro-65-2299

Chemical Name: 5-[12,12,12-Trifluoro-11-hydroxy-7,7-dimethyl-11-(trifluoromethyl)dodeca-2(E),9(Z)-dienylidene]cyclohexane-1(R),3(R)-diol
CAS No. 241151-12-2
项目整合开发状态: Phase II
项目研究机构: Basilea...
参考文献标题:Cyclohexanediole derivs.
文献作者:Mohr,P.; Barbier,P.; Pirson,W.; Muller,M.; Bauer,F.(F.Hoffmann-La Roche AG)
参考来源:EP 1056716; WO 9943646

UIC-PI, UIC-94-003

Chemical Name: N-[1(S)-Benzyl-2(R)-hydroxy-3-[N-isobutyl-N-(4-methoxyphenylsulfonyl)amino]propyl]carbamic acid (3R,3aS,6aR)-hexahydrofuro[2,3-b]furan-3-yl ester
CAS No. 206362-00-7
项目整合开发状态: Bio...
参考文献标题:Multi-drug resistant retroviral protease inhibitors and associated methods
文献作者:Hussain,K.A.; Gulnik,S.V.; Ghosh,A.K.; Erickson,J.W.(University of Illinois; US Department of Health & Human Services)
参考来源:WO 9967254

SCH-59884

Chemical Name: 4-(Phosphonooxy)butyric acid 2(S)-[4-[4-[4-[4-[5(R)-(2,4-difluorophenyl)-5-(1H-1,2,4-triazol-1-ylmethyl)tetrahydrofuran-3(R)-ylmethoxy]phenyl]piperazin-1-yl]phenyl]-5-oxo-4,5-dihydro-1H...
参考文献标题:Tetrahydrofuran antifungals
文献作者:Saksena,A.K.; Girijavallabhan,V.M.; Lovey,R.G.; Pike,R.E.; Wang,H.; Liu,Y.-T.; Ganguly,A.K.; Bennett,F.(Schering Corp.)
参考来源:EP 0773941; WO 9638443

LY-314177

Chemical Name: 1(S),4a(S)-Dimethyl-6-methoxy-9-(4-methylpiperazin-1-ylimino)-1,2,3,4,4a,9,10,10a-octahydrophenanthrene-1-carboxylic acid methyl ester
CAS No. 199291-57-1 (beta-isomer)
项目整合开发状态: ...
参考文献标题:In vitro and in vivo activity of a series of influenza A inhibitors derived from podocarpic acid
文献作者:Sachs,R.K.; Hornback,W.J.; Tang,J.; Munroe,J.E.
参考来源:39th Intersci Conf Antimicrob Agents Chemother (Sept 26 1999,San Francisco) 1999,Abst F950

SB-247386

Chemical Name: (3aS,4R,5S,6S,8R,9R,9aR,10R)-N-(Quinuclidin-4-ylcarbonyl)carbamic acid 5-hydroxy-4,6,9,10-tetramethyl-1-oxo-6-vinyldecahydro-3a,9-propano-3aH-cyclopentacycloocten-8-yl ester
CAS No. ...
参考文献标题:Carbamoyloxy derivs.of mutuline and their use as antibacterials
文献作者:Hinks,J.D.; Takle,A.K.; Hunt,E.(SmithKline Beecham plc)
参考来源:EP 0874809; EP 0934316; JP 2000503642; US 6121281; WO 9725309; WO 9805659

Ro-62-6091

Chemical Name: 3-[5-(2,4-Diaminopyrimidin-5-ylmethyl)-2,3-dimethoxyphenyl]-1-[1(R)-(2-pyridyl)-1,2,3,4-tetrahydroisoquinolin-2-yl]-2(E)-propen-1-one
CAS No. 199476-01-2, 199476-03-4 (undefined isom...
参考文献标题:2,4-Diaminopyrimidine derivs.
文献作者:Guerry,P.; Stalder,H.; Wyss,P.-C.(F.Hoffmann-La Roche AG)
参考来源:EP 0901488; JP 1999511749; US 5866583; WO 9743277