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

RWJ-337813

Chemical Name: N-[3-[4-(6,7-Dihydro-5H-pyrrolo[3,4-b]pyridin-6-yl)-3-fluorophenyl]-2-oxooxazolidin-5(S)-ylmethyl]acetamide
CAS No. 344459-54-7, 344459-57-0 (enantiomer)
项目整合开发状态: Preclinical
...
参考文献标题:Antibacterial heterobicyclic substd.phenyl oxazolidinones
文献作者:Hlasta,D.; Paget,S.(Ortho-McNeil Pharmaceutical,Inc.)
参考来源:EP 1206469; US 6413981; WO 0142242

RWJ-334181

Chemical Name: N-[3-[4-(2,3-Dihydro-1H-pyrrolo[3,4-c]pyridin-2-yl)-3-fluorophenyl]-2-oxooxazolidin-5(S)-ylmethyl]acetamide
CAS No. 344459-92-3
项目整合开发状态: Preclinical
项目研究机构: R.W. Johnson (Orig...
参考文献标题:Antibacterial heterobicyclic substd.phenyl oxazolidinones
文献作者:Hlasta,D.; Paget,S.(Ortho-McNeil Pharmaceutical,Inc.)
参考来源:EP 1206469; US 6413981; WO 0142242

NG-38

Chemical Name: 9-Isopropyl-N-(4-methoxybenzyl)-2-(perhydroazepin-1-yl)-9H-purin-6-amine
CAS No. 244030-38-4
项目整合开发状态: Biological Testing
项目研究机构: Novartis (Originator)
合成路线:The alkylation o...
参考文献标题:Discovery of estrogen sulfotransferase inhibitors from a purine library screen
文献作者:Verdugo,D.E.; Cancilla,M.T.; Ge,X.; Gray,N.S.; Chang,Y.T.; Schultz,P.G.; Negishi,M.; Leary,J.A.; Bertozzi,C.R.
参考来源:J Med Chem 2001,44(17),2683

新产品编号:823149

Chemical Name: 4-[5-[1-(3-Chlorobenzyl)-2-oxopyrrolidin-3(S)-ylaminomethyl]-1H-imidazol-1-ylmethyl]benzonitrile
CAS No. 330185-25-6, 330182-86-0 (diHCl), 330185-24-5 (enantiomer)
项目整合开发状态: Precl...
参考文献标题:Inhibitors of prenyl-protein transferase
文献作者:Beshore,D.C.; Bell,I.M.; Gallicchio,S.N.; Sisko,J.T.; Zartman,C.B.; Lumma,W.C.Jr.(Merck & Co.,Inc.)
参考来源:WO 0117992

新产品编号:759869

Chemical Name: [mu-(Ethanethioamidato-kappaN:kappaS)]bis(2,2':6',2''-terpyridine-kappaN1,kappaN1',kappaN1'')diplatinum(3+) trinitrate
CAS No. 289685-03-6, 289685-02-5 (cation)
项目整合开发状态: Biologic...
参考文献标题:Platinum(II) cpds.
文献作者:Lowe,G.(Isis Innovation Ltd.)
参考来源:EP 1155025; WO 0050431

BMS-419437

Chemical Name: N-[5-(5-tert-Butyloxazol-2-ylmethylsulfanyl)thiazol-2-yl]-2-[4-[2-hydroxy-1-(hydroxymethyl)ethylaminomethyl]phenyl]acetamide
CAS No. 333389-24-5, 333389-66-5 (hydrochloride)
项目整合开...
参考文献标题:N-[5-[[[5-Alkyl-2-oxazolyl]methyl]thio]-2-thiazolyl]-carboxamide inhibitors of cyclin dependent kinases
文献作者:Kim,K.S.; Misra,R.N.; Hunt,J.T.; Kimball,S.D.; Poss,M.A.; Han,W.-C.; Webster,K.R.; Cai,Z.-W.; Rawlins,D.B.(Bristol-Myers Squibb Co.)
参考来源:EP 1240165; WO 0144241

N-Nonyl-deoxygalactojirimycin, N-nonyl-DGJ, Alkovir

Chemical Name: (2R,3S,4R,5S)-2-(Hydroxymethyl)-1-nonyl-3,4,5-piperidinetriol; 1,5-Dideoxy-1,5-(nonylimino)-D-galactitol
CAS No. 223771-83-3
项目整合开发状态: Preclinical
项目研究机构: Thomas Jefferson Univ...
参考文献标题:Long chain N-alkyl cpds.and oxa-derivs.thereof
文献作者:Jacob,G.S.; Butters,T.D.; Fleet,G.W.J.; Carrouee,S.; Dwek,R.A.; Platt,F.M.; Zitzmann,N.; Picker,D.H.
参考来源:WO 0110429

新产品编号:519405

Chemical Name: N-[4-(3-Bromophenylamino)quinazolin-6-yl]-4-(dimethylamino)-2(E)-butenamide
CAS No. 220699-51-4
项目整合开发状态: Preclinical
项目研究机构: Wyeth Pharmaceuticals (Originator)
合成路线:5-Nitro...
参考文献标题:Substd.quinazoline derivs.and their use as tyrosine kinase inhibitors
文献作者:Wissner,A.; Johnson,B.D.; Zhang,N.; Tsou,H.-R.; Hamann,P.R.(American Cyanamid Co.)
参考来源:EP 1000039; JP 2001515071; WO 9909016

Frederine

Chemical Name: 2-(3,4-Dihydroxyphenyl)-3-(D-glucopyranosyloxy)-4H-1-benzopyran-4-one
CAS No. 307521-67-1, 199469-77-7 ((S)-isomer)
项目整合开发状态: Preclinical
项目研究机构: Universiteit Maastricht (Origi...
参考文献标题:Synthesis of novel 3,7-substituted-2-(3',4'-dihydroxyphenyl) flavones with improved antioxidant activity
文献作者:van Acker,F.A.; Hageman,J.A.; Haenen,G.R.; van Der Vijgh,W.J.; Bast,A.; Menge,W.M.
参考来源:J Med Chem 2000,43(20),3752

新产品编号:870609

Chemical Name: N-Decanoyl-L-tryptophyl-L-asparaginyl-L-aspartyl-L-threonyl-glycyl-Ndelta-(DL-tryptophyl)-L-ornithyl-L-aspartyl-D-alanyl-L-aspartyl-glycyl-D-seryl-threo-3-methyl-L-glutamyl-gamma-(2-ami...
参考文献标题:Lipopeptides as antibacterial agents
文献作者:Watson,A.D.; Hill,J.; Zhang,Y.; Finn,J.; Yu,X.Y.; Keith,D.; Morytko,M.; Parr,I.; Siedlecki,J.; Silverman,J.; Christensen,D.; Lazarova,T.(Cubist Pharmaceuticals,Inc.)
参考来源:WO 0144274