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

FY21-alphaalpha09

Chemical Name: trans-N2-Decanoyl-N5-[4-(2,5-diphenyloxazol-4-ylcarboxamido)cyclohexyl]-DL-glutamine
CAS No. 259679-03-3
项目整合开发状态: Biological Testing
项目研究机构: University of Pittsburgh (Originat...
参考文献标题:Identification of new Cdc25 dual specificity phosphatase inhibitors in a targeted small molecule array
文献作者:Yokokama,S.; Ducruet,A.P.; Rice,R.L.; Tamura,K.; Yokokawa,F.; Wipf,P.; Lazo,J.S.
参考来源:Bioorg Med Chem 2000,8(6),1451

DPC-423

Chemical Name: 1-[3-(Aminomethyl)phenyl]-N-[3-fluoro-2'-(methylsulfonyl)biphenyl-4-yl]-3-(trifluoromethyl)-1H-pyrazole-5-carboxamide
CAS No. 209957-47-1, 209957-48-2 (monotrifluoroacetate)
项目整合开...
参考文献标题:Nitrogen containing heteroaromatics as factor Xa inhibitors
文献作者:Orwat,M.J.; Cacciola,J.; Han,Q.; Fevig,J.M.; Pinto,D.J.P.; Rossi,K.A.; Pruitt,J.R.; Quan,M.L.(DuPont Pharmaceuticals Co.)
参考来源:EP 0946508; WO 9828269

SC-795

Chemical Name: (+)-1,1,1-Trifluoro-3-[N-(3-phenoxyphenyl)-N-[3-(1,1,2,2-tetrafluoroethoxy)benzyl]amino]propan-2(R)-ol
CAS No. 263264-30-8
项目整合开发状态: Preclinical
项目研究机构: Pfizer (Originator)
...
参考文献标题:(R)-Chiral halogenated 1-substd.amino-(n+1)-alkanols useful for inhibiting cholesteryl ester transfer protein activity
文献作者:Vernier,W.F.; Wang,L.; Mischke,D.A.; Hamme,A.T.; Promo,M.A.; Sikorski,J.A.; Spangler,D.P.; Grapperhaus,M.L.; Massa,M.A.; Durley,R.C.; Reinhard,E.J.; Fobian,Y.M.; Hickory,B.S.; Tollefson,M.B.; Norton,M.B.; Rueppel,M.L.(Pharmacia Corp.)
参考来源:WO 0018721; WO 0018724

ARM-434

Chemical Name: N,N-Diethyl-4-[1-(8-quinolyl)-1-(1-piperazinyl)methyl]benzamide
CAS No. 308110-21-6, 308110-65-8 (diHCl)
项目整合开发状态: Preclinical
项目研究机构: AstraZeneca (Originator)
合成路线:8-Bromoq...
参考文献标题:New diarylmethylpiperazines as potent and selective nonpeptide delta opioid receptor agonists with increased in vitro metabolic stability
文献作者:Plobeck,N.; Delorme,D.; Wei,Z.-Y.; Yang,H.O.; Zhou,F.; Schwarz,P.; Gawell,L.; Gagnon,H.; Pelcman,B.; Schmidt,R.; Yue,S.Y.; Walpole,C.; Brown,W.; Zhou,E.; Labarre,M.; Payza,K.; St-Onge,S.; Kamassah,A.; Morin,P.E.; Projean,D.; et al.
参考来源:J Med Chem 2000,43(21),3878

SCH-221153

Chemical Name: 3-[4-[1-(1H-Benzimidazol-2-ylmethyl)-3-cyclohexylureidomethyl]benzamido]-N-(benzyloxycarbonyl)-L-alanine; 3-[4-[1-(1H-Benzimidazol-2-ylmethyl)-3-cyclohexylureidomethyl]benzamido]-2(S)-(...
参考文献标题:Benzimidazole cpds.that are vitronectin receptor antagonists
文献作者:Neustadt,B.R.; Smith,E.M.(Schering Corp.)
参考来源:EP 1135374; WO 0032578

MX-1013, Z-VD-fmk, CV-1013

Chemical Name: N-(Benzyloxycarbonyl)-L-valyl-DL-aspartyl-fluoromethane
CAS No. 223568-55-6 ((S)-isomer)
项目整合开发状态: Preclinical
项目研究机构: Cytovia (Originator), Maxim (Licensee)
合成路线:2-Fluoroet...
参考文献标题:Dipeptide apoptosis inhibitors and the use thereof
文献作者:Guastella,J.; Yang,W.; Cai,S.X.; Keana,J.F.W.; Drewe,J.A.(Cytovia,Inc.)
参考来源:EP 1033910; US 6184210; WO 9918781

T-0970

Chemical Name: N'-(3-tert-Butyl-2-hydroxy-5-methoxyphenyl)-N-(3-pyridyl)-N-(4-pyridylmethyl)urea triphosphate
CAS No. 195313-54-3, 195313-53-2 (free base)
项目整合开发状态: Preclinical
项目研究机构: Tanabe...
参考文献标题:Phenol-derivs.having pharmaceutical activity and process for preparing the same
文献作者:Suzuki,T.; Ohmizu,H.; Hashimura,Y.; Kubota,H.; Tanaka,K.(Tanabe Seiyaku Co.,Ltd.)
参考来源:EP 0790240; JP 1998195037; US 5849732

VP-32947

Chemical Name: N-Propyl-N-[2-(5H-1,2,4-triazino[5,6-b]indol-3-ylsulfanyl)ethyl]-1-propanamine; 3-[2-(N,N-Dipropylamino)ethylsulfanyl]-5H-1,2,4-triazino[5,6-b]indole
CAS No. 212246-37-2, 189325-62-0...
参考文献标题:Methods for preventing and treating pestivirus infection and associated diseases
文献作者:Pevear,D.C.; Nitz,T.J.; Seipel,M.(ViroPharma,Inc.)
参考来源:WO 9836752

ICN-10776

Chemical Name: 4-Oxo-7-(beta-D-ribofuranosyl)-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidine-5-carboxamidine
CAS No. 22242-93-9
项目整合开发状态: Preclinical
项目研究机构: Valeant (Originator)
合成路线:Diazotizati...
参考文献标题:Pyrrolopyrimidine nucleosides.V.A study on the relative chemical reactivity of the 5-cyano group of the nucleoside antibiotic toyocamycin and desaminotoyocamycin.The synthesis of analogs of sangivamycin
文献作者:Hinshaw,B.C.; Gerster,J.F.; Robins,R.K.; Townsend,L.B.
参考来源:J Org Chem 1970,35(1),236

Vanidipinedilol

Chemical Name: 4-[4-[3-(tert-Butylamino)-2-hydroxypropoxy]-3-methoxyphenyl]-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylic acid dimethyl diester hydrochloride
CAS No. 257284-29-0
项目整合开发状态: Pr...
参考文献标题:Method for treating a neoplasm
文献作者:Donovan,S.(Allergan,Inc.)
参考来源:WO 0209743