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

Ro-27-0574

Chemical Name: 26,26,26,27,27,27-Hexafluoro-1alpha,25-dihydroxy-20,21-methylene-23,24-didehydro-19-norvitamin D3
CAS No. 256459-48-0
项目整合开发状态: Preclinical
项目研究机构: Roche (Originator)
合成路线:T...
参考文献标题:1,3-Dihydroxy-20,20-dialkyl-vitamin D3 analogs
文献作者:Uskokovic,M.R.; Manchand,P.S.(F.Hoffmann-La Roche AG)
参考来源:EP 1015423; WO 9912894

Ro-25-9022

Chemical Name: 26,26,26,27,27,27-Hexafluoro-1alpha,25-dihydroxy-16,17,23,24-tetradehydro-19-norvitamin D3
CAS No. 165811-43-8
项目整合开发状态: Preclinical
项目研究机构: Roche (Originator)
合成路线:Reductio...
参考文献标题:Vitamin D3 analogs
文献作者:Doran,T.I.; Hennessy,B.M.; McLane,J.A.; Pizzolato,G.; Sedarati,F.; Uskokovic,M.R.(F.Hoffmann-La Roche AG)
参考来源:EP 0654467; JP 1995188159; US 5428029

ABT-866

Chemical Name: N-[3-(1H-Imidazol-4-ylmethyl)phenyl]ethanesulfonamide
CAS No. 258526-74-8, 258526-75-9 (maleate salt (1:1))
项目整合开发状态: Preclinical
项目研究机构: Abbott (Originator)
合成路线:Reaction o...
参考文献标题:Imidazoles and related cpds.as alpha1A agonists
文献作者:Altenbach,R.J.; Holladay,M.W.; Carroll,W.A.; Meyer,M.D.; Kerwin,J.F.Jr.; Kolasa,T.; Rohde,J.; Khilevich,A.(Abbott Laboratories Inc.)
参考来源:WO 0007997

UMJD-1369

Chemical Name: 4,6-Diamino-7-(2-phenylethyl)-7H-pyrrolo[2,3-d]pyrimidine-5-carbonitrile
CAS No. 284040-35-3
项目整合开发状态: Biological Testing
项目研究机构: Lake Erie College Osteopathic Medicine (Origin...
参考文献标题:Pyrrolo[2,3-d]pyrimidines as antiviral agents
文献作者:Townsend,L.B.; Drach,J.C.(University of Michigan)
参考来源:WO 0042043

DPC-681

Chemical Name: N-[3-[N-(3-Aminophenylsulfonyl)-N-isobutylamino]-1(S)-benzyl-2(R)-hydroxypropyl]-2(S)-[2-(3-fluorobenzylamino)acetamido]-3,3-dimethylbutyramide mesylate; N-(3-Fluorobenzyl)glycyl-L-tert...
参考文献标题:Bis-amino acid sulfonamides containing N-terminally A substd.benzyl group as HIV protease inhibitors
文献作者:Kaltenbach,R.F.; Trainor,G.L.(DuPont Pharmaceuticals Co.)
参考来源:EP 1140983; WO 0042060

DPC-684

Chemical Name: N-[3-[N-(4-Aminophenylsulfonyl)-N-isobutylamino]-1(S)-benzyl-2(R)-hydroxypropyl]-2(S)-[2-(3-fluorobenzylamino)acetamido]-3,3-dimethylbutyramide; N-(3-Fluorobenzyl)glycyl-L-tert-leucine ...
参考文献标题:Bis-amino acid sulfonamides containing N-terminally A substd.benzyl group as HIV protease inhibitors
文献作者:Kaltenbach,R.F.; Trainor,G.L.(DuPont Pharmaceuticals Co.)
参考来源:EP 1140983; WO 0042060

BMS-208782

Chemical Name: (S)-4-(3-Butyl-1,2,4-oxadiazol-5-yl)-N-(2,2-dimethylcyclopentylmethyl)benzamide
CAS No. 212380-82-0 ((-)-enantiomer), 212380-81-9 ((+)-enantiomer)
项目整合开发状态: Preclinical
项目研究机构:...
参考文献标题:Benzoic acid derivs.and related cpds.as antiarrhythmic agents
文献作者:Poss,M.A.; Lloyd,J.; Rovnyak,G.C.; Caulfield,T.J.; Atwal,K.S.; Stein,P.D.; Ahmad,S.(Bristol-Myers Squibb Co.)
参考来源:WO 9837068

新产品编号:136561

Chemical Name: N-(3-Carboxypropanoyl)-L-valyl-N-[1(S)-(diphenoxyphosphinyl)-2-phenylethyl]-L-prolinamide
CAS No. 174391-80-1
项目整合开发状态: Preclinical
项目研究机构: Dyax (Originator), Osaka Medical Col...
参考文献标题:Basic alpha-aminoalkylphosphonate derivs.
文献作者:Powers,J.C.; Ni,L.; Jackson,D.S.(Georgia Technology Research Corp.)
参考来源:US 5952307

A-277249

Chemical Name: N-Methyl-4-[4-(trifluoromethyl)phenoxy]thieno[2,3-c]pyridine-2-carboxamide
CAS No. 251994-26-0
项目整合开发状态: Preclinical
项目研究机构: Abbott (Originator), Icos (Codevelopment)
合成路线:T...
参考文献标题:Cell adhesion-inhibiting antiinflammatory cpds.
文献作者:Lartey,K.; Gunawardana,I.W.; Stout,D.M.; Bhatia,P.; Patel,M.V.; Staeger,M.A.; Boyd,S.A.; Mort,N.A.; Zhu,G.-D.; McCarty,C.M.; Stewart,A.O.; Arendsen,D.L.; Condroski,K.R.; Freeman,J.C.(Abbott Laboratories Inc.)
参考来源:WO 9962908

新产品编号:465617

Chemical Name: 1-(4-Methoxyphenyl)-3-methyl-N-(2'-sulfamoylbiphenyl-4-yl)-1H-pyrazole-5-carboxamide
CAS No. 218629-72-2
项目整合开发状态: Preclinical
项目研究机构: Bristol-Myers Squibb (Originator)
合成路线...
参考文献标题:Inhibitors of factor Xa with a neutral P1 specificity group
文献作者:Dominguez,C.; Fevig,J.M.; Galemmo,R.A.Jr.; Pinto,D.J.P.; Pruitt,J.R.; lma,P.; Quan,M.L.; Han,Q.(DuPont Pharmaceuticals Co.)
参考来源:US 5998424; WO 9857937