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

新产品编号:609579

Chemical Name: 1-[2-[8-(3-Fluorophenyl)-9-methyl-9H-adenin-2-yl]ethynyl]cyclopentanol hydrochloride
CAS No. 232253-35-9, 232252-63-0 (free base), 232252-64-1 (sulfate (1:1) salt)
项目整合开发状态: Precl...
参考文献标题:Purine derivs.and adenosine A2 receptor antagonists serving as preventives/remedies for diabetes
文献作者:Asano,O.; Hoshino,Y.; Kobayashi,S.; Nagata,K.; Harada,H.; Yoshikawa,S.; Nagaoka,J.; Inoue,T.; Horizoe,T.; Yasuda,N.; Murakami,M.(Eisai Co.,Ltd.)
参考来源:EP 1054012; JP 1999263789; WO 9935147

新产品编号:448215

Chemical Name: 5-tert-Butyl-3-(2,3-dichlorophenylureido)-1H-pyrrole-2-carboxylic acid methyl ester
CAS No. 216573-65-8
项目整合开发状态: Biological Testing
项目研究机构: Bayer (Originator)
合成路线:Esterifi...
参考文献标题:Inhibition of p38 kinase activity by aryl ureas
文献作者:Gunn,D.; Ranges,G.; Chen,J.; Bombara,M.; Scott,W.; Rauner,D.; Redman,A.; Paulsen,H.; Smith,R.; Renick,J.(Bayer Corp.)
参考来源:WO 9852558

YM-193489

Chemical Name: N-(1,3-Benzodioxol-5-yl)-3-[3-(6,7-dimethoxy-1,2,3,4-tetrahydroisoquinolin-2-ylcarbonyl)piperidin-1-yl]propionamide
CAS No. 312738-02-6 ((R)-isomer, anhydrous D-tartrate), 312738-08-...
参考文献标题:Novel isoquinoline derivs.or salts thereof
文献作者:Okazaki,T.; Watanabe,T.; Wada,K.; Kakefuda,A.; Masuda,N.(Yamanouchi Pharmaceutical Co.,Ltd.)
参考来源:EP 1186601; WO 0075133

SC-73770, M-40401

Chemical Name: (PB-7-11-2344'3')-Dichloro[(4aR,6S,12S,13aR,17aR,21aR)-6,12-dimethyl-11,7-nitrilo-1,2,3,4,4a,5,6,12,13,13a,14,15,16,17,17a,18,19,20,21,21a-eicosahydro-7H-dibenzo[b,h][1,4,7,10]tetraazac...
参考文献标题:Biomaterials modified with superoxide dismutase mimics
文献作者:Udipi,K.; Joardar,S.; Forster,D.; Riley,D.; Henke,S.; Brethaur,K.; Thurmond,B.; Ornberg,R.(Pharmacia Corp.)
参考来源:WO 0072893

SR-125329, SSR-125329A

Chemical Name: N-[3-[4-(2-Adamantyl)-3,5-dichlorophenyl]-2(Z)-propenyl]-N-cyclohexyl-N-ethylamine
CAS No. 313510-43-9, 313511-26-1 (fumarate), 313510-02-0 (hydrochloride), 313511-27-2 (maleate)
...
参考文献标题:Benzene derivs.,preparation method and pharmaceutical compsns.containing same
文献作者:Paul,R.; Boigegrain,R.; Nisato,D.; Casellas,P.; Herbert,J.M.; Bourrie,B.; Bourrie,M.; Lair,P.; Vernieres,J.C.(Sanofi-Synthabo)
参考来源:EP 1192122; FR 2794742; JP 2003502306; US 6482986; WO 0076953

ZXY-1106, TX-527

Chemical Name: 1alpha,25-Dihydroxy-14,20-bisepi-23,23,24,24-tetradehydro-19-norvitamin D3
CAS No. 163379-89-3
项目整合开发状态: Preclinical
项目研究机构: Th閞amex (Originator)
合成路线:The precursor bicyclic...
参考文献标题:Novel structural analogues of vitamin D
文献作者:Bouillon,R.; Vandewalle,M.; De Clercq,P.J.(Laboratoire Th閞amex)
参考来源:EP 0707566; EP 0972762; US 6548715; WO 9501960

GW-475151A(hydrochloride), GW-475151

Chemical Name: (3S,3aS,6aR)-3-Isopropyl-1-(methylsulfonyl)-4-[2-(1-pyrrolidinylmethyl)oxazol-4-ylcarbonyl]perhydropyrrolo[3,2-b]pyrrol-2-one
CAS No. 221323-42-8, 221323-43-9 (diastereomer), 221321-...
参考文献标题:Pyrrolopyrrolone derivs.as inhibitors of neutrophil elastase
文献作者:Dowle,M.D.; Finch,H.; Harrison,L.A.; Inglis,G.G.A.; Johnson,M.R.; Macdonald,S.J.F.; Shah,P.; Smith,R.A.(Glaxo Wellcome plc)
参考来源:EP 0891362; JP 2000507950; US 5994344; WO 9736903

新产品编号:285269

Chemical Name: N-(2-Isopropoxyphenyl)-N'-(1,6-naphthyridin-2-yl)urea
CAS No. 197507-01-0
项目整合开发状态: Biological Testing
项目研究机构: Shire BioChem (Originator)
合成路线:Treatment of 2-isopropoxypheny...
参考文献标题:Naphthyridine derivs.and their analogues inhibiting cytomegalovirus
文献作者:Jin,H.; Chan,L.C.-K.; Wang,W.; Stefanac,T.; Mansour,T.S.; Nguyen-Ba,P.; Lavallee,J.-F.; Falardeau,G.(Shire BioChem Inc.)
参考来源:EP 0984967; JP 2001515464; US 5945431; WO 9734894

新产品编号:835805

Chemical Name: 3-O-(3,3-Dimethylsuccinyl)-28-O-(2,2-dimethylsuccinyl)lup-20(29)-en-3beta,28-diol
CAS No. 332346-42-6
项目整合开发状态: Biological Testing
项目研究机构: BBI Biotech Research Laboratories (Or...
参考文献标题:3,28-Di-O-(dimethylsuccinyl)-betulin isomers as anti-HIV agents
文献作者:Kashiwada,Y.; Chiyo,J.; Ikeshiro,Y.; Nagao,T.; Okabe,H.; Cosentino,L.M.; Fowke,K.; Lee,K.H.
参考来源:Bioorg Med Chem Lett 2001,11(2),183

新产品编号:804165

Chemical Name: 3'-Azido-3'-deoxy-5'-O-(4-hydroxybutyloxycarbonyl)thymidine
CAS No. 313343-81-6
项目整合开发状态: Preclinical
项目研究机构: Laphal (Originator)
合成路线:The desired product can be obtained by...
参考文献标题:Novel cpds.derived from nucleosides,preparation methods and pharmaceutical compsns.containing same
文献作者:Kraus,J.-L.; Clerc,T.; Salles,J.-P.; Vlieghe,P.(Laboratoires Laphal)
参考来源:FR 2794752; WO 0077020