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:709245

Chemical Name: 4-[3-Chloro-4-(1-methyl-1H-imidazol-2-ylsulfanyl)phenylamino]-6-methoxy-7-[3-(4-morpholinyl)propoxy]quinoline-3-carbonitrile
CAS No. 263171-01-3
项目整合开发状态: Preclinical
项目研究机构: W...
参考文献标题:Substd.3-cyanoquinolines as protein tyrosine kinase inhibitors
文献作者:Frost,P.; Floyd,M.B.Jr.; Wissner,A.; Hamann,P.R.; Zhang,N.; Tsou,H.-R.; Berger,D.M.; Salvati,M.E.(Wyeth)
参考来源:EP 1117659; JP 2002525369; WO 0018761

A-373857

Chemical Name: 5-[1-(4-Cyanophenyl)-1-(1-methyl-1H-imidazol-5-yl)methoxymethyl]-6-(2,2-difluoro-1,3-benzodioxol-5-yl)pyridine-2-carbonitrile
CAS No. 450839-23-3
项目整合开发状态: Preclinical
项目研究机构: ...
参考文献标题:Farnesyltransferase inhibitors
文献作者:Sham,H.L.; Rockway,T.W.; Li,T.; Mantei,R.A.; Li,Q.; Lin,N.-H.; Wang,L.; Wang,W.; Wang,X.; Sullivan,G.M.; Wang,G.T.; Gwaltney,S.L.II; Claiborne,A.K.; Hasvold,L.A.; Tong,Y.(Abbott Laboratories Inc.)
参考来源:US 2002115640; WO 0274747

新产品编号:937053

Chemical Name: N9-[4-(4-Methoxyphenyl)thiazol-2-yl]-N1-methyl-2-oxononanediamide
CAS No. 436151-49-4
项目整合开发状态: Preclinical
项目研究机构: Abbott (Originator)
合成路线:The known methyl 7-hydroxyheptan...
参考文献标题:Inhibitors of histone deacetylase
文献作者:Holms,J.H.; Davidsen,S.K.; Michaelides,M.R.; Guo,Y.; Heyman,H.R.; Curtin,M.L.; Wada,C.K.; Dai,Y.; Vasudevan,A.; Frey,R.R.; Ji,Z.(Abbott Laboratories Inc.)
参考来源:WO 0246129

新产品编号:938635

Chemical Name: N9-[4-[4-[2-(Dimethylamino)ethoxy]phenyl]thiazol-2-yl]-N1-methyl-2-oxononanediamide
CAS No. 436152-19-1
项目整合开发状态: Biological Testing
项目研究机构: Abbott (Originator)
合成路线:The kno...
参考文献标题:Inhibitors of histone deacetylase
文献作者:Holms,J.H.; Davidsen,S.K.; Michaelides,M.R.; Guo,Y.; Heyman,H.R.; Curtin,M.L.; Wada,C.K.; Dai,Y.; Vasudevan,A.; Frey,R.R.; Ji,Z.(Abbott Laboratories Inc.)
参考来源:WO 0246129

BMS-411886

Chemical Name: N-[1-Carbamoyl-2-[N-(2-hydroxyethyl)-N-methylamino]ethyl]-2-[(1S,18S,21E,28S,29R,30S)-30-[(2S,4S,5R,6S)-5-(dimethylamino)-4-hydroxy-4,6-dimethyltetrahydropyran-2-yloxy]-9,52-dihydroxy-1...
参考文献标题:Water soluble thiazolyl peptide derivs.
文献作者:Bronson,J.J.; Lam,K.S.; Ueda,Y.; Wichtowski,J.A.; Sorenson,M.E.; Li,W.; Kim,O.K.; Zhang,Y.; Naidu,B.N.; Connolly,T.P.(Bristol-Myers Squibb Co.)
参考来源:WO 0214354

SCH-400

Chemical Name: 4-[8-Chloro-6,11-dihydro-5H-benzo[5,6]cyclohepta[1,2-b]pyridin-11(S)-yl]-2(R)-[3(S)-(4-methyl-1H-imidazol-1-ylmethyl)piperidin-1-ylcarbonyl]piperazine-1-carboxylic acid cyclohexyl ester...
参考文献标题:Farnesyl protein transferase inhibitors
文献作者:Cooper,A.B.; Girijavallabhan,V.M.; Mallams,A.K.; Doll,R.J.; Kelly,J.M.; Rane,D.F.; Taveras,A.G.; Guzi,T.; Strickland,C.; Chao,J.(Schering Corp.)
参考来源:EP 1140904; JP 2002533335; WO 0037458

新产品编号:929143

Chemical Name: 3-[5-[2-[N-(2-Methoxyethyl)-N-methylamino]ethoxy]-1H-indol-2-yl]quinolin-2(1H)-one
CAS No. 408502-06-7, 415684-73-0 (citrate), 415684-71-8 (hydrochloride), 415684-70-7 (methanesulfon...
参考文献标题:Orally active salts with tyrosine kinase activity
文献作者:Fraley,M.E.; Kim,Y.; Karki,S.B.(Merck & Co.,Inc.)
参考来源:WO 0232861

新产品编号:764615

Chemical Name: N-[1(S)-[N-[2-(Benzyloxy)-1(R)-cyanoethyl]carbamoyl]-2-cyclohexylethyl]morpholine-4-carboxamide
CAS No. 290817-02-6
项目整合开发状态: Biological Testing
项目研究机构: Boehringer Ingelheim (O...
参考文献标题:Cpds.useful as reversible inhibitors of cathepsin S
文献作者:Frye,L.L.; Cywin,C.L.; Morwick,T.; Spero,D.M.; Thomson,D.; Ward,Y.(Boehringer Ingelheim Pharmaceuticals Inc.)
参考来源:JP 2002538151; US 6395897; WO 0051998

BIO-9002, BG-9928

Chemical Name: 3-[4-(2,6-Dioxo-1,3-dipropyl-2,3,6,9-tetrahydro-1H-purin-8-yl)bicyclo[2.2.2]oct-1-yl]propionic acid; 3-[4-(1,3-Dipropylxanthin-8-yl)bicyclo[2.2.2]oct-1-yl]propionic acid
CAS No. 3400...
参考文献标题:Polycycloalkylpurines as adenosine receptor antagonists
文献作者:Ensinger,C.L.; Kumaravel,G.; Petter,R.C.; Dowling,J.E.; Kiesman,W.F.; Chang,H.X.; Lin,K.C.(Biogen,Inc.)
参考来源:EP 1230243; JP 2003513982; WO 0134610

新产品编号:818403

Chemical Name: 2-[2-(5-Bromo-2-methoxybenzylsulfanyl)-3-chlorophenyl]-1,4,5,6-tetrahydropyrimidine
CAS No. 325823-79-8
项目整合开发状态: Biological Testing
项目研究机构: Millennium (Originator)
合成路线:Con...
参考文献标题:Melanocortin-4 receptor binding cpds.and methods of use thereof
文献作者:Maguire,M.P.; Dai,M.; Vos,T.J.(Millennium Pharmaceuticals,Inc.)
参考来源:WO 0110842