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

MnTDE-2-ImP5+, AEOL-10150

Chemical Name: (SP-4-1)-[[2,2',2'',2'''-(21H,23H-Porphine-5,10,15,20-tetrayl-.kappaN21,.kappaN22,.kappaN23,.kappaN24)tetrakis[1,3-diethyl-1H-imidazoliumato]](2-)manganese(5+) pentachloride
CAS No. ...
参考文献标题:Substd.porphyrins
文献作者:Trova,M.P.; Kitchen,D.B.; Crapo,J.D.; Gauuan,P.J.F.; Day,B.J.(National Jewish Medical and Research Center)
参考来源:EP 1155019; JP 2002535332; WO 0043395

CFM-1571

Chemical Name: 1-Benzyl-3-[3-(dimethylamino)propoxy]-N-(4-methoxyphenyl)-1H-pyrazole-5-carboxamide
CAS No. 268725-86-6
项目整合开发状态: Preclinical
项目研究机构: Tripos (Originator), University College Lo...
参考文献标题:Activators of soluble guanylate cyclase
文献作者:Glen,R.; Liu,Q.; Powell,K.; Reynolds,K.; Madge,D.; Kling,M.; Selwood,D.; Wishart,G.(University College London)
参考来源:WO 0027394

TU-572

Chemical Name: 5-Isopropoxy-2-[4-(methylsulfanyl)pyridin-2-ylmethylsulfinyl]-1H-benzimidazole
CAS No. 326592-39-6
项目整合开发状态: Preclinical
项目研究机构: Inst. Physical Chemical Res. (RIKEN) (Originato...
参考文献标题:Synthesis and characterization of a potent selective protein tyrosine phosphatase inhibitor,2-[(4-methylthiopyridin-2-yl)methylsulfinyl]benzimidazole
文献作者:Hamaguchi,T.; Takahisha,A.; Kagamizono,T.; Manaka,A.; Sato,M.; Osada,H.
参考来源:Bioorg Med Chem Lett 2000,10(23),2657

新产品编号:807329

Chemical Name: Diaqua[N,N',N''-[nitrilotris[1(R)-(hydroxymethyl)-2,1-ethylanediyl]]tris[3-(hydroxy-kappaO)-1-methyl-2-(oxo-kappaO)-1,2-dihydropyridine-4-carboxamidato]](3-)]gadolinium
CAS No. 31518...
参考文献标题:A tris-hydroxymethyl-substituted derivative of Gd-TREN-Me-3,2-HOPO: An MRI relaxation agent with improved efficiency
文献作者:Hajela,S.; et al.
参考来源:J Am Chem Soc 2000,122(45),11228

Gadomelitol, P-792, Vistarem

Chemical Name: Hydrogen [2,2',2'',2'''-[1,4,7,10-tetraazacyclododecane-1,4,7,10-triyl]tetrakis[5-[[2-[[4- [[4-[[2-[[3,5-bis[bis[(2S,3R,4R,5R)-2,3,4,5,6-pentahydroxyhexyl-2,4,6-tribromo]carbamoyl]pheny...
参考文献标题:Gadolinium complex tetramides and use in medical imaging
文献作者:Rousseaux,O.; Simonot,C.(Guerbet SA)
参考来源:EP 1178975; FR 2793795; WO 0071526

新产品编号:815239

Chemical Name: N-(1-Cyano-3-pyrrolidinyl)benzenesulfonamide
CAS No. 325775-30-2
项目整合开发状态: Biological Testing
项目研究机构: Celera (Originator), Merck & Co. (Originator), Merck Frosst (Originator) 参考文献标题:Novel,nonpeptidic cyanamides as potent and reversible inhibitors of human cathepsins K and L
文献作者:Falgueyret,J.-P.; Oballa,R.M.; Okamoto,O.; Wesolowski,G.; Aubin,Y.; Rydzewski,R.M.; Prasit,P.; Riendeau,D.; Rodan,S.B.; Percival,M.D.
参考来源:J Med Chem 2001,44(1),94

新产品编号:683933

Chemical Name: (3R,5aS,6R,8aS,9R,10S,12R,12aR)-3,6,9-Trimethyl-10-[4-(trifluoromethyl)phenoxy]decahydro-3,12-epoxy-12H-pyrano[4,3-j]-1,2-benzodioxepin
CAS No. 256341-25-0
项目整合开发状态: Preclinical 参考文献标题:Peroxide-based antimalarial cpds.
文献作者:Ward,S.A.; O'Neill,P.M.(Ultrafine Ltd.)
参考来源:WO 0104123

Xyz-033mp

Chemical Name: 3(S)-[5-Benzyl-3-[2-methyl-1(S)-(1-naphthylcarboxamido)propyl]-4,5-dihydroisoxazol-5-ylcarboxamido]-5-(2,6-dichlorobenzoyloxy)-4-oxopentanoic acid
CAS No. 331778-84-8
项目整合开发状态: Pr...
参考文献标题:Caspase inhibitor
文献作者:Chung,H.-H.; Park,M.-J.; Min,C.-H.; Kang,C.-Y.; Park,T.-K.; Chang,H.-K.; Lee,T.-H.; Moon,K.-Y.; Kim,E.E.-K.; Oh,Y.-L.; Kim,Y.-M.(LG Chem Ltd.)
参考来源:WO 0121599; WO 0121600

Dimethylaminoarglabin hydrochloride, Arglabin-DMA.HCl

Chemical Name: (3aR,4aS,6aS,9aS,9bR)-7-(Dimethylaminomethyl)-1,4a-dimethyl-5,6,6a,7,9a,9b-hexahydro-3H-oxireno[8,8a]azuleno[4,5-b]furan-8(4aH)-one hydrochloride
CAS No. 188899-01-6, 215598-04-2 (fr...
参考文献标题:Pharmaceutical compsns.of arglabin and arglabin derivs.
文献作者:Adekenov,S.M.(Paracure,Inc.)
参考来源:US 5902809; WO 9848789

A-293620

Chemical Name: 1-Methyl-N-(3,4,5-trimethoxyphenyl)-1H-indole-5-sulfonamide
CAS No. 312299-45-9
项目整合开发状态: Preclinical
项目研究机构: Abbott (Originator)
合成路线:The reaction of indoline (I) with form...
参考文献标题:Cell proliferation inhibitors
文献作者:Barr,K.J.; Steiner,B.A.; Qun,L.; Rosenberg,S.; Sham,H.; Gwaltney,S.L.II; Imade,H.M.; Woods,K.W.(Abbott Laboratories Inc.)
参考来源:WO 0073264