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

TAK-457

Chemical Name: 4-(Acetoxymethyl)-1-[2(R)-(2,4-difluorophenyl)-2-hydroxy-3(R)-[2-oxo-3-[4-(1H-tetrazol-1-yl)phenyl]imidazolidin-1-yl]butyl]-1H-1,2,4-triazol-4-ium chloride
CAS No. 214543-30-3, 21454...
参考文献标题:Azole cpds.,their production and their use
文献作者:Itoh,K.; Okonogi,K.; Kitazaki,T.(Takeda Chemical Industries,Ltd.)
参考来源:EP 0973768; JP 1999228548; JP 2000198773; WO 9843970

CS-758, R-120758

Chemical Name: trans-4-[4-[5-[2(R)-(2,4-Difluorophenyl)-2-hydroxy-1(R)-methyl-3-(1H-1,2,4-triazol-1-yl)propylsulfanyl]-1,3-dioxan-2-yl]-1(E),3(E)-butadienyl]-3-fluorobenzonitrile
CAS No. 329744-44-...
参考文献标题:Triazole antifungal agent
文献作者:Oida,S.; Tanaka,T.; Tajima,Y.; Konosu,T.; Somada,A.; Miyaoka,T.; Yasuda,H.(Sankyo Co.,Ltd.)
参考来源:EP 0841327; JP 1996333350; US 5977152; WO 9631491

MnTE-2-PyP5+, AEOL-10113

Chemical Name: (SP-4-1)-[[2,2',2'',2'''-(21H,23H-Porphine-5,10,15,20-tetrayl-kappaN21,kappaN22,kappaN23,kappaN24)tetrakis[1-ethylpyridiniumato]](2-)]manganese(5+)
CAS No. 223723-79-3, 219818-60-7 (...
参考文献标题:Substd.porphyrins
文献作者:Batinic-Haberle,I.; Fridovich,I.(Duke University)
参考来源:EP 1045851; JP 2001521939; WO 9923097

AMD-7049(free base), AMD-8664

Chemical Name: N-(2-Pyridinylmethyl)-N-[4-(1,4,7-triazacyclotetradecan-4-ylmethyl)benzyl]amine tetrahydrochloride
CAS No. 255383-00-7
项目整合开发状态: Preclinical
项目研究机构: AnorMED (Originator)
合成路...
参考文献标题:Antiviral macrocyclic cpds.
文献作者:Bogucki,D.E.; Boehringer,E.M.; Wang,Z.; Bridger,G.J.; Schols,D.; Skerlj,R.T.(AnorMED Inc.)
参考来源:EP 1095031; WO 0002870

BB-3497

Chemical Name: N2-[2(R)-(N-Formyl-N-hydroxyaminomethyl)hexanoyl]-N1,N1-dimethyl-L-tert-leucinamide; 2(R)-Butyl-N-formyl-N-hydroxy-beta-alanyl-N,N,3-trimethyl-L-valinamide
CAS No. 235784-88-0
项目整...
参考文献标题:Antibacterial agents
文献作者:Spavold,Z.M.; Launchbury,S.; Clements,J.M.; Hunter,M.G.; Davies,S.J.; Pratt,L.M.; Beckett,R.P.; Whittaker,M.(British Biotech Pharmaceuticals Ltd.)
参考来源:WO 9939704

NNC-21-0300

Chemical Name: 5'-Deoxy-2,5'-dichloro-N6-[4-(2-pyridylsulfanyl)piperidin-1-yl]adenosine
CAS No. 206270-32-8
项目整合开发状态: Preclinical
项目研究机构: Novo Nordisk (Originator)
合成路线:The N-amination of ...
参考文献标题:Novel therapeutically active adenosine derivs.
文献作者:Knutsen,L.(Novo Nordisk A/S)
参考来源:WO 9816539

SB-264128

Chemical Name: (3R,4S)-N-(1-Azabicyclo[2.2.1]hept-3-ylcarbonyl)carbamic acid (1S,2R,3S,4S,6R,7R,8R,14R)-3-hydroxy-2,4,7,14-tetramethyl-9-oxo-4-vinyltricyclo[ 5.4.3.0(1,8)]tetradec-6-yl ester hydrochlo...
参考文献标题:Carbamoyloxy derivs.of mutuline and their use as antibacterials
文献作者:Hinks,J.D.; Takle,A.K.; Hunt,E.(SmithKline Beecham plc)
参考来源:EP 0874809; EP 0934316; JP 2000503642; US 6121281; WO 9725309; WO 9805659

S-34324

Chemical Name: 4-(5-Fluoroindan-2-ylmethyl)-4,5-dihydro-1H-imidazole
CAS No. 276235-47-3
项目整合开发状态: Preclinical
项目研究机构: Servier (Originator)
合成路线:2-(Hydroxymethyl)-5-fluoroindane (I) was co...
参考文献标题:Imidazoline derivs.,preparation and pharmaceutical compsns.containing them
文献作者:Newman-Tancredi,A.; Lacoste,J.-M.; Millan,M.; Cordi,A.; Gobert,A.(ADIR et Cie.)
参考来源:EP 1010693; FR 2787451; JP 2000178255; US 6127396

S-19014

Chemical Name: 5',6'-Dimethylspiro[4,5-dihydro-1H-imidazol-4,2'-indane] fumarate
CAS No. 162098-61-5, 162098-60-4 (free base)
项目整合开发状态: Preclinical
项目研究机构: Servier (Originator)
合成路线:Knoeve...
参考文献标题:Benzospiroalkene derivs.,process for their preparation and pharmaceutical compsns.containing them
文献作者:Cordi,A.; Lacoste,J.-M.; Laubie,M.; Verbeuren,T.; Descombes,J.-J.(ADIR et Cie.)
参考来源:CA 2128359; EP 0635497; FR 2709306; JP 1995304753; US 5436261

W-1807, BAY-W-1807

Chemical Name: (-)-4(S)-(2-Chlorophenyl)-1-ethyl-2-methyl-1,4-dihydropyridine-3,5,6-tricarboxylic acid 3- isopropyl ester disodium salt
CAS No. 252721-95-2 (free acid)
项目整合开发状态: Preclinical
项...
参考文献标题:1-Alkyl-substd.1,4-dihydropyridine lactones,process for their preparation and their use in pharmaceuticals
文献作者:Puls,W.; Bossert,F.; Petzinna,D.; Schlossmann,K.; Goldmann,S.; Bischoff,H.(Bayer AG)
参考来源:DE 3410645; EP 0158138; ES 8607309; ES 8702413; ES 8702414; ES 8702415; ES 8702416; ES 8702417; ES 8702418; ES 8704173; ES 8704174; US 5026714