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:275777

Chemical Name: (2S*,3R*,4S*)-4-(1,3-Benzodioxol-5-yl)-1-(N,N-dibutylcarbamoylmethyl)-2-hexylpyrrolidinel-3-carboxylic acid
CAS No. 195706-09-3
项目整合开发状态: Preclinical
项目研究机构: Abbott (Originator...
参考文献标题:Novel benzo-1,3-dioxolyl- and benzofuranyl substd.pyrrolidine derivs.as endothelin antagonists
文献作者:Winn,M.; Boyd,S.A.; Hutchins,C.W.; Tasker,A.S.; Von Geldern,T.W.; Kester,J.A.; Sorensen,B.K.; Szczepankiewicz,B.G.; Henry,K.J.Jr.; Liu,G.; Wittenberger,S.J.; King,S.A.(Abbott Laboratories Inc.)
参考来源:EP 0885215; WO 9730045

新产品编号:277359

Chemical Name: (2S*,3R*,4S*)-4-(1,3-Benzodioxol-5-yl)-1-(N,N-dibutylcarbamoylmethyl)-2-(4-methylcyclohexyl)pyrrolidine-3-carboxylic acid
CAS No. 195732-11-7
项目整合开发状态: Biological Testing
项目研究机...
参考文献标题:Novel benzo-1,3-dioxolyl- and benzofuranyl substd.pyrrolidine derivs.as endothelin antagonists
文献作者:Winn,M.; Boyd,S.A.; Hutchins,C.W.; Tasker,A.S.; Von Geldern,T.W.; Kester,J.A.; Sorensen,B.K.; Szczepankiewicz,B.G.; Henry,K.J.Jr.; Liu,G.; Wittenberger,S.J.; King,S.A.(Abbott Laboratories Inc.)
参考来源:EP 0885215; WO 9730045

YM-53389

Chemical Name: (+)-2-Chloro-5-methoxy-4-[5-[piperidin-2(S)-ylmethyl]-1,2,4-oxadiazol-3-yl]phenylamine monohydrochloride
CAS No. 220850-98-6, 220850-99-7 ((R)-isomer), 174822-16-3 (free base, undefi...
参考文献标题:Synthesis of the selective 5-hydroxytryptamine 4 (5-HT4) receptor agonist (+)-(S)-2-chloro-5-methoxy-4-[5-(2-piperidylmethyl)-1,2,4-oxadiazol-3-yl]aniline
文献作者:Suzuki,T.; Iwaoka,K.; Imanishi,N.; Nagakura,Y.; Miyata,K.; Nakahara,H.; Ohta,M.; Mase,T.
参考来源:Chem Pharm Bull 1999,47(1),120

新产品编号:994005

Chemical Name: 4-[4-(4-Chlorophenyl)-1H-pyrazol-3-yl]morpholine
CAS No. 88743-53-7
项目整合开发状态: Preclinical
项目研究机构: Asta Medica (Originator)
合成路线:(4-Chlorophenyl)thioacetic acid morpholide (I...
参考文献标题:Synthesis,anticonvulsant activity,and structure-activity relationships of sodium channel blocking 3-aminopyrroles
文献作者:Unverferth,K.; Engel,J.; Hofgen,N.; Rostock,A.; Gunther,R.; Lankau,H.J.; Menzer,M.; Rolfs,A.; Liebscher,J.; Muller,B.; Hofmann,H.J.
参考来源:J Med Chem 1998,41(1),63

SGI-101

Chemical Name: N-(2,6-Dioxopiperidin-3-yl)-3-(4-nitrophenyl)-2-propenamide
CAS No. 167173-00-4
项目整合开发状态: Biological Testing
项目研究机构: Mansoura University (Originator)
合成路线:4-Nitrocinnamic ac...
参考文献标题:Design of drugs involving receptor-ligand-DNA interactions
文献作者:Hendry,L.B.
参考来源:WO 9514791

NS-2381-[11C], [11C]-NS-2381

Chemical Name: 8-([11C]Methyl)-3-[4-(trifluoromethyl)phenyl]-8-azabicyclo[3.2.1]oct-2-ene
CAS No. 189746-51-8 (maleate), 189746-50-7 (unlabeled)
项目整合开发状态: Preclinical
项目研究机构: NeuroSearch (Ori...
参考文献标题:8-Azabicyclo[3.2.1]oct-2-ene derivs.,their preparation and use
文献作者:Moldt,P.; Scheel-Kr黦er,J.; Olsen,G.M.; Nielsen,E.O.(NeuroSearch A/S)
参考来源:EP 0859777; JP 1998512589; WO 9713770

RPR-118723

Chemical Name: (-)-2-(6-Chloro-9-methyl-2,3-dioxo-2,3,4,9-tetrahydro-1H-indeno[1,2-b]pyrazin-9-yl)acetic acid
CAS No. 173187-06-9, 173187-05-8 ((+)-enantiomer), 173186-99-7 (undefined isomer)
项目...
参考文献标题:5H-Indeno[1,2-b]pyrazine-2,3-dione derivs.,their preparation and medicinal products containing them
文献作者:Jimonet,P.; Ribeill,Y.; Audiau,F.; Aloup,J.-C.; Barreau,M.; Mignani,S.; Genevois-Borella,A.; Damour,D.(Aventis Pharma SA)
参考来源:US 5922716; WO 9526342

新产品编号:617489

Chemical Name: 2-[2-(Dimethylamino)ethyl]-6-[2-(dimethylamino)ethylamino]-9-hydroxy-2,3-dihydro-1H,7H-pyrimido[5,6,1-de]acridine-1,3,7-trione dihydrobromide
CAS No. 236402-26-9
项目整合开发状态: Biologi...
参考文献标题:2,3-Dihydro-1H,7H-pyrimido[5,6,1-de]acridine-1,3,7-trione derivatives,a class of cytotoxic agents active on multidrug-resistant cell lines: Synthesis,biological evaluation,and structure-activity relationships
文献作者:Antonini,I.; Polucci,P.; Kelland,L.R.; Menta,E.; Pescalli,N.; Martelli,S.
参考来源:J Med Chem 1999,42(14),2535

4-Methyldicamphanoylkhellactone, PA-344, 4-Methyl-DCK

Chemical Name: Bis[(1S,1'S,4R,4'R)-4,7,7-trimethyl-3-oxo-2-oxabicyclo[2.2.1]heptane-1-carboxylic acid] (9R,10R)-4,8,8-trimethyl-2-oxo-9,10-dihydro-2H,8H-benzo[1,2-b:3,4-b']dipyran-9,10-diyl ester; (9R...
参考文献标题:Anti-AIDS agent 33.Synthesis and anti-HIV activity of mono-methyl substituted 3',4'-di-O-(-)-camphanoyl-(+)-cis-khellactone (DCK) analogues
文献作者:Xie,L.; Takeuchi,Y.; Cosentino,L.M.; Lee,K.-H.
参考来源:Bioorg Med Chem Lett 1998,8(16),2151

新产品编号:424485

Chemical Name: Bis[(1S,1'S,4R,4'R)-4,7,7-trimethyl-3-oxo-2-oxabicyclo[2.2.1]heptane-1-carboxylic acid] (9R,10R)-5,8,8-trimethyl-2-oxo-9,10-dihydro-2H,8H-benzo[1,2-b:3,4-b']dipyran-9,10-diyl ester; (9R...
参考文献标题:Anti-AIDS agent 33.Synthesis and anti-HIV activity of mono-methyl substituted 3',4'-di-O-(-)-camphanoyl-(+)-cis-khellactone (DCK) analogues
文献作者:Xie,L.; Takeuchi,Y.; Cosentino,L.M.; Lee,K.-H.
参考来源:Bioorg Med Chem Lett 1998,8(16),2151