新项目精选

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：PROTAC/分子胶降解剂：通过诱导靶蛋白泛素化降解发挥作用，而非传统“占位驱动”抑制。这类分子的项目整合需要同时考量靶点配体、E3连接酶配体及连接子的三元复合物优化，临床前到临床的转化难度显著增加。多肽/环肽药物：介于小分子与生物制品之间，兼具高选择性与口服可用性潜力。项目整合中需重点解决稳定性、递送及生产工艺放大问题。抗体-药物偶联物（ADC）：作为“生物导弹”，ADC的项目整合涉及抗体、连接子、有效载荷三部分的协同优化，需要跨学科团队的深度整合。小核酸药物（siRNA/ASO）：通过基因沉默机制发挥作用，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。展望未来，新型API项目的整合将呈现以下趋势：第一，AI贯穿全链条。从靶点发现、分子优化到临床开发、上市后监测，AI将成为贯穿API全生命周期的核心工具。第二，数据资产化。临床研究数据和真实世界数据将从“辅助工具”升级为“核心资产”，数据驱动的决策将成为项目整合的标准范式。第三，开放整合生态。API经济的成熟正在推动制药企业从“封闭研发”走向“开放协作”，通过API接口与外部数据源、技术平台、CRO/CDMO实现无缝对接. 而API技术——无论是数据接口还是组织协作的“应用程序接口”——正成为支撑这一整合的核心基础设施。
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新项目整合精选

新产品编号:1435383

Chemical Name: 4-(Acetyloxy)-6,7-dichloro-5,8-dioxo-5,8-dihydro-1-naphthalenyl acetate
项目整合开发状态: Biological Testing
项目研究机构: China Medical College (Originator), National Taiwan University (Origin...
参考文献标题:Synthesis and antiplatelet,antiinflammatory,and antiallergic activities of substituted 3-chloro-5,8-dimethoxy-1,4-naphthoquinone and related compounds
文献作者:Huang,L.-J.; Chang,F.C.; Lee,K.H.; Wang,J.P.; Teng,C.M.; Kuo,S.C.
参考来源:Bioorg Med Chem 1998,6(12),2261

新产品编号:1436965

Chemical Name: trans-7-Bromo-2-methyl-4-oxo-2,3,4,10-tetrahydro-1H-phenothiazine-3-carboxylic acid tert-butyl ester
项目整合开发状态: Preclinical
项目研究机构: 3M Pharmaceuticals (Originator), Bristol-Myers S...
参考文献标题:Synthesis,characterization,and anticonvulsant activity of enaminones.Part 5: Investigations on 3-carboalkoxy-2-methyl-2,3-dihydro-1H-phenothiazin-4[10H]-one derivatives
文献作者:Laws,M.L.; Roberts,R.R.; Nicholson,J.M.; Butcher,R.; Stables,J.P.; Goodwin,A.M.; Smith,C.A.; Scott,K.R.
参考来源:Bioorg Med Chem 1998,6(12),2289

新产品编号:1438547

Chemical Name: N-[3(R)-Benzyl-1-[1(S)-formyl-3-phenylpropyl]-2-oxopyrrolidin-3-yl]carbamic acid benzyl ester
项目整合开发状态: Biological Testing
项目研究机构: Indiana University (Originator), University of M...
参考文献标题:Structure-based design,synthesis and evaluation of conformationally constrained cysteine protease inhibitors
文献作者:Scheidt,K.A.; Roush,W.R.; McKerrow,J.H.; Selzer,P.M.; Hansell,E.; Rosenthal,P.J.
参考来源:Bioorg Med Chem 1998,6(12),2477

新产品编号:1440129

Chemical Name: N-[3(R)-Benzyl-1-[1(S)-formyl-3-phenylpropyl]-2-oxopyrrolidin-3-yl]benzenesulfonamide
项目整合开发状态: Biological Testing
项目研究机构: Indiana University (Originator), University of Michigan ...
参考文献标题:Structure-based design,synthesis and evaluation of conformationally constrained cysteine protease inhibitors
文献作者:Scheidt,K.A.; Roush,W.R.; McKerrow,J.H.; Selzer,P.M.; Hansell,E.; Rosenthal,P.J.
参考来源:Bioorg Med Chem 1998,6(12),2477

新产品编号:1441711

Chemical Name: (all-Z)-N-(2-Propynyl)-5,8,11,14-icosatetraenamide
项目整合开发状态: Biological Testing
项目研究机构: National Hellenic Research Foundation (Originator), University of Connecticut (Originator)<...
参考文献标题:Novel analogues of arachidonylethanolamide (anandamide): Affinities for the CB1 and CB2 cannabinoid receptors and metabolic stability
文献作者:Lin,S.; Khanolkar,A.D.; Fan,P.; Goutopoulos,A.; Qin,C.; Papahadjis,D.; Makriyannis,A.
参考来源:J Med Chem 1998,41(27),5353

ACEA

Chemical Name: (all-Z)-N-(2-Chloroethyl)-5,8,11,14-icosatetraenamide
项目整合开发状态: Preclinical
项目研究机构: National Hellenic Research Foundation (Originator), University of Connecticut (Originator)
合...
参考文献标题:Novel analogues of arachidonylethanolamide (anandamide): Affinities for the CB1 and CB2 cannabinoid receptors and metabolic stability
文献作者:Lin,S.; Khanolkar,A.D.; Fan,P.; Goutopoulos,A.; Qin,C.; Papahadjis,D.; Makriyannis,A.
参考来源:J Med Chem 1998,41(27),5353

新产品编号:1443293

Chemical Name: (4R,5S,6S,7R)-1,3,4,7-Tetrabenzyl-5,6-dihydroxyhexahydro-1,3-diazepin-2-one
项目整合开发状态: Biological Testing
项目研究机构: Bristol-Myers Squibb (Originator)
合成路线:1) The condensation of b...
参考文献标题:Process for the preparation of mixed anhydrides
文献作者:Trussardi,R.; Karpf,M.(F.Hoffmann-La Roche AG)
参考来源:EP 0847994

SB-T-101187

Chemical Name: [2aR-[2aalpha,4beta,4abeta,6beta,9alpha(2R,3S),10beta,11beta,12alpha,12aalpha,12balpha]]-6,12b-Diacetoxy-9-[3-(tert-butoxycarbonylamino)-3-[2,2-dimethyl-1(R)-cyclopropyl]-2-hydroxypropi...
参考文献标题:A four-week intravenous toxicity study of flecainide acetate in rats with a two-week recovery phase
文献作者:Toyoshi,T.; Nomura,T.; Ogawa,A.; et al.
参考来源:Clin Rep 1994,28(6),13

SB-T-12843

Chemical Name: [2aR-[2aalpha,4beta,4abeta,6beta,9alpha(2R,3R),10beta,11beta,12alpha,12aalpha,12balpha]]-12b-Acetoxy-12-benzoyloxy-9-[3-(tert-butoxycarbonylamino)-4,4-difluoro-2-hydroxybutyryloxy]-6-(3...
参考文献标题:Syntheses and biological activity of advanced second-generation taxoids
文献作者:Lin,S.; et al.
参考来源:216th ACS Natl Meet (Aug.23-27,Boston) 1998,Abst MEDI 315

Methanandamide-(R), (R)-Methanandamide

Chemical Name: (all-Z)-N-[2-Hydroxy-1(R)-methylethyl]-5,8,11,14-icosatetraenamide
项目整合开发状态: Preclinical
项目研究机构: National Cancer Institute (Originator), University of Connecticut (Originator)
...
参考文献标题:(R)-Methanandamide: A chiral novel anandamide possessing higher potency and metabolic stability
文献作者:Abadji,V.; Lin,S.; Taha,G.; Griffin,G.; Stevenson,L.A.; Pertwee,R.G.; Makriyannis,A.
参考来源:J Med Chem 1994,37(12),1889