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:2229547

Chemical Name: 2-(Cyclohexylsulfanyl)-6-[1-(2,6-difluorophenyl)ethyl]-5-methylpyrimidin-4(3H)-one
项目整合开发状态: Biological Testing
项目研究机构:
合成路线:The condensation of 2-(2,6-difluorophenyl)acetic a...
参考文献标题:Selected non-nucleoside reverse transcriptase inhibitors (NNRTIs): the DABOs family
文献作者:Artico,M.
参考来源:Drugs Fut 2002,27(2),159

SN-22977, NSC-683247, AMAC

Chemical Name: 9-Amino-N-[2-(dimethylamino)ethyl]-5-methylacridine-4-carboxamide
项目整合开发状态: Biological Testing
项目研究机构: University of Auckland (Originator)
合成路线:The intermediate 6-methyldipheny...
参考文献标题:Potential antitumor agents.46.Structure-activity relationships for acridine monosubstituted derivatives of the antitumor agent N-[2-(dimethylamino)ethyl]-9-aminoacridine-4-carboxamide
文献作者:Rewcastle,G.W.; Atwell,G.J.; Chambers,D.; Baguley,B.C.; Denny,W.A.
参考来源:J Med Chem 1986,29(4),472

新产品编号:2231129

Chemical Name: 7-[4-[4-[4-(3-Carboxy-1-cyclopropyl-6-fluoro-4-oxo-1,4-dihydroquinolin-7-yl)piperazin-1-ylmethyl]benzyl]piperazin-1-yl]-1-ethyl-6-fluoro-4-oxo-1,4-dihydroquinoline-3-carboxylic acid
...
参考文献标题:Synthesis and antibacterial activity of novel piperazinyl-linked fluoroquinolones
文献作者:Grucz,R.G.; Kerns,R.J.; Kaatz,G.W.; Vaka,F.; Rybak,M.J.
参考来源:41st Intersci Conf Antimicrob Agents Chemother (Dec 16 2001,Chicago) 2001,Abst F-565

新产品编号:2232711

Chemical Name: 1'-Benzyl-17-(cyclopropylmethyl)-6,7-didehydro-4,5alpha-epoxy-3,14beta-dihydroxy-4'-phenylpyrrolo[2',3':6,7]morphinan
项目整合开发状态: Preclinical
项目研究机构: University of Bath (Originator)...
参考文献标题:4'-Arylpyrrolomorphinans: Effect of a pyrrolo-N-benzyl substituent in enhancing delta-opioid antagonist activity
文献作者:Srivastava,S.K.; Husbands,S.M.; Aceto,M.D.; Miller,C.N.; Traynor,J.R.; Lewis,J.W.
参考来源:J Med Chem 2002,45(2),537

新产品编号:2234293

Chemical Name: N-[4-(3,20-Dioxopregn-4-en-7alpha-ylsulfanyl)phenyl]-N'-[1(R)-phenylethyl]urea
项目整合开发状态: Biological Testing
项目研究机构: Georgetown University (Originator)
合成路线:Progesterone (I) was...
参考文献标题:Progesterone analogs to reverse multidrug resistance
文献作者:Clarke,R.; Talebian,A.H.; Ghiorghis,A.; Leonessa,F.; Hammer,C.(Georgetown University)
参考来源:WO 9700683

新产品编号:2235875

Chemical Name: 5,20-(4-Fluorophenyl)-10,15-bis(4-sulfophenyl)-21,23-dithiaporphyrin disodium salt
项目整合开发状态: Preclinical
项目研究机构: Roswell Park Cancer Institute (Originator), State University of Ne...
参考文献标题:Water-soluble,core-modified porphyrins as novel longer-wavelength-absorbing sensitizers for photodynamic therapy.II.Effects of core heteroatoms and meso-substituents on biological activity
文献作者:Hilmey,D.G.; Abe,M.; Nelen,M.I.; Stilts,C.E.; Baker,G.A.; Baker,S.N.; Bright,F.V.; Davies,S.R.; Gollnick,S.O.; Oseroff,A.R.; Gibson,S.L.; Hilf,R.; Detty,M.R.
参考来源:J Med Chem 2002,45(2),449

新产品编号:2237457

Chemical Name: 6-O-(Piperidin-3-ylcarbonyl)-L-ascorbic acid
项目整合开发状态: Preclinical
项目研究机构: Medical College of Georgia (Originator), Universit?di Ferrara (Originator)
合成路线:Condensation between ...
参考文献标题:Prodrugs derivs.of the ascorbic acid suitable to the passage of the hematoencephalic barrier
文献作者:Manfredini,S.(Universit?di Ferrara)
参考来源:WO 0270499

新产品编号:2239039

Chemical Name: 12-[5(S)-Hydroxy-6(S)-methylpiperidin-2(R)-yl]dodecan-3-one
项目整合开发状态: Biological Testing
项目研究机构:
合成路线:The hydrolysis of the chiral isopropylidene ketal (I) with HCl in refluxi...
参考文献标题:Application of chiral building blocks to the synthesis of drugs
文献作者:Toyooka,N.; Nemoto,H.
参考来源:Drugs Fut 2002,27(2),143

新产品编号:2240621

Chemical Name: 12-[5(S)-Hydroxy-6(S)-methylpiperidin-2(S)-yl]dodecan-2-one
项目整合开发状态: Not Determined
项目研究机构:
合成路线:The hydrolysis of the chiral isopropylidene ketal (I) with HCl in refluxing m...
参考文献标题:Application of chiral building blocks to the synthesis of drugs
文献作者:Toyooka,N.; Nemoto,H.
参考来源:Drugs Fut 2002,27(2),143

新产品编号:2242203

Chemical Name: 12-[5(R)-Hydroxy-6(S)-(hydroxymethyl)piperidin-2(R)-yl]dodecan-3-one
项目整合开发状态: Not Determined
项目研究机构:
合成路线:The hydrolysis of the chiral isopropylidene ketal (I) with HCl in re...
参考文献标题:Application of chiral building blocks to the synthesis of drugs
文献作者:Toyooka,N.; Nemoto,H.
参考来源:Drugs Fut 2002,27(2),143