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:1973263

Chemical Name: 1,5-Bis(4-hydroxy-2,3,5-trimethylphenoxy)pentane
项目整合开发状态: Biological Testing
项目研究机构: Tokushima Bunri University (Originator)
合成路线:The target product can be obtained by condens...
参考文献标题:Antioxidative and 5-lipoxygenase inhibiting activities of novel bis(4-hydroxy-2,3,5-trimethylphenoxy)alkyl derivatives
文献作者:Hirano,T.; Kawasaki,N.; Miyataka,H.; Nishiki,M.; Satoh,T.
参考来源:Chem Pharm Bull 2001,49(2),225

新产品编号:1974845

Chemical Name: Acetic acid 1-[2-(1H-imidazol-4-yl)-1(R)-methylethylcarbamoyloxy]ethyl ester
项目整合开发状态: Preclinical
项目研究机构: Freie Universit鋞 Berlin (Originator), INSERM (Originator)
合成路线:Treatm...
参考文献标题:Enzyme-catalyzed prodrug approaches for the histamine H3-receptor agonist (R)-alpha-methylhistamine
文献作者:Stark,H.; Krause,M.; Rouleau,A.; Garbarg,M.; Schwartz,J.C.; Schunack,W.
参考来源:Bioorg Med Chem 2001,9(1),191

TSRI-265

Chemical Name: N1,N3-Bis[2-[5(S)-carboxy-5-[4-(trifluoromethyl)benzyloxycarboxamido]pentylamino]-2-oxoethyl]benzene-1,3-dicarboxamide
项目整合开发状态: Preclinical
项目研究机构: Scripps Research Institute (Or...
参考文献标题:Identification of a novel class of small-molecule antiangiogenic agents through the screening of combinatorial libraries which function by inhibiting the binding and localization of proteinase MMP2 to integrin alphavbeta3
文献作者:Boger,D.L.; Goldberg,J.; Silletti,S.; Kessler,T.; Cheresh,D.A.
参考来源:J Am Chem Soc 2001,123(7),1280

新产品编号:1976427

Chemical Name: 5-Chloro-N4-(cyclopropylmethyl)-N6-(2,6-dichloro-4-iodophenyl)-2-methyl-N4-propylpyrimidine-4,6-diamine
项目整合开发状态: Biological Testing
项目研究机构: National Institute on Drug Abuse (Orig...
参考文献标题:The development of a potential single photon emission computed tomography (SPECT) imaging agent for the corticotropin-releasing hormone receptor type 1
文献作者:Tian,X.; Hsin,L.-W.; Webster,E.L.; Contoreggi,C.; Chrousos,G.P.; Gold,P.W.; Habib,K.; Ayala,A.; Eckelman,W.C.; Jacobson,A.E.; Rice,K.C.
参考来源:Bioorg Med Chem Lett 2001,11(3),331

新产品编号:1978009

Chemical Name: N-[1-[2(S)-(Acetylsulfanyl)-3-methylbutanamido]cyclopentylcarbonyl]-4-(5-pyrimidinyl)-DL-phenylalanine methyl ester
项目整合开发状态: Preclinical
项目研究机构: Novartis (Originator)
合成路线:The...
参考文献标题:Synthesis and biological activity of novel potent endothelin-converting enzyme-1 inhibitors
文献作者:Firooznia,F.; Gude,C.; Chan,K.; Fink,C.A.; Qiao,Y.; Satoh,Y.; Marcopoulos,N.; Savage,P.; Beil,M.E.; Bruseo,C.W.; Trapani,A.J.; Jeng,A.Y.
参考来源:Bioorg Med Chem Lett 2001,11(3),375

新产品编号:1979591

Chemical Name: 3-[1-[4-[2-[2(R)-Hydroxy-2-(3-pyridyl)ethylamino]ethyl]phenylamino]-2(Z)-nitroethenylamino]benzamide
项目整合开发状态: Biological Testing
项目研究机构: Merck & Co. (Originator)
合成路线:Alternat...
参考文献标题:3-Pyridylethanolamines: Potent and selective human beta3 adrenergic receptor agonists
文献作者:Naylor,E.M.; Colandrea,V.J.; Candelore,M.R.; Cascieri,M.A.; Colwell,L.F.Jr.; Deng,L.; Feeney,W.P.; Forrest,M.J.; Hom,G.J.; MacIntyre,D.E.; Strader,C.D.; Tota,L.; Wang,P.R.; Wyvratt,M.J.; Fisher,M.H.; Weber,A.E.
参考来源:Bioorg Med Chem Lett 1998,8(21),3087

新产品编号:1981173

Chemical Name: 4-(Cyano-NNO-azoxy)-N-[6-[N2-cyano-N3-[3-[3-(1-piperidinylmethyl)phenoxy]propyl]guanidino]hexyl]benzamide
项目整合开发状态: Preclinical
项目研究机构: Universit?degli Studi "La Sapienza" (Origin...
参考文献标题:Anti-Helicobacter pylori agents endowed with H2-antagonist properties
文献作者:Sorba,G.; Bertinaria,M.; Di Stilo,A.; Gasco,A.; Scaltrito,M.M.; Brenciaglia,M.I.; Dubini,F.
参考来源:Bioorg Med Chem Lett 2001,11(3),403

新产品编号:1982755

Chemical Name: [2aR-[2aalpha,4beta,4abeta,6beta,9alpha(2R,3S),11beta,12alpha,12aalpha,12balpha]]-12b-Acetoxy-12-benzoyloxy-9-[3-(tert-butoxycarbonylamino)-2-hydroxy-3-phenylpropionyloxy]-11-hydroxy-4-...
参考文献标题:Orally active docetaxel analogue: Synthesis of 10-deoxy-10-C-morpholinoethyl docetaxel analogues
文献作者:Iimura,S.; Uoto,K.; Ohsuki,S.; Chiba,J.; Yoshino,T.; Iwahana,M.; Jimbo,T.; Terasawa,H.; Soga,T.
参考来源:Bioorg Med Chem Lett 2001,11(3),407

新产品编号:1984337

Chemical Name: 5-Fluoro-1-[4-(hydroxymethyl)-2,5-dihydro-2-furanyl]-1,2,3,4-tetrahydropyrimidine-2,4-dione
项目整合开发状态: Biological Testing
项目研究机构: Ewha Womans University (Originator), Korea Res. In...
参考文献标题:Synthesis and structure-activity relationships of novel apio and thioapio dideoxydidehydronucleosides as anti-HCMV agents
文献作者:Jeong,L.S.; Kim,H.O.; Moon,H.R.; Hong,J.H.; Yoo,S.J.; Choi,W.J.; Chun,M.W.; Lee,C.-K.
参考来源:J Med Chem 2001,44(5),806

新产品编号:1985919

Chemical Name: (9R,10R)-5-Methoxy-9,10-[4(R),7,7-trimethyl-3-oxo-2-oxabicyclo[2.2.1]heptan-1(S)-ylcarbonyloxy]-4,8,8-trimethyl-2,8,9,10-tetrahydrobenzo[1,2-b:3,4-b']dipyran-2-one
项目整合开发状态: Biologic...
参考文献标题:Anti-AIDS agents.42.Synthesis and anti-HIV activity of disubstituted (3'R,4'R)-3',4'-Di-O-(S)-camphanoyl-(+)-cis-khellactone analogues
文献作者:Xie,L.; Takeuchi,Y.; Cosentino,L.M.; McPhail,A.T.; Lee,K.-H.
参考来源:J Med Chem 2001,44(5),664