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:2014395

Chemical Name: 3-(N-Acetyl-N-hydroxyamino)propylphosphonic acid bis(4-methoxyphenyl) diester
项目整合开发状态: Preclinical
项目研究机构: Jomaa Pharma (Originator), Justus-Liebeg-Universit鋞 Giessen (Originator...
参考文献标题:Diaryl ester prodrugs of FR900098 with improved in vivo antimalarial activity
文献作者:Reichenberg,A.; Wiesner,J.; Weidemeyer,C.; Dreiseidler,E.; Sanderbrand,S.; Altincicek,B.; Beck,E.; Schlitzer,M.; Jomaa,H.
参考来源:Bioorg Med Chem Lett 2001,11(6),833

新产品编号:2015977

Chemical Name: 3,4-Dihydroxy-1,6-dimethyl-2-(N-methylcarbamoyl)pyridinium chloride
项目整合开发状态: Preclinical
项目研究机构: King's College London (Originator)
合成路线:Kojic acid (I) was chlorinated with ne...
参考文献标题:Synthesis of 2-amino-3-hydroxypyridin-4(1H)-ones: Novel iron chelators with enhanced pFe3+ values
文献作者:Liu,Z.D.; Piyamongkol,S.; Liu,D.Y.; Khodr,H.H.; Lu,S.L.; Hider,R.C.
参考来源:Bioorg Med Chem 2001,9(3),563

新产品编号:2017559

Chemical Name: N-[2-(Dimethylamino)ethyl]-2-methyl-7-oxo-7H-naphtho[1,2,3-de]quinoline-11-carboxamide
项目整合开发状态: Preclinical
项目研究机构: La Trobe University (Originator), University of Auckland (Orig...
参考文献标题:Synthesis and cytotoxic activity of 7-oxo-7H-dibenz [f,ij]isoquinoline and 7-oxo-7H-benzo[e]perimidine derivatives
文献作者:Bu,X.; Deady,L.W.; Finlay,G.J.; Baguley,B.C.; Denny,W.A.
参考来源:J Med Chem 2001,44(12),2004

VUF-5228

Chemical Name: N3-(4-Chlorobenzyl)-N1-cyclohexyl-S-[3-[4(5)-imidazolyl]propyl]isothiourea
项目整合开发状态: Biological Testing
项目研究机构: De Novo Pharmaceuticals (Originator), University of Cambridge (Orig...
参考文献标题:Development of a pharmacophore model for histamine H3 receptor antagonists,using the newly developed molecular modeling program SLATE
文献作者:De Esch,I.J.P.; Mills,J.E.J.; Perkins,T.D.J.; Romeo,G.; Hoffmann,M.; Wieland,K.; Leurs,R.; Menge,W.M.; Nederkoorn,P.H.; Dean,P.M.; Timmerman,H.
参考来源:J Med Chem 2001,44(11),1666

新产品编号:2019141

Chemical Name: 1,5-Bis[4,7-bis(7-chloroquinolin-4-yl)-1,4,7-triazanonan-1-yl]pentan-1,5-dione
项目整合开发状态: Biological Testing
项目研究机构: CNRS (Originator), Tibotec-Virco (Originator)
合成路线:Condensat...
参考文献标题:Antiplasmodial activity and cytotoxicity of bis-,tris-,and tetraquinolines with linear or cyclic amino linkers
文献作者:Girault,S.; Grellier,P.; Berceibar,A.; Maes,L.; Lemi鑢e,P.; Mouray,E.; Davioud-Charvet,E.; Sergheraert,C.
参考来源:J Med Chem 2001,44(11),1658

新产品编号:2020723

Chemical Name: (16alpha,17beta)-3,17-Dihydroxyestra-1(10),2,4-triene-16-carboxylic acid 2-fluoroethyl ester
项目整合开发状态: Preclinical
项目研究机构: Yale University (Originator)
合成路线:Claisen condensatio...
参考文献标题:Estradiol-16alpha-carboxylic acid esters as locally active estrogens
文献作者:Labaree,D.C.; Reynolds,T.Y.; Hochberg,R.B.
参考来源:J Med Chem 2001,44(11),1802

新产品编号:2022305

Chemical Name: N1,N1'-(2,5-Furandiyl)bis(3-methoxy-4,1-phenylene)]bis(pyridine-2-carboxamidine)
项目整合开发状态: Biological Testing
项目研究机构: Duke University (Originator), Georgia State University (Origi...
参考文献标题:Diguanidino and " reversed" diamidino 2,5-diaryulfurans as antimicrobial agents
文献作者:Stephens,C.E.; Tanious,F.A.; Kim,S.; Wilson,W.D.; Schell,W.A.; Perfect,J.R.; Franzblau,S.G.; Boykin,D.W.
参考来源:J Med Chem 2001,44(11),1741

新产品编号:2023887

Chemical Name: N1,N1'-(2,5-Furandiyl)bis(3-methyl-4,1-phenylene)bis(5-methylpyridine-2-carboxamidine)
项目整合开发状态: Biological Testing
项目研究机构: Duke University (Originator), Georgia State University ...
参考文献标题:Diguanidino and " reversed" diamidino 2,5-diaryulfurans as antimicrobial agents
文献作者:Stephens,C.E.; Tanious,F.A.; Kim,S.; Wilson,W.D.; Schell,W.A.; Perfect,J.R.; Franzblau,S.G.; Boykin,D.W.
参考来源:J Med Chem 2001,44(11),1741

ABT-675, A-315675

Chemical Name: (-)-5(R)-[1(R)-Acetamido-2(S)-methoxy-2-methylpentyl]-4(S)-[1(Z)-propenyl]pyrrolidine-2(R)-carboxylic acid
项目整合开发状态: Preclinical
项目研究机构: Abbott (Originator)0
合成路线:The title com...
参考文献标题:Inhibitors of neuraminidases
文献作者:Sham,H.L.; Kempf,D.J.; Maring,C.J.; Klein,L.L.; Zhao,C.; Wiedeman,P.E.; Hanessian,S.; Chen,Y.; Stewart,K.D.; Yeung,M.C.; Degoey,D.A.; Grampovnik,D.J.; Wang,S.; Gu,Y.G.; Xu,Y.; (Abbott Laboratories Inc.)
参考来源:WO 0128996

新产品编号:2025469

Chemical Name: N2-(N-tert-Butoxycarbonyl)-N1-[(4aS,5R)-2-cyclohexyl-1,3-dioxoperhydropyrido[1,2-c]pyrimidin-5-yl]-L-tryptophanamide; N-[1(S)-[N-[(4aS,5R)-2-Cyclohexyl-1,3-dioxoperhydropyrido[1,2-c]pyr...
参考文献标题:5-(Tryptophyl) amino-1,3-dioxoperhydropyrido[1,2-c]pyrimidine-based potent and selective CCK1 receptor antagonists: Structure-activity relationship studies on the substituent at N2-position
文献作者:Bartolom?Nebreda,J.M.; Patino-Molina,R.; Martin-Martinez,M.; Gomez-Monterrey,I.; Garcia-Lopez,M.T.; Gonzalez-Muniz,R.; Cenarruzabeitia,E.; Latorre,M.; Del Rio,J.; Herranz,R.
参考来源:J Med Chem 2001,44(13),2219