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:1307241

Chemical Name: (1R)-1-Amino-4-(amidinio)butylboronic acid dihydrochloride; L-Boroarginine dihydrochloride
项目整合开发状态: Biological Testing
项目研究机构: CNRS (Originator)
合成路线:The hydroboration of ally...
参考文献标题:Synthesis of boronic acid analogs of L-arginine as alternate substrates or inhibitors of nitric oxide synthase
文献作者:Lebarbier,C.; Carreaux,F.; Carboni,B.; Boucher,J.L.
参考来源:Bioorg Med Chem Lett 1998,8(18),2573

新产品编号:1308823

Chemical Name: (2R,3R,4R,5R)-2,5-Di(benzyloxy)-3,4-dihydroxy-N,N'-bis[2(R)-hydroxyindan-1(S)-yl]hexanediamide
项目整合开发状态: Biological Testing
项目研究机构: Link鰌ing University (Originator), Stockholm Uni...
参考文献标题:Design and synthesis of new potent C2-symmetric HIV-1 protease inhibitors.Use of L-mannaric acid as a peptidomimetic scaffold
文献作者:Alterman,M.; Bj鰎sne,M.; M黨lman,A.; Classon,B.; Kvarnstrom,I.; Danielson,H.U.; Markgren,P.O.; Nillroth,U.; Unge,T.; Hallberg,A.; Samuelsson,B.
参考来源:J Med Chem 1998,41(20),3782

新产品编号:1310405

Chemical Name: N-Methyl-2(R)-(1-methyl-1H-tetrazol-5-ylsulfanylmethyl)-4-oxo-N-[4-(trifluoromethyl)benzyl]azetidine-1-carboxamide
项目整合开发状态: Biological Testing
项目研究机构: Bio-Mega (Originator), Boeh...
参考文献标题:Potent beta-lactam inhibitors of human cytomegalovirus protease
文献作者:Yoakim,C.; Ogilvie,W.W.; Cameron,D.R.; Chabot,C.; Grand-Maitre,C.; Guse,I.; Hache,B.; Kawai,S.; Naud,J.; O'Meara,J.A.; Plante,R.; Deziel,R.
参考来源:Antivir Chem Chemother 1998,9(5),379

新产品编号:1311987

Chemical Name: (1R,3R)-1-(2,6-Difluorophenyl)-3-methyl-3H-1,3-thiazolo[3,4-a]benzimidazole
项目整合开发状态: Biological Testing
项目研究机构: Katholieke Universiteit Leuven (Originator), Universit?degli Studi...
参考文献标题:Synthesis,structure and in vitro anti-human immunodeficiency virus activity of novel 3-methyl-1H,3H-thiazolo[3,4-a]benzimidazoles
文献作者:Chimirri,A.; Grasso,S.; Monforte,A.M.; Monforte,P.; Rao,A.; Zappala,M.; Bruno,G.; Nicolo,F.; Pannecouque,C.; Witvrouw,M.; De Clercq,E.
参考来源:Antivir Chem Chemother 1998,9(5),431

新产品编号:1313569

Chemical Name: 2(S)-Allyl-3(R)-[N-[1(S)-(1H-indol-3-ylcarbonyl)-2,2-dimethylpropyl]carbamoyl]-5-methylhexanehydroxamic acid
项目整合开发状态: Biological Testing
项目研究机构: Abbott (Originator)
合成路线:Fried...
参考文献标题:Aryl ketones as novel replacements for the C-terminal amide bond of succinyl hydroxamate MMP inhibitors
文献作者:Sheppard,G.S.; Florjancic,A.S.; Giesler,J.R.; Xu,L.; Guo,Y.; Davidsen,S.K.; Marcotte,P.A.; Elmore,I.; Albert,D.H.; Terrance,J.M.; Bouska,J.J.; Goodfellow,C.L.; Morgan,D.W.; Summers,J.B.
参考来源:Bioorg Med Chem Lett 1998,8(22),3251

新产品编号:1315151

Chemical Name: 2(S)-Allyl-3(R)-[N-[1(S)-(1H-indol-3-ylcarbonyl)-2-phenylethyl]carbamoyl]-5-methylhexanehydroxamic acid
项目整合开发状态: Biological Testing
项目研究机构: Abbott (Originator)
合成路线:Friedel Cr...
参考文献标题:Aryl ketones as novel replacements for the C-terminal amide bond of succinyl hydroxamate MMP inhibitors
文献作者:Sheppard,G.S.; Florjancic,A.S.; Giesler,J.R.; Xu,L.; Guo,Y.; Davidsen,S.K.; Marcotte,P.A.; Elmore,I.; Albert,D.H.; Terrance,J.M.; Bouska,J.J.; Goodfellow,C.L.; Morgan,D.W.; Summers,J.B.
参考来源:Bioorg Med Chem Lett 1998,8(22),3251

新产品编号:1316733

Chemical Name: 3(R)-[N-[1(S)-(1H-Indol-3-ylcarbonyl)-2-phenylethyl]carbamoyl]-5-methyl-2(S)-(4-pentenyl)hexanehydroxamic acid
项目整合开发状态: Biological Testing
项目研究机构: Abbott (Originator)
合成路线:Fri...
参考文献标题:Aryl ketones as novel replacements for the C-terminal amide bond of succinyl hydroxamate MMP inhibitors
文献作者:Sheppard,G.S.; Florjancic,A.S.; Giesler,J.R.; Xu,L.; Guo,Y.; Davidsen,S.K.; Marcotte,P.A.; Elmore,I.; Albert,D.H.; Terrance,J.M.; Bouska,J.J.; Goodfellow,C.L.; Morgan,D.W.; Summers,J.B.
参考来源:Bioorg Med Chem Lett 1998,8(22),3251

新产品编号:1318315

Chemical Name: 2(S)-Hydroxy-3(R)-[N-[1(S)-(1H-indol-3-ylcarbonyl)-2,2-dimethylpropyl]carbamoyl]-5-methylhexanehydroxamic acid
项目整合开发状态: Biological Testing
项目研究机构: Abbott (Originator)
合成路线:Fri...
参考文献标题:Aryl ketones as novel replacements for the C-terminal amide bond of succinyl hydroxamate MMP inhibitors
文献作者:Sheppard,G.S.; Florjancic,A.S.; Giesler,J.R.; Xu,L.; Guo,Y.; Davidsen,S.K.; Marcotte,P.A.; Elmore,I.; Albert,D.H.; Terrance,J.M.; Bouska,J.J.; Goodfellow,C.L.; Morgan,D.W.; Summers,J.B.
参考来源:Bioorg Med Chem Lett 1998,8(22),3251

新产品编号:1319897

Chemical Name: 2(S)-Allyl-3(R)-[N-[1(S)-benzoyl-2-phenylethyl]carbamoyl]-5-methylhexanehydroxamic acid
项目整合开发状态: Biological Testing
项目研究机构: Abbott (Originator)
合成路线:Friedel Crafts acylation o...
参考文献标题:Aryl ketones as novel replacements for the C-terminal amide bond of succinyl hydroxamate MMP inhibitors
文献作者:Sheppard,G.S.; Florjancic,A.S.; Giesler,J.R.; Xu,L.; Guo,Y.; Davidsen,S.K.; Marcotte,P.A.; Elmore,I.; Albert,D.H.; Terrance,J.M.; Bouska,J.J.; Goodfellow,C.L.; Morgan,D.W.; Summers,J.B.
参考来源:Bioorg Med Chem Lett 1998,8(22),3251

新产品编号:1321479

Chemical Name: 2(S)-Allyl-3(R)-[N-[1(S)-(1H-pyrrol-2-ylcarbonyl)-2-phenylethyl]carbamoyl]-5-methylhexanehydroxamic acid
项目整合开发状态: Biological Testing
项目研究机构: Abbott (Originator)
合成路线:Friedel C...
参考文献标题:Aryl ketones as novel replacements for the C-terminal amide bond of succinyl hydroxamate MMP inhibitors
文献作者:Sheppard,G.S.; Florjancic,A.S.; Giesler,J.R.; Xu,L.; Guo,Y.; Davidsen,S.K.; Marcotte,P.A.; Elmore,I.; Albert,D.H.; Terrance,J.M.; Bouska,J.J.; Goodfellow,C.L.; Morgan,D.W.; Summers,J.B.
参考来源:Bioorg Med Chem Lett 1998,8(22),3251