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

DRL-12035

Chemical Name: N-[3-[3-Fluoro-4-[3-(2-pyridyl)-2-propenoyl]phenyl]-2-oxooxazolidin-5(S)-ylmethyl]thiocarbamic acid O-methyl ester
项目整合开发状态: Biological Testing
项目研究机构: Dr. Reddy's Laboratories (O...
参考文献标题:Synthesis and antibacterial activity of novel chalcone oxazolidinone hybrids
文献作者:Selvakumar,N.; et al.
参考来源:42nd Intersci Conf Antimicrob Agents Chemother (Sept 27 2002,San Diego) 2002,Abst F-1323

VRC-4282

Chemical Name: N-[2-Oxo-3-[4-(6-oxo-1,6-dihydropyridazin-3-yl)phenyl]oxazolidin-5(S)-ylmethyl]thioacetamide
项目整合开发状态: Biological Testing
项目研究机构: Vicuron Pharmaceuticals (Originator)
合成路线:The ...
参考文献标题:Novel antimicrobial pyridazine phenyloxazolidinones
文献作者:Luehr,G.W.; Wang,S.; Hackbarth,C.J.; Gomez,M.; Trias,J.; Patel,D.V.; Gordeev,M.F.
参考来源:42nd Intersci Conf Antimicrob Agents Chemother (Sept 27 2002,San Diego) 2002,Abst F-1320

VRC-4189

Chemical Name: N-[2-Oxo-3-[4-(6-thioxo-1,6-dihydropyridazin-3-yl)phenyl]oxazolidin-5(S)-ylmethyl]thioacetamide
项目整合开发状态: Biological Testing
项目研究机构: Vicuron Pharmaceuticals (Originator)
合成路线:T...
参考文献标题:Novel antimicrobial pyridazine phenyloxazolidinones
文献作者:Luehr,G.W.; Wang,S.; Hackbarth,C.J.; Gomez,M.; Trias,J.; Patel,D.V.; Gordeev,M.F.
参考来源:42nd Intersci Conf Antimicrob Agents Chemother (Sept 27 2002,San Diego) 2002,Abst F-1320

VRC-4228

Chemical Name: N-[3-[4-[6-(Methylsulfanyl)pyridazin-3-yl]phenyl]-2-oxooxazolidin-5(S)-ylmethyl]thioacetamide
项目整合开发状态: Biological Testing
项目研究机构: Vicuron Pharmaceuticals (Originator)
合成路线:The...
参考文献标题:Novel antimicrobial pyridazine phenyloxazolidinones
文献作者:Luehr,G.W.; Wang,S.; Hackbarth,C.J.; Gomez,M.; Trias,J.; Patel,D.V.; Gordeev,M.F.
参考来源:42nd Intersci Conf Antimicrob Agents Chemother (Sept 27 2002,San Diego) 2002,Abst F-1320

VRC-4437

Chemical Name: N-[3-[4-[6-(Methylsulfonyl)pyridazin-3-yl]phenyl]-2-oxooxazolidin-5(S)-ylmethyl]acetamide
项目整合开发状态: Biological Testing
项目研究机构: Vicuron Pharmaceuticals (Originator)
合成路线:The rea...
参考文献标题:Novel antimicrobial pyridazine phenyloxazolidinones
文献作者:Luehr,G.W.; Wang,S.; Hackbarth,C.J.; Gomez,M.; Trias,J.; Patel,D.V.; Gordeev,M.F.
参考来源:42nd Intersci Conf Antimicrob Agents Chemother (Sept 27 2002,San Diego) 2002,Abst F-1320

新产品编号:2416223

Chemical Name: N-[2-(4'-Chlorobiphenyl-4-yl)acetyl]-L-tryptophyl-L-asparaginyl-L-aspartyl-L-threonyl-glycyl-L-ornithyl-L-aspartyl-D-alanyl-L-aspartyl-glycyl-D-seryl-threo-3-methyl-L-glutamyl-gamma-(2-...
参考文献标题:Synthesis and biological activity of novel lipophilic tails of lipopeptides
文献作者:Zhang,Y.; et al.
参考来源:42nd Intersci Conf Antimicrob Agents Chemother (Sept 27 2002,San Diego) 2002,Abst F-348

新产品编号:2417805

Chemical Name: N-[2-(2-Pyridyl)ethyl]-2-thioxo-1,2-dihydropyridine-3-carbothioamide hydrochloride
项目整合开发状态: Preclinical
项目研究机构: Universidad del Pa韘 Vasco (Originator), Universit?degli Studi di P...
参考文献标题:New N-alkyl-1,2-dihydro-2-thioxo-3-pyridinecarbothioamides as antituberculous agents with improved pharmacokinetics
文献作者:Ubiali,D.; Pagani,G.; Pregnolato,M.; Piersimoni,C.; Pedraz Mu駉z,J.L.; Rodr韌uez Gasc�? A.; Terreni,M.
参考来源:Bioorg Med Chem Lett 2002,12(18),2541

新产品编号:2419387

Chemical Name: 3-Cyclopentyl-N-[1(S)-[2,5-difluoro-4-(4-morpholinyl)benzoyl]-2,2-dimethylpropyl]-2(R)-(N-formyl-N-hydroxyaminomethyl)propionamide
项目整合开发状态: Preclinical
项目研究机构: British Biotech (O...
参考文献标题:A new series of potent PDF inhibitors displaying broad-spectrum antibacterial activity against respiratory tract infections
文献作者:Ayscough,A.; Beckett,R.P.; Brookings,D.C.; Clements,J.M.; East,S.P.; Keavey,K.; Smith,K.H.; Thomas,W.; Thompson,A.J.; Todd,R.S.
参考来源:42nd Intersci Conf Antimicrob Agents Chemother (Sept 27 2002,San Diego) 2002,Abst F-1677

O-2185

Chemical Name: 4-Pentenoic acid (1R,2R,3R,5S)-3-(3,4-dichlorophenyl)-8-oxabicyclo[3.2.1]oct-2-ylmethyl ester
项目整合开发状态: Biological Testing
项目研究机构: Organix (Originator)
合成路线:Treatment of methyl...
参考文献标题:Design and synthesis of an irreversible dopamine-sparing cocaine antagonist
文献作者:Meltzer,P.C.; Liu,S.; Blanchette,H.; Blundell,P.; Madras,B.
参考来源:Bioorg Med Chem 2002,10(11),3583

TBE-9

Chemical Name: (?-8-Methyl-3,12-dioxopodocarpa-1,9(11),13-triene-2,13-dicarbonitrile; (?-(4bbeta,8abeta,10aalpha)-4b,8,8,10a-Tetramethyl-3,7-dioxo-3,4b,7,8,8a,9,10,10a-octahydrophenanthrene-2,6-dicarb...
参考文献标题:Design and synthesis of tricyclic compounds with enone functionalities in rings A and C: A novel class of highly active inhibitors of nitric oxide production in mouse macrophages
文献作者:Favaloro,F.G.Jr.; Gribble,G.W.; Honda,T.; Honda,Y.; Risingsong,R.; Sporn,M.B.; Suh,N.
参考来源:225th ACS Natl Meet (March 23 2003,New Orleans) 2003,Abst MEDI 241