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

CVS-2589

Chemical Name: N-Isobutoxy-D-seryl-L-alanine 1-amidino-2-hydroxypiperidin-3(S)-ylamide
项目整合开发状态: Preclinical
项目研究机构: Corvas (Originator)
合成路线:The title compound has been prepared by either so...
参考文献标题:Synthesis and biological activity of transition-state urokinase inhibitors
文献作者:Cohen,C.R.; Weinhouse,M.I.; Roberts,C.; et al.
参考来源:217th ACS Natl Meet (March 21 1999,Anaheim) 1999,Abst MEDI 090

CVS-3083

Chemical Name: N-[2-(Phenyl)ethylsulfonyl]-D-seryl-L-alanine N-[1-carbamimidoyl-2-hydroxypiperidin-3(S)-yl]amide
项目整合开发状态: Preclinical
项目研究机构: Corvas (Originator)
合成路线:The title compound has ...
参考文献标题:Synthesis and biological activity of transition-state urokinase inhibitors
文献作者:Cohen,C.R.; Weinhouse,M.I.; Roberts,C.; et al.
参考来源:217th ACS Natl Meet (March 21 1999,Anaheim) 1999,Abst MEDI 090

PD-151307

Chemical Name: Perhydroazepin-1-ylcarbonyl-L-leucyl-4-O-(benzyl)-L-tyrosine tert-butyl ester
项目整合开发状态: Biological Testing
项目研究机构: Neurex (Originator), Pfizer (Originator)
合成路线:By condensation...
参考文献标题:Peptidyl calcium channel blockers
文献作者:Roth,B.D.; Connor,D.T.; Malone,T.C.; Hamilton,H.W.; Rafferty,M.F.; Hu,L.-Y.; Cody,W.L.; He,J.X.; Nadasdi,L.; Brogley,L.; Urge,L.; Silva,D.F.; Song,Y.; Szoke,B.G.; Booth,R.J.; Lescosky,J.(Neurex Corp.; Pfizer Inc.)
参考来源:US 6423689

新产品编号:1522393

Chemical Name: N-[6-Methyl-1-(3-methylbutyl)piperidin-2-ylcarbonyl]-4-O-(benzyl)-L-tyrosine tert-butyl ester
项目整合开发状态: Biological Testing
项目研究机构: Elan (Originator), Pfizer (Originator)
合成路线:H...
参考文献标题:Synthesis and biological evaluation of substituted 4-(OBz)phenylalanine derivatives as novel N-type calcium channel blockers
文献作者:Hu,L.Y.; Ryder,T.R.; Nikam,S.S.; Millerman,E.; Szoke,B.G.; Rafferty,M.F.
参考来源:Bioorg Med Chem Lett 1999,9(8),1121

DDE-236, D-PBT, HI-236

Chemical Name: N-[2-[2,5-Bis(methoxy)phenyl]ethyl]-N'-(5-bromo-2-pyridinyl)thiourea
项目整合开发状态: Preclinical
项目研究机构: Parker Hughes Institute (Originator)
合成路线:2-Amino-5-bromopyridine (I) was con...
参考文献标题:NNI for treatment of multi-drug resistant HIV
文献作者:Uckun,F.M.(Parker Hughes Institute)
参考来源:WO 0056736

HI-241

Chemical Name: N-(5-Bromo-2-pyridinyl)-N'-[2-(3-fluorophenyl)ethyl]thiourea
项目整合开发状态: Biological Testing
项目研究机构: Parker Hughes Institute (Originator)
合成路线:2-Amino-5-bromopyridine (I) was cond...
参考文献标题:Rational design and synthesis of phenethyl-5-bromopyridyl thiourea derivatives as potent non-nucleoside inhibitors of HIV reverse transcriptase
文献作者:Vig,R.; Mao,C.; Venkatachalam,T.K.; Tuel-Ahlgren,L.; Sudbeck,E.A.; Uckun,F.M.
参考来源:Bioorg Med Chem 1998,6(10),1789

[18F]-FEtNTI

Chemical Name: 17-(Cyclopropylmethyl)-4,5alpha-epoxy-1'-(2-[18F]-fluoromethyl)-3,14-dihydroxy-6,7-didehydroindolo[2',3':6,7]morphinan; N1'-([18F]-Fluoroethyl)naltrindole
项目整合开发状态: Preclinical
项目...
参考文献标题:Synthesis of N1?([F-18]fluoroethyl)naltrindole ([F-18]FEtNTI): A radioligand for positron emission tomographic studies of delta opioid receptors
文献作者:Mathews,W.B.; et al.
参考来源:J Label Compd Radiopharm 1999,42(1),43

Phthalascidin, Pt-650

Chemical Name: (6aS,7R,13S,14S,16R)-5-Acetoxy-14-cyano-8-hydroxy-9-methoxy-4,10,17-trimethyl-16-(N-phthalimidomethyl)-6a,7,12,13,14,16-hexahydro-6H-7,13-imino-1,3-dioxolo[4',5':7,8]isoquino[3,2-b][3]b...
参考文献标题:Synthesis of ecteinascidin ET-743 and phathalascidin Pt-650 from cyanosafracin B
文献作者:Cuevas,C.; P閞ez,M.; Mart�? M.J.; Chicharro,J.L.; Fernandez-Rivas,C.; Flores,M.; Francesch,A.; Gallego,P.; Zarzuelo,M.; de La Calle,F.; Garcia,J.; Polanco,C.; Rodriguez,I.; Manzanares,I.
参考来源:Org Lett 2000,2(16),2545

新产品编号:1523975

Chemical Name: 2-(3,4-Dihydroxyphenyl)acetic acid (2R,3S,5R)-3-carboxy-2-methyl-1,1-dioxo-6-[(Z)-pyridin-2-ylmethylene]penam-2-ylmethyl ester sodium salt; (2S,3R,5R)-3-[2-(3,4-Dihydroxyphenyl)acetoxym...
参考文献标题:New beta-lactamase inhibitors of the class A and class C enzymes
文献作者:Buynak,J.D.; et al.
参考来源:217th ACS Natl Meet (March 21 1999,Anaheim) 1999,Abst MEDI 194

6,7-Dimethylesculetin, Scoparone

Chemical Name: 6,7-(Dimethoxy)-2H-1-benzopyran-2-one
项目整合开发状态: Not Determined
项目研究机构: Sigma-Aldrich (Supplier)
合成路线:Hydroquinone (I) is converted to 1,2,4-triacetoxybenzene (II),which is cond...
参考文献标题:
文献作者:DuH,S.B.; Parihar,D.B.
参考来源:Proc Ind Acad Sci 1947,106(19,Suppl.2),153