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:1897327

Chemical Name: (1R,2R,3aR,3bS,5R,8S,11S,14S,16R,18R,19aS,20aS,22S,23R,24aS,25S,25aR,29R,30aS,31S,32aR)-22-Hydroxy-23-(hydroxymethyl)-16,25-dimethyl-10,15-dimethylideneperhydro-1,5:8,11,14,18-triepoxy-...
参考文献标题:Total synthesis of halichondrin B and norhalichondrin B
文献作者:Aicher,T.D.; et al.
参考来源:J Am Chem Soc 1992,114(8),3162

新产品编号:1898909

Chemical Name: 4-[N-[8-(1,3-Benzodioxol-5-ylmethyl)-8-azabicyclo[3.2.1]oct-3endo-yl]-N-phenylamino]-N,N-diethylbenzamide
项目整合开发状态: Biological Testing
项目研究机构: R.W. Johnson (Originator)
合成路线:Th...
参考文献标题:Synthesis and binding affinities of 4-diarylaminotropanes,a new class of delta opioid agonists
文献作者:Boyd,R.E.; Carson,J.R.; Codd,E.E.; Gauthier,A.D.; Neilson,L.A.; Zhang,S.-P.
参考来源:Bioorg Med Chem Lett 2000,10(10),1109

新产品编号:1900491

Chemical Name: (-)-trans-N,N'-(1,8-Octanediyl)bis[4-(4-chlorophenyl)-1-methylpiperidine-3-carboxamide]
项目整合开发状态: Biological Testing
项目研究机构: Georgetown University (Originator), UT Medical Branch ...
参考文献标题:Monomeric and dimeric heterocycles,and therapeutic uses thereof
文献作者:Tamiz,A.P.; Araldi,G.L.; Kozikowski,A.P.(Georgetown University)
参考来源:WO 0020390

JMV-1640

Chemical Name: 3(S)-[1'-(L-Lysyl-L-arginyl)-3-(2-phenylethyl)-5-oxospiro[imidazolidin-4,4'-piperidin]-1-yl]acetyl-L-serylamino]-4-oxo-3,4-dihydro-2H-1,5-benzothiazepine-5-acetic acid
项目整合开发状态: Biol...
参考文献标题:Design and synthesis of potent bradykinin agonists containing a benzothiazepine moiety
文献作者:Amblard,M.; Daffix,I.; Bedos,P.; Berge,G.; Pruneau,D.; Paquet,J.L.; Luccarini,J.M.; Belichard,P.; Dodey,P.; Martinez,J.
参考来源:J Med Chem 1999,42(20),4185

新产品编号:1902073

Chemical Name: 3-[3-Amino-3-oxo-1(E)-propenyl]-1,1-dioxo-7-[(Z)-2-pyridylmethylene]-3-cephem-4-carboxylic acid sodium salt
项目整合开发状态: Biological Testing
项目研究机构: Southern Methodist University (Ori...
参考文献标题:The synthesis and evaluation of 3-substituted-7-(alkylidene)cephalosporin sulfones as beta-lactamase inhibitors
文献作者:Buynak,J.D.; Doppalapudi,R.; Adam,G.
参考来源:Bioorg Med Chem Lett 2000,10(9),853

新产品编号:1903655

Chemical Name: 2-Methylfuro[2,3-g]isoquinoline-4,7,9(6H)-trione
项目整合开发状态: Preclinical
项目研究机构: Universit?Claude Bernard Lyon 1 (Originator)
合成路线:The title furoisoquinoline was synthesized by r...
参考文献标题:Quinonic derivatives active against a virulent strain of Toxoplasma gondii.Synthesis of 2-methylfuro[2,3-g]- and [3,2-g]isoquinolinetriones
文献作者:Nebois,P.; Sarciron,M.E.; Bibal,B.; Bouammali,B.; Cherkaoui,O.; Pautet,F.; Petavy,A.F.; Walchshofer,N.; Fillion,H.
参考来源:Bioorg Med Chem Lett 2000,10(9),871

ALX-2226

Chemical Name: 2-(8-Chloro-2,3-dihydropyrrolo[1,2,3-de]-1,4-benzothiazin-6-yl)-1-ethanamine
项目整合开发状态: Preclinical
项目研究机构: NPS Allelix (Originator)
合成路线:Nitrosation of 7-chloro-3,4-dihydro-2H-...
参考文献标题:Pyrrolo[3,2,1-ij]quinoline derivatives,a 5-HT2c receptor agonist with selectivity over the 5-HT2a receptor: Potential therapeutic applications for epilepsy and obesity
文献作者:Isaac,M.; Slassi,A.; O'Brien,A.; Edwards,L.; MacLean,N.; Bueschkens,D.; Lee,D.K.; McCallum,K.L.; De Lannoy,I.; Demchyshyn,L.; Kamboj,R.
参考来源:Bioorg Med Chem Lett 2000,10(9),919

JMV-1802

Chemical Name: N2-[2-[3(S)-[N-[3-(4-Hydroxyphenyl)propionyl]-L-glutaminyl-L-tryptophyl-L-alanylamino]-2-oxoperhydroazepin-1-yl]acetyl]-N1-[1(S)-isobutyl-2-hydroxyheptyl]-L-histidinamide
项目整合开发状态: B...
参考文献标题:Synthesis and biological evaluation of bombesin constrained analogues
文献作者:Cristau,M.; Devin,C.; Oiry,C.; Chaloin,O.; Amblard,M.; Bernad,N.; Heitz,A.; Fehrentz,J.A.; Martinez,J.
参考来源:J Med Chem 2000,43(12),2356

KNI-1039

Chemical Name: 3'-Azido-5'-O-[2-[5-[1(S)-[4(R)-(N-tert-Butylcarbamoyl)-5,5-dimethylthiazolidin-3-ylcarbonyl]-2(S)-[2-(2,6-dimethylphenoxy)acetamido]-3-phenylpropoxy]-5-oxopentanamido]acetyl]-3'-deoxyt...
参考文献标题:"Double-drugs" - a new class of prodrug form of an HIV protease inhibitor conjugated with a reverse transcriptase inhibitor by a spontaneously cleavable linker
文献作者:Matsumoto,H.; Hamawaki,T.; Ota,H.; Kimura,T.; Goto,T.; Sano,K.; Hayashi,Y.; Kiso,Y.
参考来源:Bioorg Med Chem Lett 2000,10(11),1227

新产品编号:1905237

Chemical Name: 8(S)-(Chloromethyl)-5-formyl-4-hydroxy-2-methyl-6-[3-(4-methoxyphenyl)-2(E)-propenoyl]-3,6,7,8-tetrahydrobenzo[1,2-b:4,3-b']dipyrrole-1-carboxylic acid methyl ester
项目整合开发状态: Preclin...
参考文献标题:Synthesis and antitumor activity of duocarmycin derivatives: Modification at the C-7 position of segement-A of A-ring pyrrole compounds
文献作者:Amishiro,N.; Okamoto,A.; Okabe,M.; Saito,H.
参考来源:Bioorg Med Chem 2000,8(5),1195