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

LM-1669

Chemical Name: 2-(3-Benzoyl-5-ethylphenyl)ethenesulfonamide
项目整合开发状态: Biological Testing
项目研究机构: Menarini (Originator)
合成路线:An alternative method for the preparation of the precursor 3-bromo-...
参考文献标题:Trisubstd.benzenes linked to amides,esters and carboxylic acids as new cyclooxygenase II inhibitors
文献作者:Palomer Benet,A.; Maule�?Casellas,D.; Garc�?P閞ez,M.L.; Pascual Avellana,J.
参考来源:ES 2164564

新产品编号:2313393

Chemical Name: 2-[N-[4-(Carboxymethoxy)benzoyl]glycyl-L-valyl-L-prolyl-L-valyl]benzoxazole
项目整合开发状态: Preclinical
项目研究机构: Dainippon Pharmaceutical (Originator)
合成路线:N-Cbz-L-Valinal cyanohydrin...
参考文献标题:Design and synthesis of peptide-based carboxylic acid-containing transition-state inhibitors of human neutrophil elastase
文献作者:Sato,F.; Inoue,Y.; Omodani,T.; Imano,K.; Okazaki,H.; Takemura,T.; Komiya,M.
参考来源:Bioorg Med Chem Lett 2002,12(4),551

ProVP-16II

Chemical Name: [5R-[5alpha,5abeta,8aalpha,9beta(R*)]]-5-[4-(2,3-Dihydroxypropoxycarbonyloxy)-3,5-dimethoxyphenyl]-9-(4,6-O-ethylidene-beta-D-glucopyranosyloxy)-5,5a,6,8,8a,9-hexahydro-2H-furo[3',4':6,...
参考文献标题:Synthesis,hydrolytic activation and cytotoxicity of etoposide prodrugs
文献作者:Wrasidlo,W.; Schroder,U.; Bernt,K.; Hubener,N.; Shabat,D.; Gaedicke,G.; Lode,H.
参考来源:Bioorg Med Chem Lett 2002,12(4),557

新产品编号:2314975

Chemical Name: 3-[2-(6,7-Dimethoxy-1,2,3,4-tetrahydroisoquinolin-2-yl)ethyl]-2-[4-(dimethylamino)phenyl]quinazolin-4(3H)-one
项目整合开发状态: Biological Testing
项目研究机构: Xenova (Originator)
合成路线:The ...
参考文献标题:Studies on quinazolinones as dual inhibitors of Pgp and MRP1 in multidrug resistance
文献作者:Wang,S.; Ryder,H.; Pretswell,I.; Depledge,P.; Milton,J.; Hancox,T.C.; Dale,I.; Dangerfield,W.; Charlton,P.; Faint,R.; Dodd,R.; Hassan,S.
参考来源:Bioorg Med Chem Lett 2002,12(4),571

FAUC-327

Chemical Name: 3-[4-(4-Chlorophenyl)piperazin-1-ylmethyl]pyrazolo[1,5-a]pyridine-7-carbonitrile
项目整合开发状态: Preclinical
项目研究机构: Friedrich-Alexander-Universit鋞 (Originator)
合成路线:Lithiation of 8-...
参考文献标题:Di- and trisubstituted pyrazolo[1,5-a]pyridine derivatives: Synthesis,dopamine receptor binding and ligand efficacy
文献作者:L鯾er,S.; Aboul-Fadl,T.; H黚ner,H.; Gmeiner,P.
参考来源:Bioorg Med Chem Lett 2002,12(4),633

新产品编号:2316557

Chemical Name: N-[1-(Diethylaminomethyl)pentadecyl]carbamic acid tert-butyl ester
项目整合开发状态: Biological Testing
项目研究机构: Univ. Nacl. Asunci髇 (Originator), Universidad de Salamanca (Originator)
...
参考文献标题:Leishmanicidal activity of some aliphatic diamines and amino-alcohols
文献作者:del Olmo,E.; Alves,M.; L髉ez,J.L.; Inchaustti,A.; Yaluff,G.; Rojas de Arias,A.; San Feliciano,A.
参考来源:Bioorg Med Chem Lett 2002,12(4),659

新产品编号:2318139

Chemical Name: N-[4-[1(R,S)-(2,4-Diaminofuro[2,3-d]pyrimidin-5-ylmethyl)propyl]benzoyl]-L-glutamic acid
项目整合开发状态: Biological Testing
项目研究机构: Duquesne University (Originator), Roswell Park Cancer...
参考文献标题:Synthesis of N-[4-[ethyl-2-(2,4-diaminofuro[2,3-d]pyrimidin-5-yl)ethyl]benzoyl]-L-glutamic acid as an antifolate
文献作者:Gangjee,A.; Zeng,Y.; Mcguire,J.J.; Kisliuk,R.L.
参考来源:J Med Chem 2002,45(9),1942

新产品编号:2319721

Chemical Name: Benzoic acid [(3S,6Z,7S,8S,8aR)-6-(3-chloro-4-iodobenzylidene)perhydro-3,7-methanoindolizin-8-yl]methyl ester
项目整合开发状态: Biological Testing
项目研究机构: Georgetown University (Originato...
参考文献标题:Further studies on conformationally constrained tricyclic tropane analogues and their uptake inhibition at monoamine transporter sites: Synthesis of (Z)-9-(substituted arylmethylene)-7-azatricyclo[4.3.1.0(3,7)]decanes as a novel class of serotonin transpo
文献作者:Zhang,M.; Zhou,G.; Hoepping,A.; Mukhopadhyaya,J.; Johnson,K.M.; Zhang,A.; Kozilowski,A.P.
参考来源:J Med Chem 2002,45(9),1930

新产品编号:2321303

Chemical Name: N1,N4-Bis[3-oxo-3-(9H-purin-6-ylsulfanylmethoxy)propyl]-N2-[2-(polyethyleneglycol)ethoxycarbonyl]-L-asparaginamide
项目整合开发状态: Preclinical
项目研究机构: Enzon (Originator)
合成路线:Treatme...
参考文献标题:PEG prodrugs of 6-mercaptopurine (6-MP) - I: Synthesis and in vitro studies
文献作者:Choe,Y.H.; et al.
参考来源:Proc Am Assoc Cancer Res 2002,43

DD-612

Chemical Name: N-[2-(1-Pyrrolidinyl)ethyl]-glycyl-N-cyclopropyl-glycyl-N2-(1-methylpropyl)glycinamide
项目整合开发状态: Preclinical
项目研究机构: DiverDrugs (Originator), Advancell (Licensee)
合成路线:The tit...
参考文献标题:N-Alkylglycine trimeres capable of protecting neurons against excitotoxic aggressions and compsns.containing said trimeres
文献作者:Felipo Orts,V.; Montoliu Felix,C.; Ferrer Montiel,A.; Planells Cases,R.; Merino Fernandez,J.M.; Perez Paya,E.; Sanchez Baeza,F.; Humet,M.; Messeguer Peypoch,A.(DiverDrugs SL)
参考来源:WO 0228885