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:2373509

Chemical Name: 5-[3-(Dimethylamino)propyl]-6-oxo-5,6-dihydrothieno[3',2':4,5]thieno[2,3-c]quinoline-9-carboxylic acid methyl ester hydrochloride
项目整合开发状态: Biological Testing
项目研究机构: Rudjer Bosko...
参考文献标题:Synthesis,photochemical synthesis and antitumor evaluation of novel derivatives of thieno[3',2':4,5]thieno[2,3-c]quinolones
文献作者:DoganKoruznjak,J.; Slade,N.; Zamola,B.; Pavelic,K.; Karminski-Zamola,G.
参考来源:Chem Pharm Bull 2002,50(5),656

新产品编号:2375091

Chemical Name: 4,6-Dimethyl-2H-pyrano[2,3-b]thieno[3,2-e]pyridin-2-one
项目整合开发状态: Preclinical
项目研究机构: Consiglio Nazionale delle Ricerche (Originator), Universit?degli Studi di Padova (Originator)...
参考文献标题:Synthesis,photobiological activity and photoreactivity of methyl-thieno-8-azacoumarins,novel bioisosters of psoralen
文献作者:Via,L.D.; et al.
参考来源:Bioorg Med Chem Lett 2002,12(9),1253

新产品编号:2376673

Chemical Name: 5-[2-(Diethylamino)ethylaminomethyl]-2,2-dimethyl-2H,6H-pyrano[3,2-b]xanthen-6-one hydrochloride
项目整合开发状态: Biological Testing
项目研究机构: NCSR Demokritos (Originator), University of A...
参考文献标题:Design and synthesis of some new pyranoxanthenone aminoderivatives with cytotoxic activity
文献作者:Kolokythas,G.; Kostakis,I.K.; Pouli,N.; Marakos,P.; Skaltsounis,A.L.; Pratsinis,H.
参考来源:Bioorg Med Chem Lett 2002,12(11),1443

新产品编号:2378255

Chemical Name: 1,3,6-Trichloro-5,6-dihydro-4H-cyclopenta[c]thiophen-4-one
项目整合开发状态: Preclinical
项目研究机构: Universit?de Caen (Originator)
合成路线:2,5-Dichlorothiophene-3-carbaldehyde (I) is condens...
参考文献标题:Synthesis and biological evaluation of cyclopenta[c]thiophene related compounds as new antitumor agents
文献作者:Dallemagne,P.; Khan,L.P.; Alsaidi,A.; Renault,O.; Varlet,I.; Collot,V.; Bureau,R.; Rault,S.
参考来源:Bioorg Med Chem 2002,10(7),2185

新产品编号:2379837

Chemical Name: 2-Methoxy-1-naphthaldehyde (7-methoxyquinolin-4-yl)hydrazone
项目整合开发状态: Biological Testing
项目研究机构: Universit?degli Studi di Siena (Originator)
合成路线:Reaction of 7-methoxy-4-chlor...
参考文献标题:Synthesis and anti-tubercular evaluation of 4-quinolylhydrazones
文献作者:Savini,L.; Chiasserini,L.; Gaeta,A.; Pellerano,C.
参考来源:Bioorg Med Chem 2002,10(7),2193

新产品编号:2381419

Chemical Name: N-(4-Phenylbutanoyl)-L-prolyl-L-prolyl-methanol
项目整合开发状态: Biological Testing
项目研究机构: Finncovery (Originator)
合成路线:L-Proline (I) is protected as its N-Boc derivative (II) with B...
参考文献标题:4-Phenylbutanoyl-2(S)-acylpyrrolidines and 4-phenylbutanoyl-L-prolyl-2(S)-acylpyrrolidines as prolyl oligopeptidase inhibitors
文献作者:Wall�? E.A.; Christiaans,J.A.M.; Saario,S.M.; Forsberg,M.M.; Venalainen,J.I.; Paso,H.M.; Mannisto,P.T.; Gynther,J.
参考来源:Bioorg Med Chem 2002,10(7),2199

新产品编号:2383001

Chemical Name: 10-[4-[4-(2-Hydroxyethyl)piperazin-1-yl]butyl]-2-methoxyacridin-9(10H)-one
项目整合开发状态: Biological Testing
项目研究机构: Georgetown University (Originator), St. Jude Children's Res. Hosp. ...
参考文献标题:Synthesis and chemical characterization of 2-methoxy-N10-substituted acridones needed to reverse vinblastine resistance in multidrug resistant (MDR) cancer cells
文献作者:Krishnegowda,G.; Thimmaiah,P.; Hegde,R.; Dass,C.; Houghton,P.J.; Thimmaiah,K.N.
参考来源:Bioorg Med Chem 2002,10(7),2367

新产品编号:2384583

Chemical Name: N-[2-(Dimethylamino)ethyl]-6,10-dimethyl-10H-indolo[3,2-b]quinoline-4-carboxamide
项目整合开发状态: Preclinical
项目研究机构: La Trobe University (Originator), University of Auckland (Originato...
参考文献标题:Synthesis and cytotoxic activity of N-(2-diethylamino)ethylcarboxamide and other derivatives of 10H-quindoline
文献作者:Chen,J.; Deady,L.W.; Kaye,A.J.; Finlay,G.J.; Baguley,B.C.; Denny,W.A.
参考来源:Bioorg Med Chem 2002,10(7),2381

新产品编号:2386165

Chemical Name: 4-Cyano-N-[2(R)-[4-(2,3-dihydro-1,4-benzodioxin-5-yl)piperazin-1-yl]propyl]-N-(2-pyridyl)benzamide hydrochloride
项目整合开发状态: Biological Testing
项目研究机构: Wyeth Pharmaceuticals (Origin...
参考文献标题:Serotonergic agents
文献作者:Kelly,M.G.; Childers,W.E.; Rosenzweig-Lipson,S.J.(Wyeth)
参考来源:US 2002107254; US 6469007; WO 0244142

111In-DTPA-Abeta(3-40)

Chemical Name: [N-[2-[N-[2-[N,N-Bis(carboxymethyl)amino]ethyl]-N-(carboxymethyl)amino]ethyl]-N-(carboxymethyl)glycyl-L-glutamyl-L-phenylalanyl-L-arginyl-L-histidyl-L-aspartyl-L-seryl-glycyl-L-tyrosyl-...
参考文献标题:Noninvasive imaging of peripherally injected Alzheimer's disease type synthetic A beta amyloid in vivo
文献作者:Marshall,J.R.; et al.
参考来源:Bioconjugate Chem 2002,13(2),276