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:1962189

Chemical Name: (3S,4R,5R,6S)-2,7-Bis[4-(hydroxymethyl)benzyl]-3,6-bis(phenoxymethyl)hexahydro-1,2,7-thiadiazepine-4,5-diol 1,1-dioxide
项目整合开发状态: Biological Testing
项目研究机构: Medivir (Originator) 参考文献标题:Inhibitors of the C2-symmetric HIV-1 protease: Nonsymmetric binding of a symmetric cyclic sulfamide with ketoxime groups in the P2/P2' side chains
文献作者:Hult�? J.; Andersson,H.O.; Schaal,W.; Danielson,H.U.; Classon,B.; Kvarnstrom,I.; Karlen,A.; Unge,T.; Samuelsson,B.; Hallberg,A.
参考来源:J Med Chem 1999,42(20),4054

VUF-5472

Chemical Name: trans-4-Hydroxy-N-(3-phenyl-1,2,4-thiadiazol-5-yl)cyclohexanecarboxamide
项目整合开发状态: Biological Testing
项目研究机构: Universiteit Leiden (Originator), Vrije Universiteit (Originator)
...
参考文献标题:Thiazole and thiadiazole analogues as a novel class of adenosine receptor antagonists
文献作者:van Muijlwijk-Koezen,J.E.; Timmerman,H.; Vollina,R.C.; von Drabbe K黱zel,J.F.; de Groote,M.; Visser,S.; Ijzerman,A.P.
参考来源:J Med Chem 2001,44(5),749

新产品编号:1963771

Chemical Name: 1-(3-Chlorophenyl)-4-[1-[4'-(trifluoromethyl)biphenyl-4-ylmethyl]-1H-imidazol-5-ylmethyl]piperazin-2-one
项目整合开发状态: Preclinical
项目研究机构: Merck & Co. (Originator)
合成路线:3-Chloroan...
参考文献标题:Biaryl inhibitors of prenyl-protein transferase
文献作者:Williams,T.M.(Merck & Co.,Inc.)
参考来源:WO 0075135

VN-2142

Chemical Name: 1-(2-Methoxyphenyl)-4-[3-(1-naphthyloxy)-3-(3-thienyl)propyl]piperazine hydrochloride
项目整合开发状态: Preclinical
项目研究机构: Universidad de Navarra (Originator), Vita (Originator)
合成路线:...
参考文献标题:Cpds.derived from thiophene and benzothiophene,and related utilisation and compsn.
文献作者:Bosch Rovira,A.; Roca Acin,J.; Monge Vega,A.; Del Rio Zambrana,J.; Palop Cubillo,J.A.; Lasheras Aldaz,B.; Del Castillo Nieto,J.C.(Laboratorios Vita,SA)
参考来源:EP 1008594; ES 2128266; JP 2002511883; US 6262056; WO 9902516

新产品编号:1965353

Chemical Name: N'-(Pyrrolo[1,2-a]quinoxalin-4-yl)pyrazine-2-carbohydrazide
项目整合开发状态: Preclinical
项目研究机构: Ist. di Ricerche Farmacol. Mario Negri (Originator)
合成路线:Clauson-Kaas reaction between...
参考文献标题:Novel and highly potent 5-HT3 receptor agonists based on a pyrroloquinoxaline structure
文献作者:Campiani,G.; Cappelli,A.; Nacci,V.; Anzini,M.; Vomero,S.; Hamon,M.; Cagnotto,A.; Fracasso,C.; Uboldi,C.; Caccia,S.; Consolo,S.; Mennini,T.
参考来源:J Med Chem 1997,40(22),3670

新产品编号:1966935

Chemical Name: 2(R)-(1H-Imidazol-1-yl)-3-(octadecyloxy)propyl (1R,2R,3S,4R,5S,6R)-2,3,4,6-tetrahydroxy-5-(hydroxymethyl)cyclohexyl hydrogen phosphate
项目整合开发状态: Biological Testing
项目研究机构: Arizona...
参考文献标题:3-Deoxy-3-substituted-D-myo-inositol imidazolyl ether lipid phosphates and carbonate as inhibitors of the phosphatidylinositol 3-kinase pathway and cancer cell growth
文献作者:Hu,Y.; Meuillet,E.J.; Berggren,M.; Powis,G.; Kozikowski,A.P.
参考来源:Bioorg Med Chem Lett 2001,11(2),173

新产品编号:1968517

Chemical Name: N-[3-Methyl-1(S)-[N-[4-oxotetrahydrofuran-3(S)-yl]carbamoyl]butyl]benzothiophene-2-carboxamide; N2-(Benzothien-2-ylcarbonyl)-N1-[4-oxotetrahydrofuran-3(S)-yl]-L-leucinamide
项目整合开发状态:...
参考文献标题:Diastereoselective synthesis,activity and chiral stability of cyclic alkoxyketone inhibitors of cathepsin K
文献作者:Fenwick,A.E.; Gribble,A.D.; Ife,R.J.; Stevens,N.; Witherington,J.
参考来源:Bioorg Med Chem Lett 2001,11(2),199

新产品编号:1970099

Chemical Name: N-Acetyl-L-tyrosyl-N1-[1(S)-benzyl-2(R)-hydroxy-3-[8(S)-isopropyl-7,10-dioxo-2-oxa-6,9-diazabicyclo[11.2.2]heptadeca-1(15),13,16-trien-11(S)-ylamino]-3-oxopropyl]-L-valinamide
项目整合开发...
参考文献标题:Design,synthesis,and biological evaluation of HIV/FIV protease inhibitors incorporating a conformationally constrained macrocycle with a small P3' residue
文献作者:Mak,C.C.; Le,V.-D.; Lin,Y.-C.; Elder,J.H.; Wong,C.-H.
参考来源:Bioorg Med Chem Lett 2001,11(2),219

501516, GW-516, GW-501516

Chemical Name: 2-[2-Methyl-4-[4-methyl-2-[4-(trifluoromethyl)phenyl]thiazol-5-ylmethylsulfanyl]phenoxy]acetic acid
项目整合开发状态: Phase II
项目研究机构: GlaxoSmithKline (Originator), Ligand (Codevelopment)...
参考文献标题:Thiazole and oxazole derivs.and their pharmaceutical use
文献作者:Maloney,P.R.; Gellibert,F.J.; Sierra,M.L.; Chao,E.Y.-H.; Haffner,C.D.; Willson,T.M.; Sznaidman,M.L.; Xu,H.E.; Lambert,M.H.III; Sternbach,D.D.(Glaxo Group Ltd.)
参考来源:WO 0100603

新产品编号:1971681

Chemical Name: 2-(4-Benzyl-3-oxo-3,4-dihydroquinoxalin-2-ylmethoxy)-N-phenylbenzamide
项目整合开发状态: Biological Testing
项目研究机构: University of Pennsylvania (Originator)
合成路线:3-Methylquinoxalin-2-on...
参考文献标题:Structure-activity studies of substituted quinoxalinones as multiple-drug-resistance antagonists
文献作者:Lawrence,D.S.; Copper,J.E.; Smith,C.D.
参考来源:J Med Chem 2001,44(4),594