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:1549287

Chemical Name: [2R,4R,5S(E)]-1-[4,5-Bis(hydroxymethyl)tetrahydrothien-2-yl]-5-(2-bromovinyl)pyrimidine-2,4(1H,3H)-dione; [2R,4R,5S(E)]-1-[4,5-Bis(hydroxymethyl)tetrahydrothien-2-yl]-5-(2-bromovinyl)ur...
参考文献标题:Efficacy of new 5-nitroimidazoles against metronidazole-susceptible and -resistant Giardia,Trichomonas,and Entamoeba spp
文献作者:Upcroft,P.; Campbell,R.W.; Benakli,K.; Upcroft,J.A.; Vanelle,P.
参考来源:Antimicrob Agents Chemother 1999,43(1),73

新产品编号:1550869

Chemical Name: 3-[2-Bromo-4-(isopropyl)phenyl]-7-(diethylamino)-5-methylthiazolo[4,5-d]pyrimidine-2(3H)-thione
项目整合开发状态: Biological Testing
项目研究机构: Bristol-Myers Squibb (Originator)
合成路线:Anil...
参考文献标题:Thiazolo[4,5-d]pyrimidine thiones and -ones as corticotropin-releasing hormone (CRH-R1) receptor antagonists
文献作者:Beck,J.P.; Curry,M.A.; Chorvat,R.J.; Fitzgerald,L.W.; Gilligan,P.J.; Zaczek,R.; Trainor,G.L.
参考来源:Bioorg Med Chem Lett 1999,9(8),1185

新产品编号:1552451

Chemical Name: [2aR,4S,4aS,6R,9S(alphaR,betaS),11S,12S,12aR,12bS]-beta-(Benzoylamino)-alpha-hydroxybenzenepropanoic acid 6,12b-bis(acetoxy)-4-[3-[2-[3H]-3-(benzoyl)phenyl]propanoyloxy]-12-(benzoyloxy)...
参考文献标题:New photoaffinity analogs of paclitaxel
文献作者:Ojima,I.; Bounaud,P.-Y.; Ahern,D.G.
参考来源:Bioorg Med Chem Lett 1999,9(8),1189

新产品编号:1554033

Chemical Name: [2aR,4S,4aS,6R,9S(alphaR,betaS),11S,12S,12aR,12bS]-beta-(Benzoylamino)-alpha-hydroxybenzenepropanoic acid 12b-(acetoxy)-12-(benzoyloxy)-6-[2-[3H]-3-[3-(benzoyl)phenyl]propanoyloxy]-2a,3...
参考文献标题:New photoaffinity analogs of paclitaxel
文献作者:Ojima,I.; Bounaud,P.-Y.; Ahern,D.G.
参考来源:Bioorg Med Chem Lett 1999,9(8),1189

新产品编号:1555615

Chemical Name: N-[3beta-Hydroxylup-20(29)-en-28-oyl]-L-alanine
项目整合开发状态: Biological Testing
项目研究机构: University of Illinois (Originator)
合成路线:Title compound was obtained by condensation of bet...
参考文献标题:Preparation of amino acid conjugates of betulinic acid with activity against human melanoma
文献作者:Jeong,H.-J.; Chai,H.B.; Park,S.Y.; Kim,D.S.
参考来源:Bioorg Med Chem Lett 1999,9(8),1201

AR-H040922, H-409/22

Chemical Name: Nalpha-(2,2-Diphenylacetyl)-N1-[1(R)-(4-hydroxyphenyl)ethyl]-D-argininamide
项目整合开发状态: Phase II
项目研究机构: AstraZeneca (Originator)
合成路线:The protected (R)-ornithine (I) was convert...
参考文献标题:New NPY antagonists
文献作者:Pilling,G.; Bergman,N.-A.; D'Ambra,T.(AstraZeneca plc)
参考来源:EP 1017672; WO 9915498

GGTI-2151

Chemical Name: N-[4-(1H-Imidazol-4-ylmethylaminomethyl)-2-(1-naphthyl)benzoyl]-L-leucine
项目整合开发状态: Preclinical
项目研究机构: University of Pittsburgh (Originator), University of South Florida (Origina...
参考文献标题:Potent,highly selective,and non-thiol inhibitors of protein geranylgeranyltransferase-I
文献作者:Vasudevan,A.; Qian,Y.; Vogt,A.; Blaskovich,M.A.; Ohkanda,J.; Sebti,S.M.; Hamilton,A.D.
参考来源:J Med Chem 1999,42(8),1333

新产品编号:1557197

Chemical Name: N-[1-[1-(Carbamoyl)cyclopentyl]-2-oxopyrrolidin-3(R)-yl]-L-prolylamide
项目整合开发状态: Preclinical
项目研究机构: McMaster University (Originator), University of Minnesota (Originator)
合成路线...
参考文献标题:Synthesis and dopamine receptor modulating activity of novel peptidomimetics of L-prolyl-L-leucyl-glycinamide featuring alpha,alpha-disubstituted amino acids
文献作者:Evans,M.C.; Pradhan,A.; Venkatraman,S.; Ojala,W.H.; Gleason,W.B.; Mishra,R.K.; Johnson,R.L.
参考来源:J Med Chem 1999,42(8),1441

新产品编号:1558779

Chemical Name: (1S,2S)-1-(3-Hydroxy-4-methoxyphenyl)-2-(3,4,5-trimethoxyphenyl)ethane-1,2-diol
项目整合开发状态: Biological Testing
项目研究机构: Arizona State University (Originator), National Cancer Institu...
参考文献标题:Antineoplastic agents.291.Isolation and synthesis of combretastatins A-4,A-5,and A-6
文献作者:Pettit,G.R.; Singh,S.B.; Boyd,M.R.; Hamel,E.; Pettit,R.K.; Schmidt,J.M.; Hogan,F.
参考来源:J Med Chem 1995,38(10),1666

新产品编号:1560361

Chemical Name: L-Prolyl-L-leucyl-2,2-(diethyl)glycinamide
项目整合开发状态: Preclinical
项目研究机构: McMaster University (Originator), University of Minnesota (Originator)
合成路线:This compound has been obta...
参考文献标题:Synthesis and dopamine receptor modulating activity of novel peptidomimetics of L-prolyl-L-leucyl-glycinamide featuring alpha,alpha-disubstituted amino acids
文献作者:Evans,M.C.; Pradhan,A.; Venkatraman,S.; Ojala,W.H.; Gleason,W.B.; Mishra,R.K.; Johnson,R.L.
参考来源:J Med Chem 1999,42(8),1441