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:1792915

Chemical Name: 1-[2-(Diphenylmethoxy)ethyl]-2-methyl-5-nitro-1H-imidazole nitrate
项目整合开发状态: Biological Testing
项目研究机构: Universit?degli Studi "La Sapienza" (Originator), Universit?degli Studi di ...
参考文献标题:1-[2-(Diphenylmethoxy)ethyl]-2-methyl-5-nitroimidazole: A potent lead for the design of novel NNRTIs
文献作者:Silvestri,R.; Artico,M.; Massa,S.; Marceddu,T.; De Montis,F.; La Colla,P.
参考来源:Bioorg Med Chem Lett 2000,10(3),253

新产品编号:1794497

Chemical Name: 2-(Ethylamino)-1-hexadecanol
项目整合开发状态: Biological Testing
项目研究机构: Universidad de Salamanca (Originator), Universidad de Valencia (Originator)
合成路线:N-Boc-2-Aminohexadecanoic aci...
参考文献标题:Synthesis and enzyme inhibitory activities of a series of lipidic diamine and aminoalcohol derivatives on cytosolic and secretory phospholipases A2
文献作者:Lucas,R.; Ubeda,A.; Pay? M.; Alves,M.; del Olmo,E.; L髉ez,J.L.; San Feliciano,A.
参考来源:Bioorg Med Chem Lett 2000,10(3),285

新产品编号:1796079

Chemical Name: 2-[2-(Diethylamino)ethyl]-5-methyl-2H-pyrido[3',4':5,6]thiopyrano[4,3,2-cd]indazole
项目整合开发状态: Biological Testing
项目研究机构: Novuspharma (Originator)
合成路线:Condensation of 4-chloron...
参考文献标题:Synthesis and antitumor activities of 5-methyl-1- and 2-[[2-dimethylaminoethyl]amino]-aza-thiopyranoindazoles
文献作者:Krapcho,A.P.; Haydar,S.N.; Truong-Chiott,S.; Hacker,M.P.; Menta,E.; Beggiolin,G.
参考来源:Bioorg Med Chem Lett 2000,10(3),305

新产品编号:1797661

Chemical Name: 1,1'-(Heptane-1,7-diyl)bis[4-(2-amino-4-methylthiazol-5-ylcarboxamido)-N-[2-[3-(dimethylamino)propylcarbamoyl]-1-methylpyrrol-4-yl]imidazole-2-carboxamide]
项目整合开发状态: Biological Testi...
参考文献标题:Design and synthesis of novel thiazole-containing cross-linked polyamides related to tha antiviral antibiotic distamycin
文献作者:Sharma,S.K.; Tandon,M.; Lown,J.W.
参考来源:J Org Chem 2000,65(4),1102

新产品编号:1799243

Chemical Name: 2-[2-[4-(2,4-Dichlorophenyl)-1(E),3(E)-butadienyl]phenyl]-3-methoxy-2(E)-propenoic acid methyl ester
项目整合开发状态: Preclinical
项目研究机构: Roche (Originator)
合成路线:Bromination of acryla...
参考文献标题:beta-Alkoxyacrylates against malaria
文献作者:Matile,H.; Chollet,J.; Alzeer,J.; Ridley,R.G.; Hubschwerlen,C.(F.Hoffmann-La Roche AG)
参考来源:EP 0996439; WO 9902150

新产品编号:1800825

Chemical Name: 2-(Biphenyl-4-yl)-4-methyloctahydro-2H-1,4-benzoxazin-2-ol hydrochloride
项目整合开发状态: Preclinical
项目研究机构: Aristotle University of Thessaloniki (Originator)
合成路线:The title compound...
参考文献标题:Hypocholesterolemic and hypolipidemic activity of some novel morpholine derivatives with antioxidant activity
文献作者:Chrysselis,M.C.; Rekka,E.A.; Kourounakis,P.N.
参考来源:J Med Chem 2000,43(4),609

SC-22716

Chemical Name: 1-[2-(Biphenyl-4-yloxy)ethyl]pyrrolidine
项目整合开发状态: Preclinical
项目研究机构: Pfizer (Originator)
合成路线:The title compound was prepared by alkylation of 4-phenylphenol (I) with 1-(2-ch...
参考文献标题:Structure-activity relationship studies on 1-[2-(4-phenylphenoxy)ethyl]pyrrolidine (SC-22716),a potent inhibitor of leukotriene A4 (LTA4) hydrolase
文献作者:Penning,T.D.; Chandrakumar,N.S.; Chen,B.B.; Chen,H.Y.; Desai,B.N.; Djuric,S.W.; Docter,S.H.; Gasiecki,A.F.; Haack,R.A.; Miyashiro,J.M.; Russell,M.A.; Yu,S.S.; Corley,D.G.; Durley,R.C.; Kilpatrick,B.F.; Parnas,B.L.; Askonas,L.J.; et al.
参考来源:J Med Chem 2000,43(3),721

新产品编号:1802407

Chemical Name: 2,3,7,8,9,11-Hexahydro-1H-pyrrolo[1,2-a]pyrrolo[1',2':1,2]imidazo[4,5-f]benzimidazole-5,10-dione
项目整合开发状态: Biological Testing
项目研究机构: Arizona State University (Originator)
合成路线...
参考文献标题:Inhibitors of topoisomerase II based on the benzodiimidazole and dipyrroloimidazobenzimidazole ring systems: Controlling DT-diaphorase reductive inactivation with steric bulk
文献作者:Schulz,W.G.; Skibo,E.B.
参考来源:J Med Chem 2000,43(4),629

新产品编号:1803989

Chemical Name: 1-(3,4-Dichlorobenzyl)-3,4-dihydro-1H-2,1,3-benzothiadiazin-4-one S,S-dioxide
项目整合开发状态: Biological Testing
项目研究机构: Almirall Prodesfarma (Originator), CSIC (Originator)
合成路线:Ben...
参考文献标题:Benzyl derivatives of 2,1,3-benzo- and benzothieno[3,2-a]thiadiazine 2,2-dioxides: First phosphodiesterase 7 inhibitors
文献作者:Mart韓ez,A.; Castro,A.; Gil,C.; Miralpeix,M.; Segarra,V.; Domenech,T.; Beleta,J.; Palacios,J.M.; Ryder,H.; Miro,X.; Bonet,C.; Casacuberta,J.M.; Azorin,F.; Pina,B.; Puigdomenech,P.
参考来源:J Med Chem 2000,43(4),683

新产品编号:1805571

Chemical Name: 9-[5(S)-Hydroxy-4(R)-(hydroxymethyl)-2-cyclohexen-1(S)-yl]guanine
项目整合开发状态: Biological Testing
项目研究机构: Rega Institute for Medical Research (Originator)
合成路线:Coupling of known a...
参考文献标题:The cyclohexene ring system as a furanose mimic: Synthesis and antiviral activity of both enantiomers of cyclohexenylguanine
文献作者:Wang,J.; Froeyen,M.; Hendrix,C.; Andrei,G.; Snoeck,R.; De Clercq,E.; Herdewijn,P.
参考来源:J Med Chem 2000,43(4),736