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:2446281

Chemical Name: trans,trans-4'-[4-[1-O-Butyl-2-[3(R)-[butyl(hydroxy)phosphoryloxy]octanamido]-3-O-[3(R)-[butyl(hydroxy)phosphoryloxy]octanoyl]-4-O-(phosphono)-2-deoxy-beta-D-glucopyranos-6-O-ylcarbonyl...
参考文献标题:Active immunization with a glycolipid transition state analogue protects against endotoxic shock
文献作者:Jones,L.H.; Altobell,L.J.III; MacDonald,M.T.; Boyle,N.A.; Wentworth,P.Jr.; Lerner,R.A.; Janda,K.D.
参考来源:Angew Chem.Int Ed Engl 2002,41(22),4241

新产品编号:2447863

Chemical Name: Succinic acid 3,4-bis[(3R,5aS,6R,8aS,9R,10R,12R,12aR)-3,6,9-trimethylperhydro-3,12-epoxy[1,2]dioxepino[4,3-i]-2-benzopyran-10-ylmethyl]isobutyl monoester
项目整合开发状态: Preclinical
项目研...
参考文献标题:Orally active,antimalarial,anticancer,artemisinin-derived trioxane dimers with high stability and efficacy
文献作者:Posner,G.H.; Paik,I.-P.; Sur,S.; McRiner,A.J.; Borstnik,K.; Xie,S.; Shapiro,T.A.
参考来源:J Med Chem 2003,46(6),1060

新产品编号:2449445

Chemical Name: N,N'-(Octane-1,8-diyl)bis[6-[N-ethyl-N-(2-methoxybenzyl)amino]-N-methylhexanamide] dioxalate
项目整合开发状态: Biological Testing
项目研究机构: Universit?degli Studi di Bologna (Originator), Un...
参考文献标题:Structure-activity relationships of acetylcholinesterase noncovalent inhibitors based on a polyamine backbone.2.Role of the substituents on the phenyl ring and nitrogen atoms of caproctamine
文献作者:Tumiatti,V.; Rosini,M.; Bartolini,M.; Cavalli,A.; Marucci,G.; Andrisano,V.; Angeli,P.; Banzi,R.; Minarini,A.; Recanatini,M.; Melchiorre,C.
参考来源:J Med Chem 2003,46(6),954

ST-1926

Chemical Name: 3-[3'-(1-Adamantyl)-4'-hydroxybiphenyl-4-yl]-2(E)-propenoic acid
项目整合开发状态: Preclinical
项目研究机构: Sigma-Tau (Originator)
合成路线:Friedel-Crafts condensation of 4'-bromobiphenyl-4-ol ...
参考文献标题:Retinoid derivs.with antiangiogenic,antitumoral and proapoptotic activities
文献作者:Penco,S.; Merlini,L.; Giannini,G.; Vesci,L.; Pisano,C.; Dallavalle,S.(Sigma-Tau Industrie Farmaceutiche Riunite SpA)
参考来源:WO 0311808

新产品编号:2451027

Chemical Name: N4-[2-(4-Phenoxyphenyl)ethyl]quinazoline-4,6-diamine
项目整合开发状态: Preclinical
项目研究机构: Japan Energy (Originator)
合成路线:Chlorination of 6-nitro-4-quinazolone (I) in refluxing SOCl2 a...
参考文献标题:Discovery of quinazolines as a novel structural class of potent inhibitors of NF-kappaB activation
文献作者:Tobe,M.; Isobe,Y.; Tomizawa,H.; Nagasaki,T.; Takahashi,H.; Fukazawa,T.; Hayashi,H.
参考来源:Bioorg Med Chem 2003,11(3),383

新产品编号:2452609

Chemical Name: N,N-Dimethyl-N-[2-(6-nitro-2-oxo-3,7-dihydro[1,2,6]thiadiazino[3,4,5-kl]acridin-3-yl)ethyl]amine maleate
项目整合开发状态: Preclinical
项目研究机构: Medical University of Gdansk (Originator), P...
参考文献标题:Rational design,synthesis and biological evaluation of thiadiazinoacridines: A new class of antitumor agents
文献作者:Antonini,I.; Polucci,P.; Magnano,A.; Cacciamani,D.; Konieczny,M.T.; Paradziej-Lukowicz,J.; Martelli,S.
参考来源:Bioorg Med Chem 2003,11(3),399

新产品编号:2454191

Chemical Name: 4-[1-(4-Fluorophenyl)-2-methyl-5-phenyl-1H-pyrrol-3-ylmethyl]thiomorpholine
项目整合开发状态: Biological Testing
项目研究机构: Universit?degli Studi "La Sapienza" (Originator), Universit?degli ...
参考文献标题:Importance of the thiomorpholine introduction in new pyrrole derivatives as antimycobacterial agents analogues of BM 212
文献作者:Biava,M.; Porretta,G.C.; Deidda,D.; Pompei,R.; Tafi,A.; Manetti,F.
参考来源:Bioorg Med Chem 2003,11(4),515

新产品编号:2455773

Chemical Name: 2-[2-(Dimethylamino)ethyl]-6-[2-(dimethylamino)ethylamino]-8,11-dihydroxy-3,7-dihydro-2H-dibenzo[de,h]cinnoline-3,7-dione
项目整合开发状态: Preclinical
项目研究机构: Universit?degli Studi di Ca...
参考文献标题:Synthesis and biological evaluation of 2,7-dihydro-3H-dibenzo[de,h]cinnoline-3,7-dione derivatives,a novel group of anticancer agents active on a multidrug resistant cell line
文献作者:Stefanska,B.; Arciemiuk,M.; Bontemps-Gracz,M.M.; Dzieduszycka,M.; Kupiec,A.; Martelli,S.; Borowski,E.
参考来源:Bioorg Med Chem 2003,11(4),561

LaaMII

Chemical Name: N-(2-Aminododecanoyl)-glycyl-L-cysteinyl-L-cysteinyl-L-seryl-L-asparaginyl-L-prolyl-L-valyl-L-cysteinyl-L-histidyl-L-leucyl-L-glutamyl-L-histidyl-L-seryl-L-asparaginyl-L-leucyl-L-cystei...
参考文献标题:Synthesis,structure elucidation,in vitro biological activity,toxicity,and caco-2 cell permeability of lipophilic analogues of alpha-conotoxin MII
文献作者:Blanchfield,J.T.; Dutton,J.L.; Hogg,R.C.; Gallagher,O.P.; Craik,D.J.; Jones,A.; Adams,D.J.; Lewis,R.J..; Alewood,P.F.; Toth,I.
参考来源:J Med Chem 2003,46(7),1266

SB-691673

Chemical Name: 2-[2-[4-(5-Fluoro-2-oxo-2,3-dihydro-1H-benzimidazol-1-yl)piperidin-1-yl]ethyl]-2,3,4,5-tetrahydro-1H-2-benzazepin-1-one
项目整合开发状态: Biological Testing
项目研究机构: GlaxoSmithKline (Origi...
参考文献标题:Identification of a novel series of selective 5-HT7 receptor antagonists
文献作者:Forbes,I.T.; Cooper,D.G.; Dodds,E.K.; Douglas,S.E.; Gribble,A.D.; Ife,R.J.; Lightfoot,A.P.; Meeson,M.; Campbell,L.P.; Coleman,T.; Riley,G.J.; Thomas,D.R.
参考来源:Bioorg Med Chem Lett 2003,13(6),1055