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:1987501

Chemical Name: 2-[4-[2-(4,5-Dihydroxy-10-oxo-9,10-dihydroanthracen-9-yl)-2-oxoethyl]phenyl]-N-methylacetohydroxamic acid
项目整合开发状态: Biological Testing
项目研究机构: Teva (Originator)
合成路线:Acylation ...
参考文献标题:10-Substd.18-dihydroxy-9(10H)anthracenone pharmaceuticals
文献作者:Reindl,H.; Muller,K.; Weigrebe,W.(Teva Pharmaceutical Industries Ltd.)
参考来源:US 5952390

新产品编号:1989083

Chemical Name: 4-(1H-Imidazol-1-ylmethyl)-1-nitro-9H-xanthen-9-one
项目整合开发状态: Biological Testing
项目研究机构: Universit?degli Studi di Bologna (Originator), Universit鋞 des Saarlandes (Originator)
合...
参考文献标题:A new class of nonsteroidal aromatase inhibitors: Design and synthesis of chromone and xanthone derivatives and inhibition of the P450 enzymes aromatase and 17 alpha-hydroxylase/C17,20-lyase
文献作者:Recanatini,M.; Bisi,A.; Cavalli,A.; Belluti,F.; Gobbi,S.; Rampa,A.; Valenti,P.; Palzer,M.; Palusczak,A.; Hartmann,R.W.
参考来源:J Med Chem 2001,44(5),672

新产品编号:1990665

Chemical Name: 2-Cyano-2-(3-methyl-3H-imidazo[4,5-b]pyridin-2-yl)-N-(4-methylphenyl)thioacetamide
项目整合开发状态: Biological Testing
项目研究机构: Medical University of Gdansk (Originator)
合成路线:The title...
参考文献标题:Some reactions of 2-cyanomethyl-3-methyl-3H-imidazo[4,5-b]pyridine with isothiocyanates.Antituberculotic activity of the obtained compounds
文献作者:Bukowski,L.
参考来源:Pharmazie 2001,56(1),23

新产品编号:1992247

Chemical Name: N-(2-Furylmethyl)-N'-(2-thiazolyl)thiourea
项目整合开发状态: Biological Testing
项目研究机构: Parker Hughes Institute (Originator)
合成路线:Reaction of 2-aminothiazole (I) with thiocarbonyldiimi...
参考文献标题:Aromatic and heterocyclic thiazolyl thiourea cpds.and use
文献作者:Uckun,F.M.; Venkatachalam,T.K.(Parker Hughes Institute)
参考来源:WO 0232889

新产品编号:1993829

Chemical Name: N-[2-(4-Chlorophenyl)ethyl]-6-nitro-7-(1-piperazinyl)quinazolin-4-amine
项目整合开发状态: Biological Testing
项目研究机构: Japan Energy (Originator)
合成路线:Nitration of quinazolone (I) by reac...
参考文献标题:Structure-activity relationships of quinazoline derivatives: Dual-acting compounds with inhibitory activities toward both TNF-alpha production and T cell proliferation
文献作者:Tobe,M.; Isobe,Y.; Tomizawa,H.; Matsumoto,M.; Obara,F.; Nagasaki,T.; Hayashi,H.
参考来源:Bioorg Med Chem Lett 2001,11(4),545

新产品编号:1995411

Chemical Name: 4,5-Dimethoxy-2-(3,4,5-trimethoxybenzamido)benzoic acid ethyl ester
项目整合开发状态: Biological Testing
项目研究机构: Japan Energy (Originator)
合成路线:Treatment of 4,5-dimethoxy-2-nitro benzo...
参考文献标题:Synthesis and structure-activity relationship of diarylamide derivatives as selective inhibitors of the proliferation of human coronary artery smooth muscle cells
文献作者:Ogita,H.; Isobe,Y.; Takaku,H.; Sekine,R.; Goto,Y.; Misawa,S.; Hayashi,H.
参考来源:Bioorg Med Chem Lett 2001,11(4),549

UK-356618

Chemical Name: 2(R)-[3-(2-Methylbiphenyl-4-yl)propyl]-N1-[2,2-dimethyl-1(S)-[N-[1(R)-phenylethyl]carbamoyl]propyl]-N4-hydroxysuccinamide
项目整合开发状态: Biological Testing
项目研究机构: Pfizer (Originator)<...
参考文献标题:Discovery of potent and selective succinyl hydroxamate inhibitors of matrix metalloprotease-3 (stromelysin-1)
文献作者:Fray,M.J.; Dickinson,R.P.
参考来源:Bioorg Med Chem Lett 2001,11(4),571

DTPA-M2

Chemical Name: 2-[N,N-Bis[2-[N-[5-(aminosulfonyl)-1,3,4-thiadiazol-2-ylcarbamoylmethyl]-N-(carboxymethyl)amino]ethyl]amino]acetic acid
项目整合开发状态: Preclinical
项目研究机构: Universit?degli Studi di Fire...
参考文献标题:Carbonic anhydrase inhibitors: Synthesis of sulfonamides incorporating DTPA tails and of their zinc complexes with powerful topical antiglaucoma properties
文献作者:Scozzafava,A.; Menabuoni,L.; Muncione,F.; Mincione,G.; Supuran,C.T.
参考来源:Bioorg Med Chem Lett 2001,11(4),575

新产品编号:1996993

Chemical Name: (-)-(4aR,10bR)-1-(4-Hydroxybenzoyl)-5,5-dimethyl-1,2,3,4a,5,10b-hexahydro[1]benzopyrano[3,4-b][1,4]oxazine-9-carbonitrile
项目整合开发状态: Preclinical
项目研究机构: National Taiwan University ...
参考文献标题:N-acyl-1,2,3,4a,5,10b-hexahydro-[1]benzopyrano-[3,4-b][1,4]oxazine-9-carbonitriles as bladder-selective potassium channel openers
文献作者:Chiu,H.-I.; Lin,Y.-C.; Cheng,C.-Y.; Tsai,M.-C.; Yu,H.-C.
参考来源:Bioorg Med Chem 2001,9(2),383

新产品编号:1998575

Chemical Name: 1-(5-Fluorobenzothien-2-yl)-3-[4-(2-methoxyphenyl)piperazin-1-yl]propan-1-ol
项目整合开发状态: Biological Testing
项目研究机构: Universidad de Navarra (Originator), Vita (Originator)
合成路线:Fr...
参考文献标题:New 3-[4-(aryl)piperazin-1-yl]-1-(benzo[b]thiophen-3-yl)propane derivatives with dual action at 5-HT1A serotonin receptors and serotonin transporter as a new class of antidepressants
文献作者:Mart韓ez,J.; Perez,S.; Oficialdegui,A.M.; Heras,B.; Orus,L.; Villanueva,H.; Palop,J.A.; Roca,J.; Mourelle,M.; Bosch,A.; Del Castillo,J.C.; Lasheras,B.; Tordera,R.; del Rio,J.; Monge,A.
参考来源:Eur J Med Chem 2001,36(1),55