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

L-838417

Chemical Name: 7-tert-Butyl-3-(2,5-difluorophenyl)-6-(1-methyl-1H-1,2,4-triazol-5-ylmethoxy)[1,2,4]triazolo[4,3-b]pyridazine
项目整合开发状态: Preclinical
项目研究机构: Merck Sharp & Dohme (Originator)
合成路...
参考文献标题:Substd.triazolo-pyridazine derivs.as ligands for GABA receptors
文献作者:Madin,A.; Castro Pineiro,J.L.; Carling,W.R.; Street,L.J.; Russell,M.G.; Moore,K.W.; Guiblin,A.R.; Broughton,H.B.(Merck Sharp & Dohme Ltd.)
参考来源:EP 0915875; WO 9804559

新产品编号:1906819

Chemical Name: N-[1(R)-(Hydroxymethyl)-2-oxo-2-(8-oxo-1-oxaspiro[2.5]octa-4,6-dien-5-ylamino)ethyl]decanamide
项目整合开发状态: Biological Testing
项目研究机构: Universit鋞 Karlsruhe (Originator)
合成路线:Coupl...
参考文献标题:Synthesis of the first selective irreversible inhibitor of neutral sphingomyelinase
文献作者:Giannis,A.; Arenz,C.
参考来源:Angew Chem.Int Ed Engl 2000,39(8),1440

FY3-alphaalpha09

Chemical Name: N2-Decanoyl-N5-[trans-2-(2,5-diphenyloxazol-4-ylcarboxamido)cyclohexyl]-DL-glutamine
项目整合开发状态: Biological Testing
项目研究机构: University of Pittsburgh (Originator)
合成路线:D,L-Glutami...
参考文献标题:Identification of new Cdc25 dual specificity phosphatase inhibitors in a targeted small molecule array
文献作者:Yokokama,S.; Ducruet,A.P.; Rice,R.L.; Tamura,K.; Yokokawa,F.; Wipf,P.; Lazo,J.S.
参考来源:Bioorg Med Chem 2000,8(6),1451

PNU-181128

Chemical Name: N-(4-Chlorobenzyl)-4-hydroxy-6-(3-hydroxy-1-propynyl)quinoline-3-carboxamide
项目整合开发状态: Biological Testing
项目研究机构: Pfizer (Originator)
合成路线:The condensation of 2-fluoroaniline (...
参考文献标题:4-Hydroxyquinoline-3-carboxamides and hydrazides as antiviral agents
文献作者:Schnute,M.E.; Turner,S.R.; Cudahy,M.M.; Vaillancourt,V.A.; Thaisrivongs,S.; Strohbach,J.W.; Romines,K.R.; Tucker,J.A.(Pharmacia Corp.)
参考来源:EP 1042295; US 6093732; WO 9932450

AWD-12-343

Chemical Name: N-(3,5-Dichloropyridin-4-yl)-2-[5-fluoro-1-(4-fluorobenzyl)-1H-indol-3-yl]-2-oxoacetamide
项目整合开发状态: Preclinical
项目研究机构: Asta Medica (Originator)
合成路线:Alkylation of 5-fluoroindo...
参考文献标题:AWD 12-343,a new orally active PDE 4 inhibitor - Synthesis and comparison with SB 207499,rolipram and AWD 12-281
文献作者:H鰂gen,N.; et al.
参考来源:27th Natl Med Chem Symp (June 13 2000,Kansas City) 2000,Abst B-19

NO-Paracetamol, NCX-701

Chemical Name: 4-(Nitrooxy)butyric acid 4-acetamidophenyl ester
项目整合开发状态: Phase II
项目研究机构: NicOx (Originator)
合成路线:The esterification of paracetamol (I) with 4-bromobutyric acid (II) by means...
参考文献标题:Pharmaceutical cpds.
文献作者:Del Soldato,P.(NicOx SA)
参考来源:EP 1252133; WO 0112584

新产品编号:1908401

Chemical Name: (8aR,11S,14S,17R,20aS,20bR)-14,17-Dibenzyl-11-(1H-indol-3-ylmethyl)-5,8a,10,11,13,14,16,17,18,19,20a,20b-dodecahydro-6H-[1,4,7,10]tetraazacyclotetradecino[12',13':4,5]isoxazolo[3,2-a]is...
参考文献标题:Regio- and stereoselective cycloadditions of cyclic nitrones to maleic diamide forced in a peptide: Synthesis of potent ligands of human NK-2 receptor
文献作者:Valenza,S.; Cordero,F.M.; Brandi,A.; Guidi,A.; Altamura,M.; Giolitti,A.; Giuntini,F.; Pasqui,F.; Renzetti,A.R.; Maggi,C.A.
参考来源:J Org Chem 2000,65(13),4003

新产品编号:1909983

Chemical Name: (+)-2,2-Dimethylpropionic acid 4-[2,5-dioxomorpholin-3(S)-ylmethyl]-2-hydroxyphenylester
项目整合开发状态: Preclinical
项目研究机构: Universit?degli Studi di Camerino (Originator), Universit?de...
参考文献标题:Synthesis of L-(+)-3-(3-hydroxy-4-pivaloyloxybenzyl)-2,5-diketomorpholine as potential prodrug of L-Dopa
文献作者:Gingolani,G.M.; Di Stefano,A.; Mosciatti,B.; Napolitani,F.; Giorgioni,G.; Ricciutelli,M.; Claudi,F.
参考来源:Bioorg Med Chem Lett 2000,10(12),1385

新产品编号:1911565

Chemical Name: (1S,5R,6S)-6-[1(R)-Hydroxyethyl]-2-methoxy-1-methyl-1-carba-2-penem-3-carboxylic acid potassium salt
项目整合开发状态: Biological Testing
项目研究机构: Ludwig-Maximilians-Univ. M黱chen (Originat...
参考文献标题:Synthesis and biological activities of an alpha-methyl and a beta-methyl carbapenem and the corresponding unsubstituted compound
文献作者:Pfaendler,H.R.; Weishaupt,R.; Meffert,H.
参考来源:Bioorg Med Chem Lett 2000,10(12),1389

新产品编号:1913147

Chemical Name: (1R,5S,6S)-6-[1(R)-Hydroxyethyl]-1-methyl-2-[5(S)-(1-methyl-1H-tetrazol-5-ylsulfanylmethyl)pyrrolidin-3(S)-ylsulfanyl]-1-carba-2-penem-3-carboxylic acid
项目整合开发状态: Preclinical
项目研究...
参考文献标题:Synthesis and biological properties of new 1beta-methylcarbapenems having tetrazolothioether moiety
文献作者:Shin,K.J.; Koo,K.D.; Yoo,K.H.; Kim,C.; Kim,D.J.; Park,S.W.
参考来源:Bioorg Med Chem Lett 2000,10(13),1421