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

202W92, BW-202W92

Chemical Name: (-)-6-(Fluoromethyl)-5-(2,3,5-trichlorophenyl)pyrimidine-2,4-diamine
项目整合开发状态: Preclinical
项目研究机构: GlaxoSmithKline (Originator)
合成路线:Treatment of thiourea (I) with iodomethane ...
参考文献标题:Pharmacologically active CNS cpds.
文献作者:Miller,A.A.; Nobbs,M.S.; Hyde,R.M.; Leach,M.J.(Glaxo Wellcome plc)
参考来源:AU 8945964; EP 0372934; EP 0713703; EP 0715851; EP 0727212; EP 0727213; EP 0727214; JP 1990202876; US 5587380; US 5597828; US 5635507; US 5684005

F-12342

Chemical Name: exo-8-Benzyl-3-(7,8-dimethoxyphthalazin-1-ylamino)-8-azabicyclo[3.2.1]octane; exo-N-(8-Benzyl-8-azabicyclo[3.2.1]octan-3-yl)-N-(7,8-dimethoxyphthalazin-1-yl)amine
项目整合开发状态: Preclinic...
参考文献标题:Novel phthalazine derivatives with high dopamine D
文献作者:Prinssen,E.P.M.; Schambel,P.; Monse,B.M.; Koek,W.; Kleven,M.S.; Assi? M.-B.; Diard,C.; Imbert,T.
参考来源:15th European Federation for Medicinal Chemistry International Symposium on Medicinal Chemistry (Sept 6 1998,Edinburgh) 1998,Abst P.167

F-12985

Chemical Name: exo-8-Benzyl-3-(7,8-dimethoxyphthalazin-1-yloxy)-8-azabicyclo[3.2.1]octane; exo-1-(8-Benzyl-8-azabicyclo[3.2.1]octan-3-yloxy)-7,8-dimethoxyphthalazine
项目整合开发状态: Preclinical
项目研究机构...
参考文献标题:Novel phthalazine derivatives with high dopamine D
文献作者:Prinssen,E.P.M.; Schambel,P.; Monse,B.M.; Koek,W.; Kleven,M.S.; Assi? M.-B.; Diard,C.; Imbert,T.
参考来源:15th European Federation for Medicinal Chemistry International Symposium on Medicinal Chemistry (Sept 6 1998,Edinburgh) 1998,Abst P.167

新产品编号:1277183

Chemical Name: 2-Methoxy-5-[5(S)-(3,4,5-trimethoxyphenyl)-1,3-dioxolan-4(S)-yl]phenol
项目整合开发状态: Biological Testing
项目研究机构: University of Tokyo (Originator)
合成路线:The Wittig condensation of ben...
参考文献标题:Asymmetric synthesis of antimitotic combretadioxolane with potent antitumor activity against multi-drug resistant cells
文献作者:Shirai,R.; Takayama,H.; Nishikawa,A.; Koiso,Y.; Hashimoto,Y.
参考来源:Bioorg Med Chem Lett 1998,8(15),1997

新产品编号:1278765

Chemical Name: (Z)-4-(4-Phenyl-1-butenyl)-1H-imidazole fumarate
项目整合开发状态: Preclinical
项目研究机构: Bioprojet (Originator)
合成路线:The Wittig condensation of 1-tritylimidazole-4-carbaldehyde (I) with ...
参考文献标题:General construction pattern of histamine H3-receptor antagonists: Change of a paradigm
文献作者:Stark,H.; Ligneau,X.; Arrang,J.-M.; Schwartz,J.-C.; Schunack,W.
参考来源:Bioorg Med Chem Lett 1998,8(15),2011

FUB-349(free base), VUF-5514

Chemical Name: 4-(4-Phenylbutyl)-1H-imidazole fumarate
项目整合开发状态: Preclinical
项目研究机构: Bioprojet (Originator)
合成路线:The Wittig condensation of 1-tritylimidazole-4-carbaldehyde (I) with triphenyl...
参考文献标题:General construction pattern of histamine H3-receptor antagonists: Change of a paradigm
文献作者:Stark,H.; Ligneau,X.; Arrang,J.-M.; Schwartz,J.-C.; Schunack,W.
参考来源:Bioorg Med Chem Lett 1998,8(15),2011

新产品编号:1280347

Chemical Name: 2-[2-(4-Fluorophenyl)benzofuran-3-yl]-N,N-dihexylacetamide
项目整合开发状态: Preclinical
项目研究机构: Georgetown University (Originator)
合成路线:O-Phenylhydroxylamine hydrochloride (II) (prepa...
参考文献标题:Synthesis and pharmacological evaluation of benzofuran-acetamides as "antineophobic" mitochondrial DBI receptor complex ligands
文献作者:Liao,Y.; Kozikowski,A.P.; Guidotti,A.; Costa,E.
参考来源:Bioorg Med Chem Lett 1998,8(16),2099

新产品编号:1281929

Chemical Name: N,N-Dihexyl-2-(2-phenylbenzofuran-3-yl)acetamide
项目整合开发状态: Preclinical
项目研究机构: Georgetown University (Originator)
合成路线:O-Phenylhydroxylamine hydrochloride (II) (prepared from p...
参考文献标题:Synthesis and pharmacological evaluation of benzofuran-acetamides as "antineophobic" mitochondrial DBI receptor complex ligands
文献作者:Liao,Y.; Kozikowski,A.P.; Guidotti,A.; Costa,E.
参考来源:Bioorg Med Chem Lett 1998,8(16),2099

新产品编号:1283511

Chemical Name: N-(5-Bromo-2-pyridyl)-N'-[2-(1-piperidinyl)ethyl]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:Condensation of 2-amino-5-bromopyridine...
参考文献标题:Structure-based design of N-[2-(1-piperidinylethyl)]-N'-[2-(5-bromopyridyl)]-thiourea and N-[2-(1-piperazinylethyl)]-N'-[2-(5-bromopyridyl)]-thiourea as potent non-nucleoside inhibitors of HIV-1 reverse transcriptase
文献作者:Mao,C.; Vig,R.; Venkatachalam,T.K.; Sudbeck,E.A.; Uckun,F.M.
参考来源:Bioorg Med Chem Lett 1998,8(16),2213

新产品编号:1285093

Chemical Name: N-(5-bromo-2-pyridinyl)-N'-[2-(1-piperazinyl)ethyl]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:Condensation of 2-amino-5-bromopyridi...
参考文献标题:Structure-based design of N-[2-(1-piperidinylethyl)]-N'-[2-(5-bromopyridyl)]-thiourea and N-[2-(1-piperazinylethyl)]-N'-[2-(5-bromopyridyl)]-thiourea as potent non-nucleoside inhibitors of HIV-1 reverse transcriptase
文献作者:Mao,C.; Vig,R.; Venkatachalam,T.K.; Sudbeck,E.A.; Uckun,F.M.
参考来源:Bioorg Med Chem Lett 1998,8(16),2213