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:2109315

Chemical Name: 8-Methyl-3exo-(4-methylphenyl)-8-azabicyclo[3.2.1]octane-2exo-carboxylic acid 3-fluoropropyl ester
项目整合开发状态: Biological Testing
项目研究机构: McLean Hospital (Originator), Natural Pharm...
参考文献标题:Synthesis and biological evaluation of a series of novel N- or O-fluoroalkyl derivatives of tropane: Potential positron emission tomography (PET) imaging agents for the dopamine transporter
文献作者:Gu,X.-H.; Zong,R.; Kula,N.S.; Baldessarini,R.J.; Neumeyer,J.L.
参考来源:Bioorg Med Chem Lett 2001,11(23),3049

新产品编号:2110897

Chemical Name: 3exo-(4-Iodophenyl)-8-methyl-8-azabicyclo[3.2.1]octane-2exo-carboxylic acid 3-fluoropropyl ester
项目整合开发状态: Biological Testing
项目研究机构: McLean Hospital (Originator), Natural Pharmac...
参考文献标题:Synthesis and biological evaluation of a series of novel N- or O-fluoroalkyl derivatives of tropane: Potential positron emission tomography (PET) imaging agents for the dopamine transporter
文献作者:Gu,X.-H.; Zong,R.; Kula,N.S.; Baldessarini,R.J.; Neumeyer,J.L.
参考来源:Bioorg Med Chem Lett 2001,11(23),3049

新产品编号:2112479

Chemical Name: 3exo-(4-Iodophenyl)-8-methyl-8-azabicyclo[3.2.1]octane-2exo-carboxylic acid 2-fluoroethyl ester
项目整合开发状态: Biological Testing
项目研究机构: McLean Hospital (Originator), Natural Pharmaci...
参考文献标题:Synthesis and biological evaluation of a series of novel N- or O-fluoroalkyl derivatives of tropane: Potential positron emission tomography (PET) imaging agents for the dopamine transporter
文献作者:Gu,X.-H.; Zong,R.; Kula,N.S.; Baldessarini,R.J.; Neumeyer,J.L.
参考来源:Bioorg Med Chem Lett 2001,11(23),3049

新产品编号:2114061

Chemical Name: (3beta,5alpha)-3-[N-[3,3-Bis(3-carboxy-5-chloro-4-methoxyphenyl)propenoyl]-N-[6,6-bis(3-carboxy-5-chloro-4-methoxyphenyl)-5-hexenyl]amino]cholestane
项目整合开发状态: Biological Testing
项...
参考文献标题:Synthesis and anti-HIV activity of cosalane analogues incorporating two dichlorodisalicylmethane pharmacophore fragments
文献作者:Casimiro-Garcia,A.; De clercq,E.; Pannecouque,C.; Witvrouw,M.; Loftus,T.L.; Turpin,J.A.; Buckheit,R.W.Jr.; Fanwick,P.E.; Cushman,M.
参考来源:Bioorg Med Chem 2001,9(11),2827

新产品编号:2115643

Chemical Name: 6-(1-Naphthylsulfanylmethyl)pyrido[2,3-d]pyrimidine-2,4-diamine
项目整合开发状态: Biological Testing
项目研究机构: Duquesne University (Originator), Indiana University (Originator)
合成路线:Pyri...
参考文献标题:Synthesis of 2,4-diamino-6-(thioarylmethyl)pyrido [2,3-d]pyrimidines as dihydrofolate reductase inhibitors
文献作者:Gangjee,A.; Adair,O.; Queener,S.F.
参考来源:Bioorg Med Chem 2001,9(11),2929

新产品编号:2117225

Chemical Name: 3-[1-[3-(1-Methyl-7-oxo-3-propyl-6,7-dihydro-1H-pyrazolo[4,3-d]pyrimidin-5-yl)-4-propoxyphenylsulfonyl]piperidin-4-yl]propionic acid
项目整合开发状态: Biological Testing
项目研究机构: SK Chemic...
参考文献标题:Synthesis and phosphodiesterase inhibitory activity of new sildenafil analogues containing a carboxylic acid group in the 5'-sulfonamide moiety of a phenyl ring
文献作者:Kim,D.-K.; Lee,J.Y.; Lee,N.; Ryu,D.H.; Kim,J.S.; Lee,S.; Choi,J.Y.; Ryu,J.H.; Kim,N.H.; Im,G.J.; Choi,W.S.; Kim,T.K.
参考来源:Bioorg Med Chem 2001,9(11),3013

新产品编号:2118807

Chemical Name: 2-(3-Methylphenyl)-3-[4-(methylsulfonyl)phenyl]imidazo[1,2-a]pyridine
项目整合开发状态: Biological Testing
项目研究机构: Salvat (Originator)
合成路线:The Friedel-Crafts condensation of 2-[4-(met...
参考文献标题:Diarylimidazo[1,2-a]pyridine derivatives as a new class of selective COX-2 inhibitors
文献作者:Farrerons,C.; et al.
参考来源:11th RSC-SCI Med Chem Symp (Sept 9 2001,Cambridge) 2001,Abst P2

CHF-4227

Chemical Name: 3-(4-Methoxyphenyl)-4-[4-[2-(1-piperidinyl)ethoxy]benzyl]-2H-1-benzopyran-7-ol hydrochloride
项目整合开发状态: Phase I
项目研究机构: Chiesi (Originator)
合成路线:The title compound is synthesize...
参考文献标题:2H-1-Benzopyran derivs.,processes for their preparation and pharmaceutical compsns.thereof
文献作者:Delcanale,M.; Civelli,M.; Armani,E.; Amari,G.; Galbiati,E.(Chiesi Farmaceutici SpA)
参考来源:EP 1229036; EP 1281710; EP 1355906; WO 0259113

FS-32

Chemical Name: N,N-Dimethyl-N-[3-(5-methyl-3-phenyl-1H-indazol-1-yl)propyl]amine
项目整合开发状态: Biological Testing
项目研究机构: National Tsing Hua University (Originator)
合成路线:Alkylation of N,N-dimethy...
参考文献标题:An expedient synthesis of 1-[3-(dimethylamino)propyl]-5-methyl-3-phenyl-1H-indazole (FS-32) - An antidepressant
文献作者:Yeu,J.P.; et al.
参考来源:Synthesis 2001,(12),1775

新产品编号:2120389

Chemical Name: N-[4-(Dimethylamino)butyl]-4-iodobenzamide
项目整合开发状态: Preclinical
项目研究机构: INSERM (Originator), Univ. Blaise Pascal-Clermont-Ferrand II (Originator)
合成路线:Alkylation of the lithiu...
参考文献标题:Structure-activity relationships and optimisation of the selective MDR modulator 2-(3,4-dimethoxyphenyl)-5-(9-fluorenylamino)-2-(methylethyl) pentanenitrile and its N-methyl derivative
文献作者:Dei,S.; Teodori,E.; Garnier-Suillerot,A.; Gualtieri,F.; Scapecchi,S.; Budriesi,R.; Chiarini,A.
参考来源:Bioorg Med Chem 2001,9(10),2673