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:1425891

Chemical Name: 3-[3(R)-(4-Amidinophenyl)-2-methylisoxazolidin-5(S)-ylacetamido]-2(S)-(3-methylphenylsulfonamido)propionic acid hydrochloride
项目整合开发状态: Preclinical
项目研究机构: Bristol-Myers Squibb (O...
参考文献标题:Platelet glycoprotein IIb/IIIa receptor antagonists derived from isoxazolidines
文献作者:Confalone,P.N.; Jin,F.; Mousa,S.A.
参考来源:Bioorg Med Chem Lett 1999,9(1),55

新产品编号:1427473

Chemical Name: 1-(8-Bromobenzo[1,2-b:4,5-b']difuran-4-yl)propane-2-amine hydrochloride
项目整合开发状态: Preclinical
项目研究机构: Lilly (Originator)
合成路线:Alkylation of hydroquinone (I) with 1-bromo-2-chlo...
参考文献标题:A novel (benzodifuranyl)aminoalkane with extremely potent activity at the 5-HT2A receptor
文献作者:Parker,M.A.; Marona-Lewicka,D.; Lucaites,V.L.; Nelson,D.L.; Nichols,D.E.
参考来源:J Med Chem 1998,41(26),5148

Almuheptolide A-(+), (+)-Almuheptolide A

Chemical Name: [4R-(4alpha,5alpha,6alpha,7beta,8alpha)]-4,5-Diethoxy-6,7-dihydroxy-8-phenyloxocan-2-one
项目整合开发状态: Biological Testing
项目研究机构: Universidad de Valencia (Originator)
合成路线:(+)-Almu...
参考文献标题:Enantiospecific semisynthesis of (+)-almuheptolide-A,a novel natural heptolide inhibitor of the mammalian mitochondrial respiratory chain
文献作者:Bermejo,A.; Tormo,J.R.; Cabedo,N.; Estornell,E.; Figad閞e,B.; Cortes,D.
参考来源:J Med Chem 1998,41(26),5158

新产品编号:1429055

Chemical Name: [4R-(4alpha,5alpha,6alpha,7beta,8alpha)]-6,7-Diacetoxy-4,5-diethoxy-8-phenyloxocan-2-one
项目整合开发状态: Biological Testing
项目研究机构: Universidad de Valencia (Originator)
合成路线:(+)-Almu...
参考文献标题:Enantiospecific semisynthesis of (+)-almuheptolide-A,a novel natural heptolide inhibitor of the mammalian mitochondrial respiratory chain
文献作者:Bermejo,A.; Tormo,J.R.; Cabedo,N.; Estornell,E.; Figad閞e,B.; Cortes,D.
参考来源:J Med Chem 1998,41(26),5158

RTI-5989-29

Chemical Name: 3-(4-Hydroxyphenyl)-N-[1(S)-[4(R)-(3-hydroxyphenyl)-3(R),4-dimethylpiperidin-1-ylmethyl]-2-methylpropyl]propionamide
项目整合开发状态: Biological Testing
项目研究机构: Lilly (Originator), Natio...
参考文献标题:Identification of an opioid kappa receptor subtype-selective N-substituent for (+)-(3R,4R)-dimethyl-4-(3-hydroxyphenyl)piperidine
文献作者:Thomas,J.B.; Fall,M.J.; Cooper,J.B.; Rothman,R.B.; Mascarella,S.W.; Xu,H.; Partilla,J.S.; Dersch,C.M.; McCullough,K.B.; Cantrell,B.E.; Zimmerman,D.M.; Carroll,F.I.
参考来源:J Med Chem 1998,41(26),5188

Synadenol-(R)-(-), (R)-(-)-Synadenol

Chemical Name: (-)-(Z)-9-[2(R)-(Hydroxymethyl)cyclopropylidenemethyl]adenine
项目整合开发状态: Biological Testing
项目研究机构: University of Michigan (Originator), University of Toronto (Originator), Wayne S...
参考文献标题:(Z)- and (E)-2-((Hydroxymethyl)cyclopropylidene)methyladenine and -guanine.New nucleoside analogues with a broad-spectrum antiviral activity
文献作者:Qiu,Y.-L.; et al.
参考来源:J Med Chem 1998,41(1),10

BAS-118

Chemical Name: N-Methyl-3-[2-(2-naphthyl)acetamido]benzamide
项目整合开发状态: Preclinical
项目研究机构: Mitsubishi Chemical (Originator)
合成路线:2-Naphthylacetic acid (I) was converted to the corresponding a...
参考文献标题:Amide derivs.
文献作者:Ando,R.; Watanabe,K.; Chiba,N.; Kawamura,M.(Mitsubishi Chemical Corp.)
参考来源:EP 0887341; JP 1999071336

新产品编号:1430637

Chemical Name: 2,3-Dichloro-5,8-dimethoxy-1,4-naphthalenedione
项目整合开发状态: Biological Testing
项目研究机构: China Medical College (Originator), National Taiwan University (Originator), University of Nor...
参考文献标题:Synthesis and antiplatelet,antiinflammatory,and antiallergic activities of substituted 3-chloro-5,8-dimethoxy-1,4-naphthoquinone and related compounds
文献作者:Huang,L.-J.; Chang,F.C.; Lee,K.H.; Wang,J.P.; Teng,C.M.; Kuo,S.C.
参考来源:Bioorg Med Chem 1998,6(12),2261

新产品编号:1432219

Chemical Name: 2-Chloro-3,5,8-trimethoxy-1,4-naphthalenedione
项目整合开发状态: Biological Testing
项目研究机构: China Medical College (Originator), National Taiwan University (Originator), University of Nort...
参考文献标题:Synthesis and antiplatelet,antiinflammatory,and antiallergic activities of substituted 3-chloro-5,8-dimethoxy-1,4-naphthoquinone and related compounds
文献作者:Huang,L.-J.; Chang,F.C.; Lee,K.H.; Wang,J.P.; Teng,C.M.; Kuo,S.C.
参考来源:Bioorg Med Chem 1998,6(12),2261

新产品编号:1433801

Chemical Name: 6,7-Dichloro-5,8-dimethoxy-1,4-naphthalenedione
项目整合开发状态: Biological Testing
项目研究机构: China Medical College (Originator), National Taiwan University (Originator), University of Nor...
参考文献标题:Synthesis and antiplatelet,antiinflammatory,and antiallergic activities of substituted 3-chloro-5,8-dimethoxy-1,4-naphthoquinone and related compounds
文献作者:Huang,L.-J.; Chang,F.C.; Lee,K.H.; Wang,J.P.; Teng,C.M.; Kuo,S.C.
参考来源:Bioorg Med Chem 1998,6(12),2261