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:2084003

Chemical Name: 9(S)-Benzyl-1,13(S)-dimethyl-3,7,10,14,19-pentaoxo-12(S)-(2-phenylvinyl)-1,4,8,11,15-pentaazacyclononadecane-5(R),16(R)-dicarboxylic acid
项目整合开发状态: Biological Testing
项目研究机构: Univ...
参考文献标题:Serine-threonine protein phosphatase inhibitors derived from nodularin: Role of the 2-methyl and 3-diene groups in the Adda residue and the effect of macrocyclic conformational restraint
文献作者:O'Donnell,M.E.; et al.
参考来源:J Chem Soc - Perkins Trans I 2001,(14),1696

KPN-2001

Chemical Name: (3R,3aR,5aS,5bR,8S,9aR,10R,10aS,10bS)-3-[1(R),5-Dimethylhexyl]-8,9a-dihydroxy-3a,5b-dimethylperhydrocyclopenta[a]fluorene-10-carbaldehyde
项目整合开发状态: Biological Testing
项目研究机构: Kyus...
参考文献标题:Orostanal,a novel abeo-sterol inducing apoptosis in leukemia cell from a marine sponge,Stelletta hiwasaensis
文献作者:Miyamoto,T.; et al.
参考来源:Tetrahedron Lett 2001,42(36),6349

新产品编号:2085585

Chemical Name: 1-(2-Phenylethyl)-2-(2-propynyl)hydrazine
项目整合开发状态: Preclinical
项目研究机构: CV Technologies (Originator)
合成路线:The condensation of 2-phenylethylhydrazine (I) with propargyl bromide ...
参考文献标题:Synthesis of N-propargylphenelzine and analogues as neuroprotective agents
文献作者:Ling,L.; Urichuk,L.J.; Sloley,B.D.; Coutts,R.T.; Baker,G.B.; Shan,J.J.; Pang,P.K.T.
参考来源:Bioorg Med Chem Lett 2001,11(20),2715

MCL-118

Chemical Name: 17-(3-Iodo-2-propenyl)morphinan-3-ol
项目整合开发状态: Biological Testing
项目研究机构: Harvard Medical School (Originator), University of Rochester Medical Center (Originator)
合成路线:This com...
参考文献标题:Mixed kappa agonists and mu agonists/antagonists as potential pharmacotherapeutics for cocaine abuse: Synthesis and opioid receptor binding affinity of N-substituted derivatives of morphinan
文献作者:Neumeyer,J.L.; Gu,X.-H.; van Vliet,L.A.; DeNunzio,N.J.; Rusovici,D.E.; Cohen,D.J.; Negus,S.S.; Mello,N.K.; Bidlack,J.M.
参考来源:Bioorg Med Chem Lett 2001,11(20),2735

新产品编号:2087167

Chemical Name: N1-[3-(N-Benzyloxysulfamoyl)-1(S)-(2-phenylethyl)-2-propenyl]-N2-(morpholin-4-ylcarbonyl)-L-phenylalaninamide
项目整合开发状态: Biological Testing
项目研究机构: University of California, San Fr...
参考文献标题:Potent second generation vinyl sulfonamide inhibitors of the trypanosomal cysteine protease cruzain
文献作者:Roush,W.R.; Cheng,J.B.; Knapp-Reed,B.; Alvarez-Hernandez,A.; McKerrow,J.H.; Hansell,E.; Engel,J.C.
参考来源:Bioorg Med Chem Lett 2001,11(20),2759

(R)-Roscovitine, CYC-202

Chemical Name: 6-(Benzylamino)-2-[1(R)-(hydroxymethyl)propylamino]-9-isopropylpurine
项目整合开发状态: Phase II
项目研究机构: CNRS (Originator), Institute of Cancer Research (Originator), Cyclacel (Licensee)<...
参考文献标题:Novel purine derivs.having,in particular,antiproliferative properties,and biological uses thereof
文献作者:Meijer,L.; Bisagni,E.; Legraverend,M.(CNRS (Centre National de la Recherche Scientifique))
参考来源:EP 0874847; FR 2741881; JP 2000501408; US 2002049218; US 6316456; WO 9720842

新产品编号:2088749

Chemical Name: 9-[2-[[2(Z)-(3,4-Dimethoxy-5-oxo-2,5-dihydrofuran-2-ylidene)ethoxy](hydroxy)phosphorylmethoxy]ethyl]adenine; [2-(6-Amino-9H-purin-9-yl)ethoxy]methyl]phosphonic acid 2(Z)-(3,4-dimethoxy-...
参考文献标题:Design,synthesis,and biological evaluation of novel nucleoside and nucleotide analogues as agents against DNA viruses and/or retroviruses
文献作者:Hakimelahi,G.H.; Ly,T.W.; Moosavi-Movahedi,A.A.; Jain,M.L.; Zakerinia,M.; Davari,H.; Mei,H.C.; Sambaiah,T.; Moshfegh,A.A.; Hakimelahi,S.
参考来源:J Med Chem 2001,44(22),3710

4-Bbz-put

Chemical Name: 4-(4-Aminobutylaminomethyl)phenylboronic acid dihydrochloride
项目整合开发状态: Preclinical
项目研究机构: CNRS (Originator)
合成路线:The mono-Boc-protected diamine (II) was obtained by reaction ...
参考文献标题:N'-Benzylpolyamines as vectors of boron and fluorine for cancer therapy and imaging: Synthesis and biological evaluation
文献作者:Martin,B.; Posseme,F.; Le Barbier,C.; Carreaux,F.; Carboni,B.; Seiler,N.; Moulinoux,J.P.; Delcros,J.G.
参考来源:J Med Chem 2001,44(22),3653

OP-1030

Chemical Name: 4-[4-(2-Methoxyphenyl)piperazin-1-yl]-N,N-dimethyl-2,2-diphenylbutyramide hydrochloride
项目整合开发状态: Preclinical
项目研究机构: SSP (Originator)
合成路线:The target disubstituted piperazine ...
参考文献标题:New mu-opioid receptor agonists with piperazine moiety
文献作者:Komoto,T.; Okada,T.; Sato,S.; Niino,Y.; Oka,T.; Sakamoto,T.
参考来源:Chem Pharm Bull 2001,49(10),1314

新产品编号:2090331

Chemical Name: N-[2-[2-(4-Butylphenylsulfonyl)-1,2,3,4-tetrahydroisoquinolin-1-yl]ethyl]pyridine-3-carboxamide
项目整合开发状态: Preclinical
项目研究机构: AstraZeneca (Originator), Organon (Originator)
合成路...
参考文献标题:Parallel synthesis and biological activity of a new class of high affinity and selective delta-opioid ligand
文献作者:Barn,D.R.; Caulfield,W.L.; Cottney,J.; McGurk,K.; Morphy,J.R.; Rankovic,Z.; Roberts,B.
参考来源:Bioorg Med Chem 2001,9(10),2609