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:1343627

Chemical Name: 4-[2-[4-[3-[4-(2-Methoxyphenyl)piperazin-1-yl]-1-(4-methylphenyl)propoxy]benzamido]phenoxy]butanoic acid
项目整合开发状态: Biological Testing
项目研究机构: Zeria (Originator)
合成路线:Reduction ...
参考文献标题:Synthesis of benzanilide derivatives as dual actin
文献作者:Yoshida,K.; Horikoshi,Y.; Eta,M.; Chikazawa,J.; Ogishima,M.; Fukuda,Y.; Sato,H.
参考来源:Bioorg Med Chem Lett 1998,8(21),2967

新产品编号:1345209

Chemical Name: [5S-(5alpha,6beta,11beta,12alpha)]-5-(Benzoyloxy)-4,6-dihydroxy-12-(2-hydroxyethoxy)-9,13,13-trimethyl-11-(phenylsulfanyl)-5,6,7,8,11,12-hexahydro-6,10-methanobenzocyclodecen-8-one
项...
参考文献标题:Synthesis of C-ring aromatic taxoids and evaluation of their multi-drug resistance reversing activity
文献作者:Morihira,K.; Nishimori,T.; Kusama,H.; Horiguchi,Y.; Kuwajima,I.; Tsuruo,T.
参考来源:Bioorg Med Chem Lett 1998,8(21),2973

新产品编号:1346791

Chemical Name: N-Isopropylcarbamic acid 5,10-dioxo-5,10-dihydropyrido[3,2-g]quinolin-3-ylmethyl ester
项目整合开发状态: Biological Testing
项目研究机构: Chungbuk National University (Originator), Konkuk Univ...
参考文献标题:Synthesis and in vitro cytotoxicity of 3-substituted-1,8-diazaanthraquinones produced by Lewis-acid catalyzed hetero Diels-Alder reaction
文献作者:Lee,H.; Lee,S.I.; Yang,S.I.
参考来源:Bioorg Med Chem Lett 1998,8(21),2991

新产品编号:1348373

Chemical Name: 3-[4-[4-[4-[3-(7-Methoxy-5-oxo-2,3,5,11a(S)-tetrahydro-1H-pyrrolo[2,1-c][1,4]benzodiazepin-8-yloxy)propionamido]-1-methylpyrrole-2-carboxamido]-1-methylpyrrole-2-carboxamido]-1-methylpy...
参考文献标题:Design,synthesis and biological activity of a pyrrolo[2,1-c][1,4]benzodiazepine (PBD)-distamycin hybrid
文献作者:Baraldi,P.G.; Cacciari,B.; Guiotto,A.; Leoni,A.; Romagnoli,R.; Spalluto,G.; Mongelli,N.; Howard,P.W.; Thurston,D.E.; Bianchi,N.; Gambari,R.
参考来源:Bioorg Med Chem Lett 1998,8(21),3019

新产品编号:1349955

Chemical Name: 20-(Acetoxyimino)-4,16-pregnadien-3-one
项目整合开发状态: Biological Testing
项目研究机构: University of Maryland (Originator)
合成路线:Title compound was obtained by Oppenauer oxidation of 3-be...
参考文献标题:Synthesis and in vitro activity of some epimeric 20alpha-hydroxy,20-oxime and aziridine pregnene derivatives as inhibitors of human 17alpha-hydroxylase/C17,20-lyase and 5alpha-reductase
文献作者:Ling,Y.-Z.; Li,J.S.; Kato,K.; Liu,Y.; Wang,X.; Klus,G.T.; Marat,K.; Nnane,I.P.; Brodie,A.M.
参考来源:Bioorg Med Chem 1998,6(10),1683

新产品编号:1351537

Chemical Name: N-[2-[2-[N-[1(S)-(Carboxymethyl)pentyl]carbamoyl]phenyldisulfanyl]benzoyl]-1a- homo-L-norleucine; N,N'-Disulfanediylbis(1,2-phenylene)biscarbonylbis(1a-homo-L-norleucine)
项目整合开发状态: B...
参考文献标题:2,2'-Dithiobisbenzamides derived from alpha-,beta- and gamma-amino acids possessing anti-HIV activities: Synthesis and structure-activity relationship
文献作者:Vara Prasad,J.V.N.; Loo,J.A.; Boyer,F.E.; Stier,M.A.; Gogliotti,R.D.; Turner,W.J.; Harvey,P.J.; Kramer,M.R.; Mack,D.P.; Scholten,J.D.; Gracheck,S.J.; Domagala,J.M.
参考来源:Bioorg Med Chem 1998,6(10),1707

18-VDOC

Chemical Name: 21-Hydroxy-18-vinylpregn-4-ene-3,20-dione; 11-Deoxy-18-vinylcorticosterone
项目整合开发状态: Biological Testing
项目研究机构: CNRS (Originator)
合成路线:Hydrolysis of ketal (I) with p-toluenesul...
参考文献标题:18-Vinyldeoxycorticosterone: A potent inhibitor of the bovine cytochrome P-450(11beta)
文献作者:Davioud,E.; Piffeteau,A.; Delorme,C.; Coustal,S.; Marquet,A.
参考来源:Bioorg Med Chem 1998,6(10),1781

HI-253

Chemical Name: N-(5-Bromo-2-pyridinyl)-N'-[2-(2-chlorophenyl)ethyl]thiourea
项目整合开发状态: Preclinical
项目研究机构: Parker Hughes Institute (Originator)
合成路线:2-Amino-5-bromopyridine (I) was condensed w...
参考文献标题:Rational design and synthesis of phenethyl-5-bromopyridyl thiourea derivatives as potent non-nucleoside inhibitors of HIV reverse transcriptase
文献作者:Vig,R.; Mao,C.; Venkatachalam,T.K.; Tuel-Ahlgren,L.; Sudbeck,E.A.; Uckun,F.M.
参考来源:Bioorg Med Chem 1998,6(10),1789

新产品编号:1353119

Chemical Name: N-(5-Bromo-2-pyridinyl)-N'-[2-(3-chlorophenyl)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:2-Amino-5-bromopyridine (I) was cond...
参考文献标题:Rational design and synthesis of phenethyl-5-bromopyridyl thiourea derivatives as potent non-nucleoside inhibitors of HIV reverse transcriptase
文献作者:Vig,R.; Mao,C.; Venkatachalam,T.K.; Tuel-Ahlgren,L.; Sudbeck,E.A.; Uckun,F.M.
参考来源:Bioorg Med Chem 1998,6(10),1789

新产品编号:1354701

Chemical Name: Benzoyl-L-asparaginyl-L-(4-benzoyl)phenylalanyl-L-threoninamide
项目整合开发状态: Biological Testing
项目研究机构: University of Michigan (Originator)
合成路线:Coupling of N-Boc-benzoylphenylala...
参考文献标题:The design,synthesis,and initial evaluation of benzophenone-containing peptides as potential photoaffinity labels of oligosaccharyltransferase
文献作者:Xu,T.; Khanna,H.; Coward,J.K.
参考来源:Bioorg Med Chem 1998,6(10),1821