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:1248707

Chemical Name:
项目整合开发状态:
项目研究机构:
合成路线:The optical resolution of 4-amino-5-chloro-2-methyl-2,3-dihydrobenzofuran-7-carboxylic acid (I) by means of brucine in methanol gives the (+)-isomer (...
参考文献标题:Benzo[b]furancarboxamide derivs.,process for their preparation and their use as gastrointestinal mobility-enhancing agents
文献作者:Baba,Y.; Usui,T.; Iwata,N.(Sanwa Kagaku Kenkyusho Co.,Ltd.)
参考来源:EP 0640602; JP 1995112985; US 5442077

新产品编号:1250289

Chemical Name:
项目整合开发状态:
项目研究机构:
合成路线:Cycloaddition of betaine (I) with phenyl fluorovinyl sulfone (II) in refluxing acetonitrile produced a mixture of 6-b (III),6-a (IV),and 7-b (V) sulfo...
参考文献标题:Synthesis and biological activity of new 6- and 7-substituted 2beta-butyl-3-phenyltropanes as ligands for the dopamine transporter
文献作者:Prakash,K.R.C.; et al.
参考来源:Med Chem Res 1998,8(1-2),43

新产品编号:1251871

Chemical Name: N,N'-Bis[2-(fluorenyl-9-ylmethoxycarbonyl)-1,2,3,4-tetrahydroisoquinolin-3-ylcarbonyl]-2,2-(diamino)ethanol
项目整合开发状态: Biological Testing
项目研究机构: Universit?di Ferrara (Originator)<...
参考文献标题:Structure-activity relationships of HIV-1 protease inhibitors containing gem-diaminoserine core unit
文献作者:Marastoni,M.; et al.
参考来源:Arzneim-Forsch Drug Res 1998,48(6),709

新产品编号:1253453

Chemical Name: 4(S)-(tert-Butoxycarbonyl-L-valyl-L-leucyl-L-phenylalanylamino)-6-carbamoyl-2(E)-hexenoic acid methyl ester
项目整合开发状态: Biological Testing
项目研究机构: Lilly (Originator)
合成路线:By depr...
参考文献标题:Synthesis and evaluation of peptidyl Michael acceptors that inactivate human rhinovirus 3C protease and inhibit virus replication
文献作者:Kong,J.; Venkatraman,S.; Furness,K.; Nimkar,S.; Shepherd,T.A.; Wang,Q.M.; Aub? J.; Hanzlik,R.P.
参考来源:J Med Chem 1998,41(14),2579

新产品编号:1255035

Chemical Name: N-[2-(Dimethylamino)ethyl)-11-oxo-2-(3-pyridyl)-11H-pyrido[2,1-b]quinazoline-6-carboxamide
项目整合开发状态: Biological Testing
项目研究机构: Wyeth Pharmaceuticals (Originator)
合成路线:Condensa...
参考文献标题:Hetero-biaryl-pyridoquinazolinone derivs.as anti-cancer agents
文献作者:Trova,M.P.; Zhang,N.(American Cyanamid Co.)
参考来源:EP 0944628; WO 9823617

MEN-11467

Chemical Name: N-[2-(4-Methylphenyl)acetyl]-N-methyl-(3-naphthyl)-L-alanine N-[2-(1H-indol-3-ylcarboxamido)cyclohexyl]amide
项目整合开发状态: Preclinical
项目研究机构: Menarini (Originator)
合成路线:3-Indolylc...
参考文献标题:Pseudo-peptide cpds.as antagonists of neurokinines
文献作者:Potier,E.; Fincham,C.; Sisto,A.; Terracciano,R.(Menarini Industrie Farma Riunite srl)
参考来源:WO 9845262

新产品编号:1256617

Chemical Name: 5-(2-Methoxyphenyl)-7-methyl-3-oxo-2(Z)-benzylidene-5H-1,3-thiazolo[3,2-a]pyrimidine-6(3H)-carboxylic acid methyl ester
项目整合开发状态: Preclinical
项目研究机构: Hacettepe University (Origina...
参考文献标题:Condensed heterocyclic compounds: Synthesis and antiinflammatory activity of novel thiazolo[3,2-a]pyrimidines
文献作者:Kelicen,P.; Ertan,M.; Demirdamar,R.; Krebs,B.; Tozkoparan,B.; L鋑e,M.
参考来源:Arch Pharm 1998,331(6),201

HAK-2701

Chemical Name: 5'(R)-Ethynyladenosine; 9-(6,7-Dideoxy-beta-D-allo-hept-5-ynofuranosyl)adenine
项目整合开发状态: Biological Testing
项目研究机构: Hokkaido University (Originator), Tokyo Metropolitan Institute ...
参考文献标题:Nucleosides and nucleotides.177.9-(6,7-dideoxy-beta-D-allo-hept-5-ynofuranosyl)adenine: A selective and potent ligand for P3 purinoceptor-like protein
文献作者:Matsuda,A.; Kosaki,H.; Saitoh,Y.; Yoshimura,Y.; Minakawa,N.; Nakata,H.
参考来源:J Med Chem 1998,41(15),2676

新产品编号:1258199

Chemical Name: 8-[2-[4-(1,3-Benzodioxol-5-yl)butylamino]ethoxy]-6-fluoro-3,4-dihydro-2H-1-benzopyran-4-one hydrochloride
项目整合开发状态: Preclinical
项目研究机构: Yamanouchi (Originator)
合成路线:6-Fluoro-8-...
参考文献标题:Synthesis and pharmacological characterization of novel 6-fluorochroman derivatives as potential 5-HT1A receptor antagonists
文献作者:Yasunaga,T.; Kimura,T.; Naito,R.; Kontani,T.; Wanibuchi,F.; Yamashita,H.; Nomura,T.; Tsukamoto,S.; Yamaguchi,T.; Mase,T.
参考来源:J Med Chem 1998,41(15),2765

新产品编号:1259781

Chemical Name: 4(S)-(Benzyloxycarbonyl-L-leucyl-L-phenylalanylamino)-6-carbamoyl-2(E)-hexenoic acid ethyl ester
项目整合开发状态: Biological Testing
项目研究机构: Agouron (Originator)
合成路线:The condensation...
参考文献标题:Structure-based design,synthesis,and biological evaluation of irreversible human rhinovirus 3C protease inhibitors.1.Michael acceptor structure-activity studies
文献作者:Dragovich,P.S.; Webber,S.E.; Babine,R.E.; Fuhrman,S.A.; Patick,A.K.; Matthews,D.A.; Lee,C.A.; Reich,S.H.; Prins,T.J.; Marakovits,J.T.; Littlefield,E.S.; Zhou,R.; Tikhe,J.; Ford,C.E.; Wallace,M.B.; Meador,J.W.III; Ferre,R.A.; et al.
参考来源:J Med Chem 1998,41(15),2806