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:1139549

Chemical Name: (3S,7R,10R,13E,16S)-10-(3-Chloro-4-methoxybenzyl)-16-[2(S),3(S)-epoxy-1(S)-methyl-3-phenylpropyl]-3-isobutyl-7-methyl-1,4-dioxa-8,11-diazacyclohexadec-13-ene-2,5,9,12-tetraone
项目整合开发...
参考文献标题:Pharmaceutical cpds.
文献作者:Moore,R.E.; Patel,V.F.; Ray,J.E.; Toth,J.E.(Eli Lilly and Company; University of Hawaii; Wayne State University)
参考来源:EP 0850057; JP 2000501067; WO 9707798; WO 9708334

RGH-5279

Chemical Name: (-)-(13aR,13bS)-13a-Ethyl-2,3,5,6,13a,13b-hexahydro-1H-indolo[3,2,1-de]pyrido[3,2,1-ij][1,5]naphthyridine-12-carboxylic acid 2-acetoxyethyl ester hydrochloride
项目整合开发状态: Preclinical<...
参考文献标题:Trans apovincaminic acid ester derivs.as drugs
文献作者:Sz醤tay,C.; Moldvai,I.; Vedres,A.; Incze,M.; Kreidl,J.; Czibula,L.; Farkas,J.; Deutschn?Juh醩z,I.; Gere,A.; Pellioniszn?Par骳zai,M.; Lapis,E.; Szekeres,A.; Z醞ern?Bal醶s,M.; Sarkadi,A.; et al.(Gedeon Richter Ltd.)
参考来源:EP 0876367; JP 2000502676; US 6093720; WO 9723481

新产品编号:1141131

Chemical Name: 3-(4-Methoxyphenylsulfonyl)-7-phenylheptanohydroxamic acid
项目整合开发状态: Biological Testing
项目研究机构: Aventis Pharma (Originator)
合成路线:Horner-Emmons condensation of 5-phenylpentanal ...
参考文献标题:Dual inhibition of phosphodiesterase 4 and matrix metalloproteinases by an (arylsulfonyl)hydroxamic acid template
文献作者:Groneberg,R.D.; Burns,C.J.; Morrissette,M.M.; Ullrich,J.W.; Morris,R.L.; Darnbrough,S.; Djuric,S.W.; Condon,S.M.; McGeehan,G.M.; Labaudiniere,R.; Neuenschwander,K.; Scotese,A.C.; Kline,J.A.
参考来源:J Med Chem 1999,42(4),541

GW-250495

Chemical Name: 16alpha,17alpha-[(R)-Butylidenedioxy]-6alpha,9alpha-difluoro-11beta-hydroxy-3-oxo-4-androstene-17beta-carbothioic acid S-(2-oxotetrahydrofuran-3-y) ester
项目整合开发状态: Phase I
项目研究机构:...
参考文献标题:Lactone derivs.of 17beta-carboxy,carbothio and amide androstane derivs.
文献作者:Biggadike,K.; Procopiou,P.A.(Glaxo Wellcome plc)
参考来源:JP 1999501675; US 6197761; WO 9724365

新产品编号:1142713

Chemical Name: N-[5-Amino-5-methyl-2(E)-hexenoyl]-N-methyl-3-(2-naphthyl)-D-alanine N-[1(R)-benzyl-2-(methylsulfonamido)ethyl]-N-methylamide
项目整合开发状态: Biological Testing
项目研究机构: Novo Nordisk (Or...
参考文献标题:New growth hormone secretagogues: C-terminal modified sulfonamide-analogues of NN703
文献作者:Peschke,B.; Hansen,B.S.
参考来源:Bioorg Med Chem Lett 1999,9(9),1295

PD-157667

Chemical Name: 2-(4,4-Diphenylbutyl)-6-(perhydroazepin-1-yl)-1,2,3,4-tetrahydroisoquinolin-5-ol
项目整合开发状态: Biological Testing
项目研究机构: Neurex (Originator), Pfizer (Originator)
合成路线:Alkylation o...
参考文献标题:Synthesis and structure-activity relationship of substituted 1,2,3,4-tetrahydroisoquinolines as N-type calcium channel blockers
文献作者:Yuen,P.; Schelkun,R.M.; Szoke,B.; Tarczy-Hornoch,K.
参考来源:Bioorg Med Chem Lett 1998,8(18),2415

新产品编号:1144295

Chemical Name: 4-[1-(4-Phenylbutyl)piperidin-4-yl]phenol
项目整合开发状态: Preclinical
项目研究机构: Pfizer (Originator)
合成路线:The alkylation of 4-(4-methoxyphenyl)piperidine (I) with 4-phenylbutyl tosylate...
参考文献标题:4-Substd.piperidine analogs and their use as subtype selective NMDA receptor antagonists
文献作者:Bigge,C.F.; Cai,S.X.; Weber,E.; Woodward,R.; Keana,J.F.W.; Lan,N.C.; Guzikowski,A.P.; Zhou,Z.-L.; Yeun,P.-W.(CoCensys,Inc.; Pfizer Inc.)
参考来源:EP 0869792; JP 2000500773; WO 9723216

SDZ-268970

Chemical Name: (3S,7R,10R,13E,16S)-10-(3-Chloro-4-methoxybenzyl)-16-[2(R),3(R)-epoxy-1(S)-methyl-3-phenylpropyl]-3-isobutyl-7-methyl-1,4-dioxa-8,11-diazacyclohexadec-13-ene-2,5,9,12-tetraone
项目整合开发...
参考文献标题:Synthesis and biological evaluation of novel cryptophycin analogs with modification in the beta-alanine region
文献作者:Shih,C.; Gossett,L.S.; Gruber,J.M.; Grossman,C.S.; Andis,S.L.; Schultz,R.M.; Worzalla,J.F.; Corbett,T.H.; Metz,J.T.
参考来源:Bioorg Med Chem Lett 1999,9(1),69

新产品编号:1145877

Chemical Name: 4-[4-(4-Benzylpiperidin-1-yl)-1-butynyl]phenol
项目整合开发状态: Preclinical
项目研究机构: Pfizer (Originator)
合成路线:4-Benzylpiperidine (I) was alkylated with butynyl tosylate (II) to afford ...
参考文献标题:Subtype-selective N-methyl-D-aspartate receptor antagonists: Synthesis and biological evaluation of 1-(arylakynyl)-4-benzylpiperidines
文献作者:Wright,J.L.; Gregory,T.F.; Bigge,C.F.; Boxer,P.A.; Serpa,K.; Meltzer,L.T.; Wise,L.D.; Cai,S.X.; Hawkinson,J,E.; Konkoy,C.S.; Whittemore,E.R.; Woodward,R.M.; Zhou,Z.L.
参考来源:J Med Chem 1999,42(13),2469

PD-158143

Chemical Name: 4,4'-(1-Methyl-4,4-diphenylbutylidene)bis[2-(perhydroazepin-1-ylmethyl)phenol] dioxalate
项目整合开发状态: Biological Testing
项目研究机构: Neurex (Originator), Pfizer (Originator)
合成路线:The ...
参考文献标题:Synthesis and biological activity of substituted bis-(4-hydroxyphenyl)methanes as N-type calcium channel blockers
文献作者:Schelkun,R.M.; Yuen,P.; Malone,T.C.; Rock,D.M.; Stoehr,S.; Szoke,B.; Tarczy-Hornoch,K.
参考来源:Bioorg Med Chem Lett 1999,9(16),2447