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。
如有产品相关项目调研推广服务, 请致函联系我们

客户展示

新项目整合精选

NSC-658879

Chemical Name: 4''-(Hydroxymethyl)-2,2':5',2''-terthiophene-5-carbaldehyde
项目整合开发状态: Biological Testing
项目研究机构: Industrial Technol. & Res. Inst. (Originator), Purdue Research Foundation (Origina...
参考文献标题:Polythiophene anti-tumor agents
文献作者:Chang,C.-T.; Chang,C.-J.; Lee,C.-T.; Lin,F.-L.; Tsai,J.-D.; Ashendel,C.L.; Chan,T.C.K.; Geahlen,R.L.; Waters,D.J.(Industrial Technology & Research Institute; Purdue Research Foundation)
参考来源:EP 1007035; WO 9823269

RPR-122818

Chemical Name: 3(R)-(4-Methoxyphenylsulfonyl)-2(S)-methyl-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:The reaction of 5-phenylpentanal...
参考文献标题:Substd.(aryl,heteroaryl,arylmethyl or heteroarylmethyl) hydroxamic acid cpds.
文献作者:Groneberg,R.D.; Neuenschwander,K.W.; Djuric,S.W.; McGeehan,G.M.; Burns,C.J.; Condon,S.M.; Morrissette,M.M.; Salvino,J.M.; Scotese,A.C.; Ullrich,J.W.(Aventis Pharma SA)
参考来源:EP 0871439; JP 2000503012; WO 9724117

CX-659S

Chemical Name: N-(6-Amino-3-methyl-2,4-dioxo-1-phenyl-1,2,3,4-tetrahydropyrimidin-5-yl)-6-hydroxy-2,5,7,8-tetramethyl-3,4-dihydro-2H-1-benzopyran-2(S)-carboxamide
项目整合开发状态: Preclinical
项目研究机构: J...
参考文献标题:Hydroquinone derivs.and their medicinal use
文献作者:Isobe,Y.; Goto,Y.; Tobe,M.; Takahashi,O.(Japan Energy Corp.)
参考来源:JP 1998147575; US 5821247

Ro-60-0759

Chemical Name: (+)-trans-8-Ethyl-7-hydroxy-9-methoxy-2-methyl-1,3,4,4a,5,10b-hexahydrobenzo[h]isoquinolin-6(2H)-one
项目整合开发状态: Preclinical
项目研究机构: Roche (Originator)
合成路线:The reaction of benza...
参考文献标题:Tricyclic benzo[e]isoindoles and benzo[h]isoquinolines
文献作者:Stadler,H.; B�? M.; Wichmann,J.(F.Hoffmann-La Roche AG)
参考来源:EP 0958285; JP 2000507965; WO 9830546

BCX-1170

Chemical Name: Furan-2-carboxylic acid 4-[3-amino-3-imino-1(E)-propenyl]phenyl ester methanesulfonate
项目整合开发状态: Preclinical
项目研究机构: BioCryst (Originator)
合成路线:The reaction of 4-hydroxybenzald...
参考文献标题:Development of novel inhibitors of complement and coagulation serine proteases
文献作者:Niwas,S.; Moore,R.; Kilpatrick,J.M.; Babu,Y.S.; Johnson,H.; Kellogg,D.
参考来源:216th ACS Natl Meet (Aug.23-27,Boston) 1998,Abst MEDI 088

JS-2-13-P2, (S)-2-Me-EM-138, 2-Me-PGA, M-PGA

Chemical Name: (-)-(S)-2-Methyl-2-(1-oxo-2,3-dihydro-1H-isoindol-2-yl)pentanedioic acid
项目整合开发状态: Preclinical
项目研究机构: Children's Medical Center Corp. (Originator), EntreMed (Originator)
合成路线:...
参考文献标题:Synthesis and enantiomeric separation of 2-phthalimidino-glutaric acid analogues: Potent inhibitors of tumor metastasis
文献作者:Shah,J.H.; Swartz,G.M.; Papathanassiu,A.E.; Treston,A.M.; Fogler,W.E.; Madsen,J.W.; Green,S.J.
参考来源:J Med Chem 1999,42(16),3014

WHI-07

Chemical Name: 3'-Azido-5-bromo-5'-O-[4-bromophenoxy[1-(methoxycarbonyl)ethylamino]phosphoryl]-3'-deoxy-6-methoxy-5,6-dihydrothymidine
项目整合开发状态: Preclinical
项目研究机构: Parker Hughes Institute (Orig...
参考文献标题:AZT derivs.exhibiting spermicidal and anti-viral activity
文献作者:Uckun,F.M.; Venkatachalam,T.; D'Cruz,O.(Parker Hughes Institute)
参考来源:WO 9948902

PD-165167

Chemical Name: 7-[N-[2-(Phenylamino)ethyl]aminomethyl]-2H-[1]benzopyran-2-one
项目整合开发状态: Preclinical
项目研究机构: Pfizer (Originator)
合成路线:Photochemical bromination of 7-methylcoumarin (I) using N-...
参考文献标题:Design,synthesis,and evaluation of coumarins as potent and selective dopamine D4 antagonists
文献作者:Kesten,S.R.; et al.
参考来源:216th ACS Natl Meet (Aug.23-27,Boston) 1998,Abst MEDI 123

WQ-3345, WQ-2942(free base)

Chemical Name: 7-Amino-1-(5-amino-2,4-difluorophenyl)-6-fluoro-8-methyl-4-oxo-1,4-dihydroquinoline-3-carboxylic acid ethanolamine salt
项目整合开发状态: Preclinical
项目研究机构: Wakunaga (Originator)
合成路线...
参考文献标题:Novel pyridonecarboxylic acid derivs.or salts thereof and drugs containing the same as the active ingredient
文献作者:Sakae,N.; Yazaki,A.; Kuramoto,Y.; Yoshida,J.; Niino,Y.; Oshita,Y.; Hirao,Y.; Hayashi,N.; Amano,H.(Wakunaga Pharmaceutical Co.,Ltd.)
参考来源:EP 0945435; WO 9823592

L-168721

Chemical Name: N-(6-Aminohexyl)-2-[6-phenyl-2-(2-phenylethyl)-4-oxo-3,4-dihydro-3-quinazolinyl]acetamide hydrochloride
项目整合开发状态: Biological Testing
项目研究机构: Merck & Co. (Originator)
合成路线:The c...
参考文献标题:Modeling directed design and biological evaluation of quinazolinones as non-peptidic growth hormone secretagogues
文献作者:Ye,Z.; Gao,Y.; Bakshi,R.K.; Chen,M.H.; Rohrer,S.P.; Feighner,S.D.; Pong,S.S.; Howard,A.D.; Blake,A.; Birzin,E.T.; Locco,L.; Parmar,R.M.; Chan,W.W.; Schaeffer,J.M.; Smith,R.G.; Patchett,A.A.; Nargund,R.P.
参考来源:Bioorg Med Chem Lett 2000,10(1),5