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:1685339

Chemical Name: 2-[2-(4-Chlorophenyl)-8-methylimidazo[1,2-a]pyridin-3-yl]-N,N-dipropylacetamide
项目整合开发状态: Preclinical
项目研究机构: Universit?degli Studi di Bari (Originator), Universit?degli Studi di ...
参考文献标题:Novel 2-phenylimidazo[1,2-a]pyridine derivatives as potent and selective ligands for peripheral benzodiazepine receptors: Synthesis,binding affinity,and in vivo studies
文献作者:Trapani,G.; Franco,M.; latrofa,A.; Ricciardi,L.; Carotti,A.; Serra,M.; Sanna,E.; Biggio,G.; Liso,G.
参考来源:J Med Chem 1999,42(19),3934

PE2Br

Chemical Name: 8-[3-Bromo-2(E)-propenyl]-3beta-(4-methylphenyl)-8-azabicyclo[3.2.1]octane-2beta-carboxylic acid methyl ester
项目整合开发状态: Preclinical
项目研究机构: INSERM (Originator)
合成路线:The reactio...
参考文献标题:Synthesis,ligand binding,QSAR,and CoMFA study of 3beta-(p-substitutedphenyl)tropane-2beta-carboxylic acid methyl esters
文献作者:Gao,Y.; Rahman,M.A.; Abraham,P.; Boja,J.W.; Carroll,F.I.; Lewin,A.H.; Kuhar,M.J.; Parham,K.
参考来源:J Med Chem 1991,34(9),2719

BZA-[99mTcO], [99mTcO]-BZA

Chemical Name: [4-[4-[N-(2-Diethylamino)ethyl]carbamoyl]benzyl]-2,6,6,9-tetramethyl-4,7-diaza-2,9-dithiol]oxotechnecium
项目整合开发状态: Preclinical
项目研究机构: CIS Bio International (Originator), INSERM (...
参考文献标题:Technetium-99m radiolabelling of an N-amino-alkyl-benzamide nitrido- and oxo-technetium bis(aminoethanethiol) derivative synthesis and biological results.Potential melanoma tracer agents
文献作者:Auzeloux,P.; et al.
参考来源:J Label Compd Radiopharm 1999,42(6),567

BZA-[99mTcN], [99mTcN]-BZA

Chemical Name: [4-[4-[N-[2-(Diethylamino)ethyl]carbamoyl]benzyl]-2,6,6,9-tetramethyl-4,7-diazadecane-2,9-dithiol]nitrilotechnecium
项目整合开发状态: Preclinical
项目研究机构: CIS Bio International (Originator...
参考文献标题:Technetium-99m radiolabelling of an N-amino-alkyl-benzamide nitrido- and oxo-technetium bis(aminoethanethiol) derivative synthesis and biological results.Potential melanoma tracer agents
文献作者:Auzeloux,P.; et al.
参考来源:J Label Compd Radiopharm 1999,42(6),567

FMA-481

Chemical Name: 11-Deoxy-3-des(cladinosyl)-11-[2-[N-methyl-N-(3-quinolylmethyl)amino]ethylamino]-3-O-(2-pyridylacetyl)-6-O-methylerythromycin A 11-N,12-O-cyclic carbamate
项目整合开发状态: Biological Testin...
参考文献标题:Erythromycin A derivs.
文献作者:Ishii,T.; Tanikawa,T.; Matsuura,A.; Sugimoto,T.; Asaka,T.; Kashimura,M.(Taisho Pharmaceutical Co.,Ltd.)
参考来源:EP 0945459; WO 9823628

PNU-176968

Chemical Name: N-[3-[3-Fluoro-4-(5-thiazolyl)phenyl]-2-oxooxazolidin-5(S)-ylmethyl]acetamide
项目整合开发状态: Preclinical
项目研究机构: Pfizer (Originator)
合成路线:Lithiation of thiazole (I) with butyllithiu...
参考文献标题:Carbon-carbon-linked 5-membered heteroarylphenyl oxazolidinones with broad-spectrum antibacterial activity
文献作者:Anderson,D.J.; Allwine,D.A.; Genin,M.J.; et al.
参考来源:39th Intersci Conf Antimicrob Agents Chemother (Sept 26 1999,San Francisco) 1999,Abst F570

EDP-137

Chemical Name: 5-[(3aS,4S,6aR)-3a,4,6a-Trimethyl-2-oxoperhydrothieno[3,4-d]imidazol-4-yl]pentanoic acid 7-[N-[2-(2-azidophenyl)ethyl]-N-methylamino]-4-cyano-4-(3,4-dimethoxyphenyl)heptyl ester
项目整合...
参考文献标题:Synthesis and binding properties of photoactivable biotin-conjugated verapamil derivatives for the study of P-170 glycoprotein
文献作者:Teodori,E.; Ettori,D.; Garnier-Suillero,A.; Gualtieri,F.; Manetti,D.; Romanelli,M.N.; Scapecchi,S.
参考来源:Bioorg Med Chem 1999,7(9),1873

新产品编号:1686921

Chemical Name: 3'-N-(Cyclopenten-1-ylcarbonyl)-3'-N-debenzoylpaclitaxel
项目整合开发状态: Preclinical
项目研究机构: Korea Inst. Sci. Technol. (Originator)
合成路线:The condensation of trichloroacetyl-baccatin ...
参考文献标题:Synthesis and biology of 3'-N-acyl-N-debenzoylpaclitaxel analogues
文献作者:Roh,E.J.; Song,C.E.; Kim,D.; Pae,H.O.; Chung,H.T.; Lee,K.S.; Chai,K.B.; Lee,C.O.; Choi,S.U.
参考来源:Bioorg Med Chem 1999,7(9),2115

新产品编号:1688503

Chemical Name: 1-(4'-Fluorobiphenyl-4-ylmethyl)-1H-imidazole
项目整合开发状态: Preclinical
项目研究机构: Universit鋞 des Saarlandes (Originator)
合成路线:This compound has been obtained by condensation of 1-(4-...
参考文献标题:Imidazole substituted biphenyls: A new class of highly potent and in vivo active inhibitors of P450 17 as potential therapeutics for treatment of prostate cancer
文献作者:Wachall,B.G.; Hector,M.; Zhuang,Y.; Hartmann,R.W.
参考来源:Bioorg Med Chem 1999,7(9),1913

新产品编号:1690085

Chemical Name: 3-[(E)-2-(1-Oxidopyridin-2-yl)vinyl]-7(Z)-(2-pyridylmethylene)-3-cephem-4-carboxylic acid sodium salt S,S-dioxide
项目整合开发状态: Biological Testing
项目研究机构: Southern Methodist Universit...
参考文献标题:beta-Lactamase inhibiting cpds.
文献作者:Nidamarthy,S.D.; Buynak,J.D.; Rao,A.S.; Doppalapudi,V.R.; Adam,G.C.(Research Corporation Technologies,Inc.)
参考来源:WO 0063213