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:2424133

Chemical Name: (4S,7R,8S,9S,13R,14S,16S)-13,14-Epoxy-4,8-dihydroxy-5,5,7,9-tetramethyl-16-[(E)-1-methyl-2-(methylthiazol-4-yl)vinyl]-2,6-dioxo-1-oxacyclohexadecane-13-carbonitrile; (1S,3S,7S,10R,11S,1...
参考文献标题:C12-cyano epothilone derivs.
文献作者:Vite,G.D.; Regueiro-Ren,A.(Bristol-Myers Squibb Co.)
参考来源:US 2003186965; WO 0377903

PHI-P518

Chemical Name: [4-[2-[4-[2-(Trichloromethyl)quinazolin-4-ylamino]phenyl]diazenyl]phenyl]arsonic acid tetrahydrochloride
项目整合开发状态: Biological Testing
项目研究机构: Parker Hughes Institute (Originator)<...
参考文献标题:Organic-arsonic cpds.
文献作者:Uckun,F.M.(Parker Hughes Institute)
参考来源:US 6686344

VL-0395

Chemical Name: N-[2-(1H-Indol-2-ylcarboxamido)benzoyl]-DL-phenylalanine
项目整合开发状态: Preclinical
项目研究机构: Rotta (Originator)
合成路线:Condensation of isatoic anhydride (I) with DL-phenylalanine ethyl...
参考文献标题:Anthranilic acid derivatives: A new class of non-peptide CCK1 receptor antagonists
文献作者:Varnavas,A.; Lassiani,L.; Valenta,V.; Berti,F.; Mennuni,L.; Makovec,F.
参考来源:Bioorg Med Chem 2003,11(5),741

JWH-229

Chemical Name: (6aR,10aR)-3-(1,1-Dimethylhexyl)-1-methoxy-6,6,9-trimethyl-6a,7,10,10a-tetrahydro-6H-dibenzo[b,d]pyran
项目整合开发状态: Biological Testing
项目研究机构: Clemson University (Originator), Virgin...
参考文献标题:1-Methoxy-,1-deoxy-11-hydroxy- and 11-hydroxy-1-methoxy-DELTA(8)-tetrahydrocannabinols: New selective ligands for the CB2 receptor
文献作者:Huffman,J.W.; Bushell,S.M.; Miller,J.R.A.; Wiley,J.L.; Martin,B.R.
参考来源:Bioorg Med Chem 2002,10(12),4119

新产品编号:2425715

Chemical Name: 4,6-Dichloro-3-(2,4-dioxo-3-phenylimidazolidin-1-ylmethyl)-1H-indole-2-carboxylic acid
项目整合开发状态: Preclinical
项目研究机构: Johannes Gutenberg-Universit鋞 Mainz (Originator)
合成路线:Diazo...
参考文献标题:Hydantoin-substituted 4,6-dichloroindole-2-carboxylic acids as ligands with high affinity for the glycine binding site of the NMDA receptor
文献作者:Jansen,M.; Potschka,H.; Brandt,C.; Lcher,W.; Dannhardt,G.
参考来源:J Med Chem 2003,46(1),64

新产品编号:2427297

Chemical Name: 6-Amino-2-phenyl-1-(beta-D-ribofuranosyl)imidazo[4,5-e][1,3]diazepine-4,8(1H,5H)-dione
项目整合开发状态: Biological Testing
项目研究机构: Nabi Biopharmaceuticals (Originator), University of Mar...
参考文献标题:In vitro inhibition of the measles virus by novel ring-expanded ('fat') nucleoside analogues containing the imidazo[4,5-e]diazepine ring system
文献作者:Zhang,N.; Chen,H.-M.; Sood,R.; Kalicharran,K.; Fattom,A.I.; Naso,R.B.; Barnard,D.L.; Sidwell,R.W.; Hosmane,R.S.
参考来源:Bioorg Med Chem Lett 2002,12(23),3391

新产品编号:2428879

Chemical Name: 1-[3-[3-(Allyloxy)-3-oxo-1-propenyl]phenyl]-1,1-difluoromethylphosphonic acid diammonium salt
项目整合开发状态: Biological Testing
项目研究机构: University of Waterloo (Originator)
合成路线:Cond...
参考文献标题:Synthesis of [difluoro-(3-alkenylphenyl)-methyl]-phosphonic acids on non-crosslinked polystyrene and their evaluation as inhibitors of PTP1B
文献作者:Hum,G.; Lee,J.; Taylor,S.D.
参考来源:Bioorg Med Chem Lett 2002,12(23),3471

URB-597

Chemical Name: N-Cyclohexylcarbamic acid 3'-carbamoylbiphenyl-3-yl ester
项目整合开发状态: Preclinical
项目研究机构: Universit?degli Studi "La Sapienza" (Originator), Universit?degli Studi di Bari (Originator...
参考文献标题:Modulation of anxiety through blockade of anandamide hydrolysis
文献作者:Kathuria,S.; Gaetani,S.; Fegley,D.; Vali�? M.; Duranti,A.; Tontini,A.; Mor,M.; Tarzia,G.; La Rana,G.; Calignano,A.; Giustino,A.; Tattoli,M.; Palmery,M.; Cuomo,V.; Piomelli,D.
参考来源:Nat Med 2003,9(1),76

新产品编号:2430461

Chemical Name: (1R,2S,3S,3aS,4R,6aR,7aR,11aS,11bR,11cR)-4,9-Bis(ethoxycarbonyloxy)-1,2-dihydroxy-8,11a-dimethyl-5,10-dioxo-2,3,3a,4,5,6a,7,7a,10,11,11a,11b-dodecahydro-1H-3,11c-(epoxymethano)phenanthr...
参考文献标题:New semisynthetic quassinoids with in vivo antimalarial activity
文献作者:Murakami,N.; Sugimoto,M.; Kawanishi,M.; Tamura,S.; Kim,H.-S.; Begum,K.; Wataya,Y.; Kobayashi,M.
参考来源:J Med Chem 2003,46(4),638

NIDA-41020

Chemical Name: 1-(2,4-Dichlorophenyl)-5-(4-methoxyphenyl)-4-methyl-N-(1-piperidinyl)-1H-pyrazole-3-carboxamide
项目整合开发状态: Preclinical
项目研究机构: National Institute on Drug Abuse (Originator)
合成路线...
参考文献标题:Synthesis,structure-activity relationship,and evaluation of SR141716 analogues: Development of central cannabinoid receptor ligands with lower lipophilicity
文献作者:Katoch-Rouse,R.; Pavlova,O.A.; Caulder,T.; Hoffman,A.F.; Mukhin,A.G.; Horti,A.G.
参考来源:J Med Chem 2003,46(4),642