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:1054121

Chemical Name: 6-O-Demethyl-3-O-(isopropoxycarbonyl)-6-O-(pivaloyl)galanthamine hydrochloride; (4aS,6R,8aS)-6-(Isopropoxycarbonyloxy)-11-methyl-3-(pivaloyloxy)-5,6,9,10,11,12-hexahydro-4aH-benzofuro[3...
参考文献标题:Galanthamine derivatives for the treatment of Alzeimer's disease
文献作者:Bores,G.M.; Kosley,R.W.Jr.
参考来源:Drugs Fut 1996,21(6),621

新产品编号:1055703

Chemical Name: (1R,2R)-1-[2-(2,4-Difluorophenyl)-2-hydroxy-1-methyl-3-(1,2,4-triazol-1-yl)propyl]-3-[4-(1,1,2,2-tetrafluoroethoxy)phenyl]imidazolidin-2-one
项目整合开发状态: Biological Testing
项目研究机构: T...
参考文献标题:Optically active antifungal azoles.VIII.Synthesis and antifungal activity of 1-[(1R,2R)-2-(2,4-difluoro- and 2-fluorophenyl)-2-hydroxy-1-methyl-3-(1H-1,2,4-triazol-1-yl)propyl]-3-(4-substituted phenyl)-2(1H,3H)-imidazolones and 2-imidazolidinones
文献作者:Kitazaki,T.; Tasaka,A.; Tamura,N.; Matsushita,Y.; Hosono,H.; Hayashi,R.; Okonogi,K.; Itoh,K.
参考来源:Chem Pharm Bull 1999,47(3),351

Korupensamine B

Chemical Name: (R-biar)-6,8-Dihydroxy-5-(4-hydroxy-5-methoxy-7-methyl-1-naphthyl)-1(R),3(R)-dimethyl-1,2,3,4-tetrahydroisoquinoline
项目整合开发状态: Biological Testing
项目研究机构: US Department of Health &...
参考文献标题:Total synthesis of michellamines A-C,korupensamines A-D,and ancistrobrevine B
文献作者:Hoye,T.R.; et al.
参考来源:J Org Chem 1999,64(19),7184

Korupensamine C

Chemical Name: (S-biar)-6,8-Dihydroxy-5-(4,5-dimethoxy-7-methyl-1-naphthyl)-1(R),3(R)-dimethyl-1,2,3,4-tetrahydroisoquinoline
项目整合开发状态: Biological Testing
项目研究机构: US Department of Health & Human...
参考文献标题:Total synthesis of michellamines A-C,korupensamines A-D,and ancistrobrevine B
文献作者:Hoye,T.R.; et al.
参考来源:J Org Chem 1999,64(19),7184

L-164710

Chemical Name: 1-[5-(2,2-Diphenylacetyl)-1-(3,5-diphenylbenzyl)-4,5,6,7-tetrahydro-1H-imidazo[4,5-c]pyridin-6(S)-ylcarbonyl]pyrrolidine-2(S)-carboxylic acid tert-butyl ester
项目整合开发状态: Biological Te...
参考文献标题:Non-peptide ligands of the human C5a receptor: Structure-activity relationship of a series of tetrahydroimidazopyridines
文献作者:Kim,D.; et al.
参考来源:213th ACS Natl Meet (April 13-17,San Francisco) 1997,Abst MEDI 088

LAS-333

Chemical Name: 2(R)-Amino-3-[6,7-dimethyl-3-(phosphonomethyl)quinolin-2-yl]propionic acid; 3-[6,7-dimethyl-3-(phosphonomethyl)quinolin-2-yl]-D-alanine
项目整合开发状态: Biological Testing
项目研究机构: AstraZ...
参考文献标题:Heterocyclic cpds.
文献作者:Swahn,B.-M.(AstraZeneca plc)
参考来源:EP 0736032; JP 1997506895; US 5710139; WO 9517410

Phomoidride A, CP-225917

Chemical Name: (+)-2-[11-Hydroxy-5-[2-hydroxy-3-oxo-6(E)-octenyl]-6-[6(E)-octenyl]-1,3,13-trioxo-3,4,5,6,9,10-hexahydro-1H-11,9-(epoxymethano)-4,8-methanocyclonona[c]furan-9-yl]acetic acid
项目整合开发状态...
参考文献标题:Total synthesis of the CP molecules CP-263,114 and CP-225,917 - Part 1: Synthesis of key intermediates and intelligence gathering
文献作者:Nicolaou,K.C.; et al.
参考来源:Angew Chem.Int Ed Engl 1999,38(11),1669

新产品编号:1057285

Chemical Name: (1R,2R)-1-[2-(2-Fluorophenyl)-2-hydroxy-1-methyl-3-(1,2,4-triazol-1-yl)propyl]-3-[4-(1,1,2,2-tetrafluoroethoxy)phenyl]imidazolidin-2-one
项目整合开发状态: Biological Testing
项目研究机构: Taked...
参考文献标题:Optically active antifungal azoles.VIII.Synthesis and antifungal activity of 1-[(1R,2R)-2-(2,4-difluoro- and 2-fluorophenyl)-2-hydroxy-1-methyl-3-(1H-1,2,4-triazol-1-yl)propyl]-3-(4-substituted phenyl)-2(1H,3H)-imidazolones and 2-imidazolidinones
文献作者:Kitazaki,T.; Tasaka,A.; Tamura,N.; Matsushita,Y.; Hosono,H.; Hayashi,R.; Okonogi,K.; Itoh,K.
参考来源:Chem Pharm Bull 1999,47(3),351

RK-682

Chemical Name: 3-Hexadecanoyl-5-(hydroxymethyl)tetrahydrofuran-2,4-dione
项目整合开发状态: Preclinical
项目研究机构:
合成路线:An efficient synthesis of the optically active compound has been reported.Acid hyd...
参考文献标题:Asymmetric synthesis of a 3-acyltetronic acid derivative,RK-682,and formation of its calcium salt during silica gel column chromatography
文献作者:Sodeoka,M.; Sampe,R.; Kojima,S.; Baba,Y.; Morisaki,N.; Hashimoto,Y.
参考来源:Chem Pharm Bull 2001,49(2),206

SCH-23863

Chemical Name: N-[2-(5-Ethoxy-10,11-dihydro-5H-dibenzo[a,d]cyclohepten-5-yl)ethyl]-N,N-dimethylamine
项目整合开发状态: Preclinical
项目研究机构: Schering-Plough (Originator)
合成路线:Title compound was obtaine...
参考文献标题:Tricyclic derivs.,pharmaceutical compsns.containing them
文献作者:Ting,P.C.; Solomon,D.L.; Friary,R.J.; Villani,F.J.; Piwinski,J.J.; Lee,J.F.; Seidl,V.A.; Jakway,J.P.; Vashi,D.B.(Schering Corp.)
参考来源:EP 0733035; JP 1997500656; US 5538986; WO 9515939