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

BrHPP sodium salt

Chemical Name: Diphosphoric acid 4-bromo-3-hydroxy-3-methylbutyl ester trisodium salt
项目整合开发状态: Preclinical
项目研究机构: INSERM (Originator)
合成路线:The reaction of 3-methyl-3-buten-1-ol (I) with tos...
参考文献标题:Phosphohalohydrins,method for making same and uses
文献作者:Peyrat,M.-A.; Bonneville,M.; Fournie,J.-J.; Belmant,C.(INSERM (Institut National de la Sante et de la Recherche Medicale))
参考来源:FR 2782721; WO 0012516

RWJ-28810

Chemical Name: [4-[2-(4-Nitrophenyl)ethyl]piperazin-1-yl](4-nitrophenyl)methanone
项目整合开发状态: Biological Testing
项目研究机构: R.W. Johnson (Originator)
合成路线:The acylation of piperazine (II) with 4-n...
参考文献标题:Synthesis and selective class III type antiarrhythmic activity of 4-aroyl (and aryl)-1-aralkylpiperazines
文献作者:Kanojia,R.M.; et al.
参考来源:219th ACS Natl Meet (March 26 2000,San Francisco) 2000,Abst MEDI 204

SM-31900

Chemical Name: 3(S)-[2-[4-(Aminomethyl)-2-[1(R)-carboxyethoxy]phenylamino]-2-oxoethyl]-7-chloro-1,3,4,5-tetrahydrobenzo[c,d]indole-2-carboxylic acid hydrochloride
项目整合开发状态: Preclinical
项目研究机构: S...
参考文献标题:Tricyclic indole-2-carboxylic acid cpd.used as NMDA receptor antagonist
文献作者:Katayama,S.; Kishimoto,H.; Ae,N.; Nagata,R.(Sumitomo Pharmaceuticals Co.,Ltd.)
参考来源:WO 0056711

TMG

Chemical Name: 2-(alpha-D-Glucopyranosyloxymethyl)-2,5,7,8-tetramethyl-3,4-dihydro-2H-1-benzopyran-6-ol
项目整合开发状态: Preclinical
项目研究机构: CCI Corporation (Originator), Kyoto Prefectural University o...
参考文献标题:Chromanol glycoside and method for production thereof
文献作者:Murase,H.; Tsujii,T.; Kunieda,T.(CCI Corporation)
参考来源:US 5478812

新产品编号:1829301

Chemical Name: 3-(1,3-Benzodioxol-5-yl)propionic acid N'-[4-(dimethylamino)benzylidene]hydrazide
项目整合开发状态: Preclinical
项目研究机构: Universidade Federal do Rio de Janeiro (Originator)
合成路线:The reg...
参考文献标题:Synthesis and analgesic activity of novel N-acylarylhydrazones and isosters,derived from natural safrole
文献作者:Lima,P.C.; Lima,L.M.; da Silva,K.C.; Leda,P.H.; de Miranda,A.L.; Fraga,C.A.; Barreiro,E.J.
参考来源:Eur J Med Chem 2000,35(2),187

新产品编号:1830883

Chemical Name: (?-N-[5-(Diethylamino)-1-(4-nitrophenyl)pentyl]benzamide
项目整合开发状态: Preclinical
项目研究机构: Center for Chemistry of Drugs (Originator)
合成路线:Nibentan is obtained as illustrated in Sc...
参考文献标题:Synthesis and antifibrillatory activity of nibentan and its analogues
文献作者:Mashkovskiy,M.D.; Yurhakov,S.D.; Davydova,N.K.; Sizova,O.S.; Vinogradova,S.M.; L'vov,A.I.; Glushov,R.G.; Yuzhakov,S.D.; Mashkovskiy MD.
参考来源:Eur J Med Chem 2000,35(2),205

新产品编号:1832465

Chemical Name: 7alpha-[10-(N-Butyl-N-methylcarbamoyl)decyl]-3-hydroxy-19-nor-17alpha-pregna-1,3,5(10)-triene-21,17-carbolactone
项目整合开发状态: Biological Testing
项目研究机构: Universit?Laval (Originator)<...
参考文献标题:N-Butyl-N-methyl-11-(3'-hydroxy-21',17'-carbolactone-19'-nor-17'alpha-pregna-1',3',5' (10')-trien-7'alpha-yl)-undecanamide: an inhibitor of type 2 17beta-hydroxysteroid dehydrogenase that does not have oestrogenic or androgenic activity
文献作者:Sam,K.M.; Labrie,F.; Poirier,D.
参考来源:Eur J Med Chem 2000,35(2),217

新产品编号:1834047

Chemical Name: 7-[4-[3-[4-Amino-5-(3,4,5-trimethoxybenzyl)pyrimidin-2-ylimino]-5-bromo-2-oxo-2,3-dihydro-1H-indol-1-ylmethyl]piperazin-1-yl]-1-ethyl-6-fluoro-4-oxo-1,4-dihydroquinoline-3-carboxylic ac...
参考文献标题:Synthesis,antibacterial,antifungal and anti-HIV activities for norfloxacin Mannich bases
文献作者:Pandeya,S.N.; Sriram,D.; Nath,G.; De Clercq,E.
参考来源:Eur J Med Chem 2000,35(2),249

新产品编号:1835629

Chemical Name: 2-[N-(Benzyloxycarbonyl)-L-leucyl-glycyl-L-prolyl]benzothiazole
项目整合开发状态: Biological Testing
项目研究机构: CNRS (Originator), Universidade de Brasilia (Originator)
合成路线:Condensation ...
参考文献标题:Synthesis and activity of pyrrolidinyl- and thiazolidinyl-dipeptide derivatives as inhibitors of the Tc80 prolyl oligopeptidase from Trypanosoma cruzi
文献作者:Joyeau,R.; Maoulida,C.; Gullet,C.; Frappier,F.; Teixeira,A.R.L.; Schr関el,J.; Santana,J.; Grellier,P.
参考来源:Eur J Med Chem 2000,35(2),257

新产品编号:1837211

Chemical Name: 1-[N-(Benzyloxycarbonyl)-L-leucyl-glycyl]pyrrolidine-2(S)-carbonitrile
项目整合开发状态: Biological Testing
项目研究机构: CNRS (Originator), Universidade de Brasilia (Originator)
合成路线:Conden...
参考文献标题:Synthesis and activity of pyrrolidinyl- and thiazolidinyl-dipeptide derivatives as inhibitors of the Tc80 prolyl oligopeptidase from Trypanosoma cruzi
文献作者:Joyeau,R.; Maoulida,C.; Gullet,C.; Frappier,F.; Teixeira,A.R.L.; Schr関el,J.; Santana,J.; Grellier,P.
参考来源:Eur J Med Chem 2000,35(2),257