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:1691667

Chemical Name: 6-[3-[19-Amino-14(S)-carboxy-19-imino-8,12-dioxo-2,9,13,18-tetraazanonadecanoyl]phenyl]-3,8-diamino-5-methylphenanthridinium chloride; N-[N-[5-[3-(3,8-Diamino-5-methylphenanthridinium-6...
参考文献标题:Synthesis and antiviral activity of ethidium - Arginine conjugates directed against the TAR RNA of HIV-1
文献作者:Peytou,V.; Condom,R.; Patino,N.; Guedj,R.; Aubertin,A.M.; Gelus,N.; Bailly,C.; Terreux,R.; Cabrol-Bass,D.
参考来源:J Med Chem 1999,42(20),4042

新产品编号:1693249

Chemical Name: 3-(Ethoxycarbonyl)-5-(ethylsulfanylcarbonyl)-4,6-diethyl-1-methyl-2-phenylpyridinium iodide
项目整合开发状态: Biological Testing
项目研究机构: National Institutes of Health (Originator)
合成路线...
参考文献标题:Selective A3 adenosine receptor antagonists: Water-soluble 3,5-diacyl-1,2,4-trialkylpyridinium salts and their oxidative generation from dihydropyridine precursors
文献作者:Xie,R.; Li,A.H.; Ji,X.D.; melman,N.; Olah,M.E.; Stiles,G.L.; Jacobson,K.A.
参考来源:J Med Chem 1999,42(20),4232

新产品编号:1694831

Chemical Name: 3-[1-Methylpyrrolidin-2(R)-ylmethyl]-1H-indol-5-ol
项目整合开发状态: Preclinical
项目研究机构: Purdue University (Originator)
合成路线:Alternatively,5-methoxyindole (III) was N-silylated employi...
参考文献标题:Further studies on oxygenated tryptamines with LSD-like activity incorporating a chiral pyrrolidine moiety into the side chain
文献作者:Gerasimov,M.; Marona-Lewicka,D.; Kurrasch-Orbaugh,D.M.; Qandil,A.M.; Nichols,D.E.
参考来源:J Med Chem 1999,42(20),4257

新产品编号:1696413

Chemical Name: 1-[4-(4-Fluorophenyl)-4-oxobutyl]piperidine-4-carboxylic acid methyl ester
项目整合开发状态: Preclinical
项目研究机构: Central Drug Research Institute (Originator)
合成路线:The reaction of piper...
参考文献标题:Synthesis and SAR studies of 1-substituted-n-(4-alkoxycarbonylpiperidin-1-yl)alkanes as potent antiarrhythmic agents
文献作者:Tripathi,R.C.; Pandey,S.K.; Kar,K.; Saxena,A.K.
参考来源:Bioorg Med Chem Lett 1999,9(18),2693

Salvicine

Chemical Name: 8-(3,4-Dihydroxy-4-methylpentyl)-3-isopropyl-7-methylnaphthalene-1,2-dione
项目整合开发状态: Preclinical
项目研究机构: Chinese Academy of Sciences (Originator)
合成路线:The epoxidation of naphth...
参考文献标题:Synthesis and antitumour activity of novel diterpenequinone salvicine and the analogs
文献作者:Zhang,J.S.; Ding,J.; Tang,Q.M.; Li,M.; Zhao,M.; Lu,L.J.; Chen,L.J.; Yuan,S.T.
参考来源:Bioorg Med Chem Lett 1999,9(18),2731

新产品编号:1697995

Chemical Name: 4-Hydroxy-3-[2-oxo-3(S)-(thieno[2,3-c]pyridin-2-ylsulfonamido)pyrrolidin-1-ylmethyl]benzamidine
项目整合开发状态: Preclinical
项目研究机构: Aventis Pharma (Originator)
合成路线:Reaction of salic...
参考文献标题:Substd.sulfonic acid N-[(aminoiminomethyl)phenylalkyl]-azaheterocyclamide cpds.
文献作者:Ewing,W.R.; Becker,M.R.; Choi-Sledeski,Y.M.; Pauls,H.W.; McGarry,D.G.; Davis,R.S.; Spada,A.P.(Aventis Pharma SA)
参考来源:EP 0894088; JP 2000505815; US 5731315; WO 9824784

MnBOPP

Chemical Name: Disodium [7,12-Bis[1,2-bis[(1,2-dicarba-closo-dodecaboran(12)-1-ylcarbonyl)oxy]ethyl]-3,8,13,17-tetramethyl-21H,23H-porphine-2,18-dipropanoato(4-)]manganate(1-) acetate hydrate
项目整合开...
参考文献标题:Metallo porphyrin compsns.
文献作者:Kahl,S.B.; Craik,C.S.(Universit�?Regensburg; University of California,Oakland)
参考来源:JP 1996501103; WO 9405285

新产品编号:1699577

Chemical Name: 7-[6-Deoxy-4-O,5-dimethyl-3-O-(5-methyl-1H-pyrrol-2-ylcarbonyl)-alpha-L-mannopyranosyloxy]-4-[2-(1H-imidazol-2-ylsulfanyl)ethoxy]-8-methyl-2H-1-benzopyran-2-one
项目整合开发状态: Biological ...
参考文献标题:Structure-activity relationship in two series of aminoalkyl substituted coumarin inhibitors of gyrase B
文献作者:Laurin,P.; Ferroud,D.; Schio,L.; Klich,M.; Dupuis-Hamelin,C.; Mauvais,P.; Lassaigne,P.; Bonnefoy,A.; Musicki,B.
参考来源:Bioorg Med Chem Lett 1999,9(19),2875

新产品编号:1701159

Chemical Name: 7-[6-Deoxy-4-O,5-dimethyl-3-O-(5-methyl-1H-pyrrol-2-ylcarbonyl)-alpha-L-mannopyranosyloxy]-8-methyl-2-oxo-5-pentyl-2H-1-benzopyran-3-carboxylic acid
项目整合开发状态: Biological Testing
项...
参考文献标题:Synthesis and biological evaluation of coumarincarboxylic acids as inhibitors of gyrase B.L-Rhamnose as an effective substitute for L-noviose
文献作者:Ferroud,D.; Collard,J.; Klich,M.; Dupuis-Hamelin,CF.; Mauvais,P.; Lassaigne,P.; Bonnefoy,A.; Musicki,B.
参考来源:Bioorg Med Chem Lett 1999,9(19),2881

新产品编号:1702741

Chemical Name: 3(R)-(Cyclopentylmethyl)-2(R)-[N-methyl-N-(methylsulfonyl)aminomethyl]-4-oxo-4-(1-piperidinyl)butyrohydroxamic acid
项目整合开发状态: Preclinical
项目研究机构: British Biotech (Originator)
合...
参考文献标题:The synthesis and biological evaluation of non-peptidic matrix metalloproteinase inhibitors
文献作者:Martin,F.M.; Beckett,R.P.; Bellamy,C.L.; Courtney,P.F.; Davies,S.J.; Drummond,A.H.; Dodd,R.; Pratt,L.M.; Patel,S.R.; Ricketts,M.L.; Todd,R.S.; Tuffnel,A.R.; Ward,J.W.; Whittaker,M.
参考来源:Bioorg Med Chem Lett 1999,9(19),2887