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:1750201

Chemical Name: (4aR,6aS,6bR,8aS,12aS,12bR,14bR)-8a-(Methoxycarbonyl)-4,4,6a,6b,11,11,14b-heptamethyl-3,13-dioxo-3,4,4a,5,6,6a,6b,7,8,8a,9,10,11,12,12a,12b,13,14b-octadecahydropicene-2-carboxylic acid;...
参考文献标题:Design and synthesis of 2-cyano-3,12-dioxoolean-1,9-dien-28-oic acid,a novel and highly active inhibitor of nitric oxide production in mouse macrophages
文献作者:Honda,T.; Rounds,B.A.V.; Gribble,G.W.; Suh,N.; Wang,Y.; Sporn,M.B.
参考来源:Bioorg Med Chem Lett 1998,8(19),2711

新产品编号:1751783

Chemical Name: N-[3(R)-[N-[N-[1-Amidino-2-hydroxypiperidin-3(S)-yl]carbamoylmethyl]carbamoyl]-3-(benzylsulfonamido)propyl]pyrazine-2-carboxamide
项目整合开发状态: Biological Testing
项目研究机构: Corvas (Orig...
参考文献标题:Exploration solid-phase synthesis of factor Xa inhibitors: Discovery and application of P3-heterocyclic amides as novel types of non-basic arginine surrogates
文献作者:Ho,J.Z.; Levy,O.E.; Gibson,T.S.; Nguyen,K.; Semple,J.E.
参考来源:Bioorg Med Chem Lett 1999,9(24),3459

新产品编号:1753365

Chemical Name: 2-(2-Adamantyl)piperidine
项目整合开发状态: Biological Testing
项目研究机构: National Hellenic Research Foundation (Originator), Rega Institute for Medical Research (Originator), University of ...
参考文献标题:Synthesis of 2-(2-adamantyl)piperidines and structure anti-influenza virus a activity relationship study using a combination of NMR spectroscopy and molecular modeling
文献作者:Kolocouris,A.; Tataridis,D.; Fytas,G.; Mavromoustalkos,T.; Foscolos,G.B.; Kolocouris,N.; De Clercq,E.
参考来源:Bioorg Med Chem Lett 1999,9(24),3465

Piperacillin

Chemical Name: 4-Ethyl-2,3-dioxopiperazinecarbonylampicillin; 6-D-(-)-alpha-(4-Ethyl-2,3-dioxo-1-piperazinylcarbonylamino)-alpha-phenylacetamidopenicillanic; (2S,5R,6R)-6-[(R)-2-(4-Ethyl-2,3-dioxo-1-p...
参考文献标题:Piperacillin
文献作者:Loren,J.G.; Casta馿r,J.
参考来源:Drugs Fut 1978,3(11),829

新产品编号:1754947

Chemical Name: 4-(3-Fluorophenyl)-2-hydroxy-4-oxobut-2(Z)-enoic acid methyl ester
项目整合开发状态: Biological Testing
项目研究机构: GlaxoSmithKline (Originator)
合成路线:By condensation of 3-chloroacetophenon...
参考文献标题:Synthesis and SAR of 4-aryl-2-hydroxy-4-oxobut-2-enoic acids esters and 2-amino-4-aryl-4-oxobut-2-enoic acids and esters: Potent inhibitors of kynurenine-3-hydroxylase as potential neuroprotective agents
文献作者:Drysdale,M.J.; Hind,S.L.; Janssen,M.; Reinhard,J.F.Jr.
参考来源:J Med Chem 2000,43(1),123

新产品编号:1756529

Chemical Name: 5-[2-(Ethylsulfonyloxy)-1,3-dioxo-2,3-dihydro-1H-isoindol-5-ylamino]-5-oxopentanoic acid methyl ester
项目整合开发状态: Biological Testing
项目研究机构: State University of New Jersey (Originat...
参考文献标题:6-Acylamino-2-[(alkylsulfonyl)oxy]-1H-isoindole-1,3-dione mechanism-based inhibitors of human leukocyte elastase
文献作者:Kerrigan,J.E.; Walters,M.C.; Forrester,K.J.; Crowder,J.B.; Christopher,L.J.
参考来源:Bioorg Med Chem Lett 2000,10(1),27

新产品编号:1758111

Chemical Name: N-[1(S)-[N-[1(S)-[N-[1(S)-(1,3-Benzothiazol-2-yl)carbonyl-2-[2-oxopyrrolidin-3(S)-yl]ethyl]carbamoyl]-2-(4-fluorophenyl)ethyl]carbamoyl]-2-methylpropyl]-5-methylisoxazole-3-carboxamide<...
参考文献标题:Structure-based design of ketone-containing,tripeptidyl human rhinovirus 3C protease inhibitors
文献作者:Dragovich,P.S.; Zhou,R.; Webber,S.E.; Prins,T.J.; Kwok,A.K.; Okano,K.; Fuhrman,S.A.; Zalman,L.S.; Maldonado,F.C.; Brown,E.L.; Meador,J.W.3rd.; Patick,A.K.; Ford,C.E.; Brothers,M.A.; Binford,S.L.; Matthews,D.A.; Ferre,R.A.; Worland,S.T.
参考来源:Bioorg Med Chem Lett 2000,10(1),45

新产品编号:1759693

Chemical Name: 2,4-Dihydroxy-3,6-dimethylbenzoic acid 4-(ethoxycarbonyl)-3-hydroxy-2,5-dimethylphenyl ester
项目整合开发状态: Biological Testing
项目研究机构: Universit鋞 Regensburg (Originator), Westf鋖ische W...
参考文献标题:Depsides as non-redox inhibitors of leukotriene B4 biosynthesis and HaCaT cell growth.1.Novel analogues of barbatic and diffractaic acid
文献作者:Kumar,S.; M黮ler,K.
参考来源:Eur J Med Chem 1999,34(12),1035

新产品编号:1761275

Chemical Name: N-[2-(Diethylamino)ethyl]-2-(4-oxo-1,2,3-benzotriazin-3-yl)acetamide
项目整合开发状态: Preclinical
项目研究机构: Universit?degli Studi di Napoli (Originator)
合成路线:Condensation of 1,2,3-benzo...
参考文献标题:Preparation and local anaesthetic activity of benzotriazinone and benzoyltriazole derivatives
文献作者:Caliendo,G.; De Nucci,G.; Meli,R.; Mattace Raso,G.; Fiorino,F.; Perissutti,E.; Zanesco,A.; Grieco,P.; Santagada,V.
参考来源:Eur J Med Chem 1999,34(12),1043

新产品编号:1762857

Chemical Name: (?-N-[2-(7-Methoxynaphthalen-1-yl)propyl]butyramide
项目整合开发状态: Biological Testing
项目研究机构: CNRS (Originator)
合成路线:Alkylation of (7-methoxy-1-naphthyl)acetonitrile (I) with iodome...
参考文献标题:Synthesis of beta-substituted naphth-1-yl ethylamido derivatives as new melatoninergic agonists
文献作者:Math?Allainmat,M.; le Gall,M.; Jellimann,C.; Andrieux,J.; Langlois,M.
参考来源:Bioorg Med Chem 1999,7(12),2945