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

MRS-2286

Chemical Name: 2-[2-[2-Chloro-6-(methylamino)purin-9-yl]ethyl]propane-1,3-diol bis(monophosphate) tetraammonium salt
项目整合开发状态: Biological Testing
项目研究机构: National Institutes of Health (Originato...
参考文献标题:Acyclic analogues of deoxyadenosine 3',5'-bisphosphates as P2Y1 receptor antagonists
文献作者:Kim,Y.C.; Gallo-Rodriguez,C.; Jang,S.Y.; Nandanan,E.; Adams,M.; Harden,T.K.; Boyer,J.L.; Jacobson,K.A.
参考来源:J Med Chem 2000,43(4),746

BAY-41-8543

Chemical Name: 2-[1-(2-Fluorobenzyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]-5-(4-morpholinyl)pyrimidine-4,6-diamine
项目整合开发状态: Preclinical
项目研究机构: Bayer (Originator)
合成路线:The condensation between 2-f...
参考文献标题:Substd.pyrazolo derivs.condensed with six-membered heterocyclic rings
文献作者:Hter,J.; Stasch,J.-P.; Dembowsky,K.; Perzborn,E.; Straub,A.; Feurer,A.; Alonso-Alija,C.; Stahl,E.(Bayer AG)
参考来源:DE 19834044; EP 1102768; WO 0006569

新产品编号:1807153

Chemical Name: (3bS,4aR)-6-[3-[4-[4-(Acetylamino)-1-methyl-1H-imidazol-2-ylcarboxamido]-1-methyl-1H-pyrrol-2-yl]-2(E)-propenoyl]-2-methyl-8-oxo-1,4,4a,5,6,8-hexahydrocyclopropa[c]pyrrolo[3,2-e]indole-...
参考文献标题:Highly cooperative DNA dialkylation by the homodimer of imidazole - Pyrrole diamide - CPI conjugate with vinyl linker
文献作者:Tao,Z.-F.; et al.
参考来源:J Am Chem Soc 2000,122(8),1602

新产品编号:1808735

Chemical Name: 5-(1-Piperidinyl)-5H-1-benzopyran[4,3-d]pyrimidin-2-amine
项目整合开发状态: Preclinical
项目研究机构: Universit?degli Studi di Genova (Originator), Universit?degli Studi di Parma (Originator) 参考文献标题:Synthesis and pharmacological screening of novel non-acidic gastroprotective antipyretic anti-inflammatory agents with anti-platelet properties.5-Alkyl/cycloalkylamino substituted 2-amino-5H-[1]benzopyrano[4,3-d]pyrimidines
文献作者:Barocelli,E.; Bertoni,S.; Bruno,O.; Ranise,A.; Schenone,S.; Chiavarini,M.; Ballabeni,V.
参考来源:Arzneim-Forsch Drug Res 2000,50(2),140

新产品编号:1810317

Chemical Name: 3-[2-(4-Methoxyphenyl)-2-oxoethyl]-5-(4-oxo-2-phenyl-4H-1-benzopyran-6-ylmethylene)thiazolidine-2,4-dione
项目整合开发状态: Biological Testing
项目研究机构: Ankara 躰iversitesi (Originator)
合...
参考文献标题:Synthesis of 3-substituted phenacyl-5-[2-phenyl-4H-4-oxo-1-benzopyran-6-yl(methylenyl]thiazolidine-2,4-diones and evaluation of their antimicrobial activity
文献作者:Altanlar,N.; Ayhan-Killergil,G.
参考来源:Arzneim-Forsch Drug Res 2000,50(2),154

Nafoxidine hydrochloride

Chemical Name: 1-[2-[4-(6-Methoxy-2-phenyl-3,4-dihydronaphthalen-1-yl)phenoxy]ethyl]pyrrolidine hydrochloride
项目整合开发状态: Not Determined
项目研究机构: Pfizer (Originator)
合成路线:The condensation of 3-m...
参考文献标题:Nafoxidine
文献作者:Thorpe,P.; Casta馿r,J.
参考来源:Drugs Fut 1978,3(3),211

新产品编号:1811899

Chemical Name: 4-[2-[3-[2-[2-(3-Hydroxyphenyl)ethyl]benzyloxy]-5-(isopropoxy)phenoxy]ethyl]benzamidine
项目整合开发状态: Biological Testing
项目研究机构: Pfizer (Originator)
合成路线:Addition of hydroxylamine ...
参考文献标题:Design and biological evaluation of non-peptide analogues of omega-conotoxin MVIIA
文献作者:Menzler,S.; Bikker,J.A.; Suman-Chauhan,N.; Horwell,D.C.
参考来源:Bioorg Med Chem Lett 2000,10(4),345

新产品编号:1813481

Chemical Name: 8-Chloro-6-methyl-2,3,5,6-tetrahydro-1H-benzo[c]quinolizin-3-one
项目整合开发状态: Biological Testing
项目研究机构: Universit?degli Studi di Firenze (Originator)
合成路线:Lactam (I) was protecte...
参考文献标题:Synthesis of 8-chloro-benzo[c]quinolizin-3-ones as potent and selective inhibitors of human steroid 5alpha-reductase 1
文献作者:Guarna,A.; Occhiato,E.G.; Scarpi,D.; Zorn,C.; Danza,G.; Comerci,A.; Mancina,R.; Serio,M.
参考来源:Bioorg Med Chem Lett 2000,10(4),353

新产品编号:1815063

Chemical Name: 2,5-Bis(1-methyl-1H-indol-3-yl)pyrazine
项目整合开发状态: Biological Testing
项目研究机构: Chinese Academy of Sciences (Originator)
合成路线:Reaction of indole (I) with chloroacetyl chloride (II...
参考文献标题:Syntheses and cytotoxicity evaluation of bis(indolyl)thiazole,bis(indolyl)pyrazinone and bis(indolyl)pyrazine: Analogues of cytotoxic marine bis(indole) alkaloid
文献作者:Jiang,B.; Gu,X.H.
参考来源:Bioorg Med Chem 2000,8(2),363

新产品编号:1816645

Chemical Name: 3,6-Di(1H-indol-3-yl)-1,2-dihydropyrazin-2-one
项目整合开发状态: Biological Testing
项目研究机构: Chinese Academy of Sciences (Originator)
合成路线:Reaction of indole (I) with chloroacetyl chlor...
参考文献标题:Syntheses and cytotoxicity evaluation of bis(indolyl)thiazole,bis(indolyl)pyrazinone and bis(indolyl)pyrazine: Analogues of cytotoxic marine bis(indole) alkaloid
文献作者:Jiang,B.; Gu,X.H.
参考来源:Bioorg Med Chem 2000,8(2),363