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:1737545

Chemical Name: 8-Chloro-3-(2-propynyloxycarbonyl)pyrazolo[5,1-c][1,2,4]benzotriazine 5-oxide
项目整合开发状态: Preclinical
项目研究机构: Universit?degli Studi di Firenze (Originator), Universit?degli Studi di...
参考文献标题:Benzodiazepine receptor (BZR) ligands.5.New 3-alkyloxycarbonyl-,3-cyclo-alkyloxycarbonyl-,3-aryloxy-carbonylderivatives of pyrazolo [5,1-c][1,2,4]benzotriazine 5-oxides: A study on the 3-ester function modification
文献作者:Costa,B.; Ciciani,G.; Costanzo,A.; Ipponi,A.; Martini,C.; Bruni,F.; Guerrini,G.; Selleri,S.; Lucacchini,A.; Aiello,M.
参考来源:Med Chem Res 1999,9(5),322

新产品编号:1739127

Chemical Name: 8-Chloro-3-(benzyloxycarbonyl)pyrazolo[5,1-c][1,2,4]benzotriazine 5-oxide
项目整合开发状态: Preclinical
项目研究机构: Universit?degli Studi di Firenze (Originator), Universit?degli Studi di Pis...
参考文献标题:Benzodiazepine receptor (BZR) ligands.5.New 3-alkyloxycarbonyl-,3-cyclo-alkyloxycarbonyl-,3-aryloxy-carbonylderivatives of pyrazolo [5,1-c][1,2,4]benzotriazine 5-oxides: A study on the 3-ester function modification
文献作者:Costa,B.; Ciciani,G.; Costanzo,A.; Ipponi,A.; Martini,C.; Bruni,F.; Guerrini,G.; Selleri,S.; Lucacchini,A.; Aiello,M.
参考来源:Med Chem Res 1999,9(5),322

新产品编号:1740709

Chemical Name: N1,N1-Dimethyl-N3-[4-(2-phenylvinyl)pyrrolo[1,2-a]quinoxalin-1-ylmethyl]propane-1,3-diamine trioxalate
项目整合开发状态: Biological Testing
项目研究机构: INSERM (Originator), Servier (Originato...
参考文献标题:Synthesis of new pyrrolo[1,2-a]quinoxalines: Potential non-peptide glucagon receptor antagonists
文献作者:Guillon,J.; Rault,S.; Kervran,A.; Renard,P.; Manechez,D.; Pfeiffer,B.; Dallemagne,P.
参考来源:Eur J Med Chem 1998,33(4),293

新产品编号:1742291

Chemical Name: (1R,2R,3R,5S)-3-(4-Methylphenyl)-8-(2-phenylethyl)-2-phenyl-8-azabicyclo[3.2.1]octane
项目整合开发状态: Biological Testing
项目研究机构: Georgetown University (Originator), UT Medical Branch at...
参考文献标题:Synthesis and biological properties of new 2beta-alkyl- and 2beta-aryl-3-(substituted phenyl)tropane derivatives: Stereochemical effect of C-3 on affinity and selectivity for neuronal dopamine and serotonin transporters
文献作者:Kozikowski,A.P.; Araldi,G.L.; Prakash,K.R.; Zhang,M.; Johnson,K.M.
参考来源:J Med Chem 1998,41(25),4973

新产品编号:1743873

Chemical Name: (-)-4-[N-[1-Allyl-3(S)-methylpiperidin-4(R)-yl]-N-phenylamino]-N,N-diethylbenzamide
项目整合开发状态: Biological Testing
项目研究机构: National Institute on Drug Abuse (Originator), Research Tr...
参考文献标题:(?-4-[(N-Allyl-cis-3-methyl-4-piperidinyl)phenylamino]-N,N-diethylbenzamide displays selective binding for the delta opioid receptor
文献作者:Thomas,J.B.; Herault,X.M.; Rothman,R.B.; Burges,J.P.; Mascarella,S.W.; Xu,H.; Horel,R.B.; Dersch,C.M.; Carroll,F.I.
参考来源:Bioorg Med Chem Lett 1999,9(20),3053

新产品编号:1745455

Chemical Name: 2-Methyl-6-(2-methoxyphenyl)-3-nitro-4,5,6,7-tetrahydropyrazolo[1,5-d][1,2,4]triazine-4,7-dione
项目整合开发状态: Preclinical
项目研究机构: Universit?di Ferrara (Originator)
合成路线:Treatment o...
参考文献标题:1H-Pyrazolo[2,3-d][1,2,4]triazine-3,7-diones as a new class of human leukocyte elastase inhibitors
文献作者:Baraldi,P.G.; et al.
参考来源:Arzneim-Forsch Drug Res 1999,49(12),997

新产品编号:1747037

Chemical Name: (3R,5aS,6R,8aS,9R,10R,12R,12aR)-10-[2-(2-Fluorobenzyloxy)ethyl]-3,6,9-trimethylperhydro-3,12-epoxypyrano[4,3-j]-1,2-benzodioxepine; 10beta-[2-(2-Fluorobenzyloxy)ethyl]-10-deoxoartemisin...
参考文献标题:Novel,potent,semisynthetic antimalarial carba analogues of the first-generation 1,2,4-trioxane artemether
文献作者:O'Neill,P.M.; Searle,N.L.; Kan,K.W.; Storr,R.C.; Maggs,J.L.; Ward,S.A.; Raynes,K.; Park,K.
参考来源:J Med Chem 1999,42(26),5487

AR-0598

Chemical Name: trans-3-[4-(5-Amidino-1-benzofuran-2-ylcarboxamido)cyclohexyl]propionic acid ethyl ester
项目整合开发状态: Preclinical
项目研究机构: Mitsubishi Pharma (Originator)
合成路线:Selective O-alkylatio...
参考文献标题:Novel fused-ring carboxylic acid cpds.or salt thereof,and medicinal use thereof
文献作者:Ono,S.; Yoshida,T.; Ashimori,A.; Kosaka,K.; Okada,T.; Maeda,K.; Eda,M.; Mori,F.; Inoue,Y.; Ebisu,H.; Imada,T.; Ikegawa,R.; Wang,F.; Nakamura,N.(Welfide Corporation)
参考来源:EP 0712844; JP 1996053398; JP 1996231548; US 5635527; US 5753670; WO 9533720

新产品编号:1748619

Chemical Name: 3,4,5-Trihydroxybenzoic acid 2(R)-(3,4-dihydroxyphenyl)-5,7-dihydroxy-4(S)-[2(R)-(3,4-dihydroxyphenyl)-5,7-dihydroxy-3(R)-(3,4,5-trihydrobenzoyloxy)-3,4-dihydro-2H-1-benzopyran-8-yl]-3,...
参考文献标题:Synthetic methods for polyphenols
文献作者:Lippman,M.E.; Kozikowski,A.P.; Tueckmantel,W.; Romanczyk,L.J.Jr.(Mars,Inc.)
参考来源:WO 9919319

ABH

Chemical Name: 2(S)-Amino-6-(borono)hexanoic acid
项目整合开发状态: Preclinical
项目研究机构: Boston University (Originator), Temple University (Originator), University of Pennsylvania (Originator)
合成路线:Th...
参考文献标题:Inhibition of Mn2+2-arginase by borate leads to the design of a transition state analogue inhibitor,2(S)-amino-6-boronohexanoic acid
文献作者:Ash,D.E.; Carroll,P.J.; Baggio,R.; Cavalli,R.C.; Christianson,D.W.; Kanyo,Z.F.; Elbaum,D.
参考来源:J Am Chem Soc 1997,119(34),8107