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:2286499

Chemical Name: 2'-Deoxy-3'-O-[4-[2-[2-(2-hydroxyethoxy)ethoxy]ethoxy]-4-oxobutyryl]-5-iodouridine
项目整合开发状态: Preclinical
项目研究机构: Universit?degli Studi di Catania (Originator), Universit?degli Stu...
参考文献标题:New oligoethylene ester derivatives of 5-iodo-2'-deoxyuridine as dermal prodrugs: Synthesis,physicochemical properties,and skin permeation studies
文献作者:Bonina,F.P.; Rimoli,M.G.; Avallone,L.; Barbato,F.; Amato,M.; Puglia,C.; Ricci,M.; De Caprariis,P.
参考来源:J Pharm Sci 2002,91(1),171

新产品编号:2288081

Chemical Name: N-[4-(2-Benzothiazolyl)phenyl]-N-[11C]methylamine
项目整合开发状态: Preclinical
项目研究机构: University of Pittsburgh (Originator)
合成路线:Condensation of 2-aminothiophenol (I) with 4-nitroben...
参考文献标题:Thioflavin derivs.for use in antemortem diagnosis of Alzheimer's disease and in vivo imaging and prevention of amyloid deposition
文献作者:Wang,Y.; Klunk,W.E.; Mathis,C.A.Jr.(University of Pittsburgh)
参考来源:WO 0216333

LM-1685

Chemical Name: 1-(4-Chlorobenzyl)-5-(methylsulfonyl)-1H-indole-2-carboxylic acid methyl ester
项目整合开发状态: Biological Testing
项目研究机构: Menarini (Originator)
合成路线:The title compound was obtained b...
参考文献标题:Identification of novel cyclooxygenase-2 selective inhibitors using pharmacophore models
文献作者:Palomer,A.; Cabr? F.; Pascual,J.; Campos,J.; Trujillo,M.A.; Entrena,A.; Gallo,M.A.; Garc�? L.; Maule�? D.; Espinosa,A.
参考来源:J Med Chem 2002,45(7),1402

Serofendic acid

Chemical Name: (4beta,8alpha,10alpha,15beta)-15-Hydroxy-17-(methylsulfinyl)atisan-18-oic acid
项目整合开发状态: Biological Testing
项目研究机构: Eisai (Originator)
合成路线:Serofendic acid has been synthesized...
参考文献标题:Isolation of a diterpenoid substance with potent neuroprotective activity from fetal calf serum
文献作者:Kume,T.; Asai,N.; Nishikawa,H.; Mano,N.; Terauchi,T.; Taguchi,R.; Shirakawa,H.; Osakada,F.; Mori,H.; Asakawa,N.; Yonaga,M.; Nishizawa,Y.; Sugimoto,H.; Shimohama,S.; Katsuki,H.; Kaneko,S.; Akaike,A.
参考来源:Proc Natl Acad Sci USA 2002,99(5),3288

CHIR-200131

Chemical Name: 4-Amino-3-[5-[3(S)-(dimethylamino)pyrrolidin-1-yl]benzimidazol-2-yl]-1,2-dihydroquinolin-2-one
项目整合开发状态: Preclinical
项目研究机构: Chiron (Originator)
合成路线:The cyclization of the phe...
参考文献标题:Quinolinone derivs.
文献作者:Harris,A.; Renhowe,P.; Machajewski,T.; Shafer,C.; Wernette-Hammond,M.-E.; Pecchi,S.; Taylor,C.; McCrea,B.; McBride,C.; Jazan,E.(Chiron Corp.)
参考来源:WO 0222598

A-289099

Chemical Name: 1-Methyl-5-[5(S)-(3,4,5-trimethoxyphenyl)-4,5-dihydrooxazol-2-yl]-1H-indole
项目整合开发状态: Preclinical
项目研究机构: Abbott (Originator)
合成路线:Enantioselective dihydroxylation of styrene (...
参考文献标题:Synthesis and biological evaluation of 2-indolyloxazolines as a new class of tubulin polymerization inhibitors.Discovery of A-289099 as an orally active antitumor agent
文献作者:Li,Q.; Woods,K.W.; Claiborne,A.; Gwaltney,S.L.II; Barr,K.J.; Liu,G.; Gehrke,L.; Credo,R.B.; Hui,Y.H.; Lee,J.; Warner,R.B.; Kovar,P.; Nukkala,M.A.; Zielinski,N.A.; Tahir,S.K.; Fitzgerald,M.; Kim,K.H.; Marsh,K.; Frost,D.; et al.
参考来源:Bioorg Med Chem Lett 2002,12(3),465

新产品编号:2289663

Chemical Name: N-Methyl-N-[2-[2-[2-(methylamino)vinyl]-4-[1-methyl-4-(3,4,5-trimethoxyphenyl)-1H-imidazol-5-yl]phenyl]vinyl]amine hydrochloride
项目整合开发状态: Preclinical
项目研究机构: Abbott (Originator)<...
参考文献标题:Potent,orally active heterocycle-based combretastatin A-4 analogues: Synthesis,structure-activity relationship,pharmacokinetics,and in vivo antitumor activity evaluation
文献作者:Wang,L.; Woods,K.W.; Li,Q.; Barr,K.J.; McCroskey,R.M.; Hannick,S.M.; Gherke,L.; Credo,R.B.; Hui,Y.H.; Marsch,K.; Warner,R.; Lee,J.Y.; Zielinski-Mozng,N.; Frost,D.; Rosenberg,S.H.; Sham,H.L.
参考来源:J Med Chem 2002,45(8),1697

新产品编号:2291245

Chemical Name: N5-(2-Carboxybenzoyl)-N2-[4-[2-(2,4-diaminoquinazolin-6-yl)ethyl]benzoyl]-L-ornithine
项目整合开发状态: Biological Testing
项目研究机构: Dana-Farber Cancer Institute (Originator), Harvard Medic...
参考文献标题:Synthesis and in vitro antitumor activity of new deaza analogues of the nonpolyglutamatable antifolate Nalpha-(4-amino-4-deoxypteroyl)-Nalpha-hemiphtaloyl-L-ornithine (PT523)
文献作者:Vaidya,C.M.; Wright,J.E.; Rosowsky,A.
参考来源:J Med Chem 2002,45(8),1690

新产品编号:2292827

Chemical Name: 1-[5-(Biphenyl-4-yloxy)pentyl]-3-(4-pyridyl)imidazolidin-2-one
项目整合开发状态: Biological Testing
项目研究机构: National Health Research Institutes (Originator)
合成路线:The reaction of pyridi...
参考文献标题:Imidazolidinone cpds.
文献作者:Hsu,M.-C.; Li,W.-T.; Chang,C.-M.; Shia,K.-S.; Shih,S.-R.; Chern,J.-H.; Chen,S.-J.(National Health Research Institutes)
参考来源:US 2003087936; US 6706739

BH-1625(NOH)TB-2

Chemical Name: (+)-1alpha-Hydroxy-25-(hydroxyimino)-26,26,26-trimethyl-27-norvitamin D3
项目整合开发状态: Preclinical
项目研究机构: Johns Hopkins University (Originator), M.D. Anderson Cancer Center (Originat...
参考文献标题:Conceptually new low-calcemic oxime analogues of the hormone 1alpha,25-dihydroxyvitamin D3: Synthesis and biological testing
文献作者:Posner,G.H.; Halford,B.A.; Peleg,S.; Dolan,P.; Kensler,T.W.
参考来源:J Med Chem 2002,45(8),1723