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:2042871

Chemical Name: 1-[4-[4-[1(S)-[4-(1,3-Benzodioxol-5-ylmethyl)phenyl]ethyl]-3(S)-methylpiperazin-1-yl]piperidin-1-yl]-1-(2,6-dimethylphenyl)methanone
项目整合开发状态: Biological Testing
项目研究机构: Schering-...
参考文献标题:Piperazine-based CCR5 antagonists as HIV-1 inhibitors.I: 2(S)-methyl piperazine as a key pharmacophore element
文献作者:Tagat,J.R.; McCombie,S.W.; Steensma,R.W.; Lin,S.; Nazareno,D.V.; Baroudy,B.M.; Vantuno,N.; Xu,S.; Liu,J.
参考来源:Bioorg Med Chem Lett 2001,11(16),2143

新产品编号:2044453

Chemical Name: 3-Methyl-2-[N-methyl-N-[4-(pyridin-4-yloxy)phenylsulfonyl]amino]benzohydroxamic acid
项目整合开发状态: Preclinical
项目研究机构: Wyeth Pharmaceuticals (Originator)
合成路线:Condensation of 4-flu...
参考文献标题:Preparation and use of orthosulfonamido aryl hydroxamic acids as matrix metalloproteinase and TACE inhibitors
文献作者:Gu,Y.; Nelson,F.C.; Zask,A.; Du,M.T.; Levin,J.I.; Venkatesan,M.(American Cyanamid Co.)
参考来源:US 5929097

新产品编号:2046035

Chemical Name: O15-[(6R,7R)-2-Carboxy-5-oxido-8-oxo-7-(2-phenoxyacetamido)-5-thia-1-azabicyclo[4.2.0]oct-2-en-3-ylmethyl]retinoic acid; Retinoic acid (6R,7R)-4-carboxy-1-oxo-7-(2-phenoxyacetamido)ceph...
参考文献标题:Design and synthesis of a cephalosporin-retinoic acid prodrug activated by a monoclonal antibody-beta-lactamese conjugate
文献作者:Hakimelahi,G.H.; Ly,T.W.; Yu,S.F.; Zakerinia,M.; Khalafi-Nezhad,A.; Soltani,M.N.; Gorgani,M.N.; Chadegani,A.R.; Moosavi-Movahedi,A.A.
参考来源:Bioorg Med Chem 2001,9(8),2139

新产品编号:2047617

Chemical Name: 2,3-Dimethyl-5-[4-(methylsulfonyl)phenyl]-4-phenyl-2,3-dihydroisoxazole
项目整合开发状态: Preclinical
项目研究机构: University of Alberta (Originator)
合成路线:The title compound was prepared fr...
参考文献标题:Design and synthesis of 4,5-diphenyl-4-isoxazolines: Novel inhibitors of cyclooxygenase-2 with analgesic and antiinflammatory activity
文献作者:Habeeb,A.G.; Praveen Rao,P.N.; Knaus,E.E.
参考来源:J Med Chem 2001,44(18),2921

S-35031

Chemical Name: 3-[6-(4-Chlorophenylsulfonamido)-3-[2-(4-methylpiperazin-1-yl)phenoxymethyl]-5,6,7,8-tetrahydronaphthalen-1-yl]propionic acid
项目整合开发状态: Preclinical
项目研究机构: Servier (Originator) 参考文献标题:Benzenesulfonamide derivs.,process for their preparation and pharmaceutical compsns.containing them
文献作者:Verbeuren,T.; Simonet,S.; Descombes,J.-J.; Cimetiere,B.; Lavielle,G.(ADIR et Cie.)
参考来源:EP 1118610; FR 2803848; JP 2001226353

2,7-Dibromocryptolepine

Chemical Name: 2,7-Dibromo-5-methyl-10H-indolo[3,2-b]quinolin-5-ium iodide
项目整合开发状态: Preclinical
项目研究机构: London School Hygiene Tropical Medicine (Originator), University of Bradford (Originator)...
参考文献标题:Synthesis and evaluation of cryptolepine analogues for their potential as new antimalarial agents
文献作者:Wright,C.W.; Addae-Kyereme,J.; Breen,A.G.; Brown,J.E.; Cox,M.F.; Croft,S.L.; Gokcek,Y.; Kendrick,H.; Phillips,R.M.; Pollet,P.L.
参考来源:J Med Chem 2001,44(19),3187

GW-569180A

Chemical Name: N-[1-[2(R)-Hydroxy-2-phenylethyl]-5-(4-methylpiperazin-1-ylmethyl)-1H-benzimidazol-2-yl]-4-methoxybenzamide mesylate
项目整合开发状态: Preclinical
项目研究机构: GlaxoSmithKline (Originator)
...
参考文献标题:2-Aminobenzimidazoles: A class of orally bioavailable and brain permeable neuropeptide YY5 antagonists
文献作者:Heyer,D.; et al.
参考来源:222nd ACS Natl Meet (Aug 26 2001,Chicago) 2001,Abst MEDI 284

新产品编号:2049199

Chemical Name: N,N'-Bis[3-(biphenyl-3-ylmethylamino)propyl]heptane-1,7-diamine
项目整合开发状态: Preclinical
项目研究机构: Albert Einstein College of Medicine (Originator), Johns Hopkins University (Originato...
参考文献标题:Novel alkylpolyamide analogues that possess both antitrypanosomal and antimicrosporidial activity
文献作者:Zou,Y.; Wu,Z.; Sirisoma,N.; Woster,P,M.; Casero,R.A.Jr.; Weiss,L.M.; Rattendi,D.; Lane,S.; Bacchi,C.J.
参考来源:Bioorg Med Chem Lett 2001,11(12),1613

新产品编号:2050781

Chemical Name: 2-(2,6-Dichlorophenyl)-3-(6-methylpyridin-2-yl)thiazolidin-4-one
项目整合开发状态: Biological Testing
项目研究机构: Rega Institute for Medical Research (Originator), Universit?degli Studi di Ca...
参考文献标题:Discovery of 2,3-diaryl-1,3-thiazolidin-4-ones as potent anti-HIV-1 agents
文献作者:Barreca,M.L.; Chimirri,A.; De Luca,L.; Monforte,A.M.; Monforte,P.; Rao,A.; Zappala,M.; Balzarini,J.; De Clercq,E.; Pannecouque,C.; Witvrouw,M.
参考来源:Bioorg Med Chem Lett 2001,11(13),1793

新产品编号:2052363

Chemical Name: N-[2-(2-Benzoxazolyl)tetrahydrofuran-2-ylcarbonyl]-4-(2,6-dimethoxyphenyl)-L-phenylalanine
项目整合开发状态: Preclinical
项目研究机构: Merck & Co. (Originator)
合成路线:N-Boc-L-tyrosine tert-but...
参考文献标题:Heterocycle amides as cell adhesion inhibitors
文献作者:Yang,G.X.; Hagmann,W.K.; Doherty,G.; Chang,L.L.; Delaszlo,S.E.(Merck & Co.,Inc.)
参考来源:WO 0112183