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:1457531

Chemical Name: 2(S)-(6-Methoxynaphthalen-2-yl)propionic acid 2-(6-hydroxy-2,5,7,8-tetramethyl-3,4-dihydro-2H-1-benzopyran-2-yl)ethyl ester
项目整合开发状态: Biological Testing
项目研究机构: Alcon (Originator)...
参考文献标题:Esters and amides of non-steroidal anti-inflammatory carboxylic acids which may be used as anti-oxidants,5-lipoxygenase inhibitors and non-steroidal anti-inflammatory products
文献作者:Hellberg,M.; Graff,G.; Gamache,D.A.; Nixon,J.C.; Garner,W.H.(Alcon Laboratories,Inc.)
参考来源:EP 0799219; JP 1998511663; WO 9620187

新产品编号:1459113

Chemical Name: N-[3-(4-Cyanobenzamido)-2,2-dimethylnonanoyl]-L-phenylalanine ethyl ester
项目整合开发状态: Biological Testing
项目研究机构: Nippon Steel (Originator)
合成路线:The condensation of ethyl isobutyr...
参考文献标题:N-[2,2-Dimethyl-3-(N-(4-cyanobenzoyl)amino)nonanoyl]-L-phenylalanine ethyl ester as a stable ester-type inhibitor of chymotrypsin-like serine proteases: Structural requirements for potent inhibition of alpha-chymotrypsin
文献作者:Iijima,K.; Katada,J.; Yasuda,E.; Uno,I.; Hayashi,Y.
参考来源:J Med Chem 1999,42(2),312

新产品编号:1460695

Chemical Name: 12-[N2-Cyano-N3-(4-pyridinyl)guanidino]dodecylcarbamic acid tert-butyl ester
项目整合开发状态: Biological Testing
项目研究机构: Leo (Originator)
合成路线:The title compound was synthesized by ac...
参考文献标题:Synthesis and positive inotropic effects of 1-acyl-5,6-diethoxy-2-methylthiobenzimidazoles
文献作者:Brukstus,A.; Dauksas,V.; Garaliene,V.; Labanauskas,L.
参考来源:Arzneim-Forsch Drug Res 1998,48(12),1137

新产品编号:1462277

Chemical Name: 4-[2-[1-[bis(4-Propylphenyl)methyl]-1H-benzimidazol-5-ylcarboxamido]phenoxy]butyric acid ethyl ester
项目整合开发状态: Preclinical
项目研究机构: Kyowa Hakko (Originator)
合成路线:The target comp...
参考文献标题:Indole and benzimidazole derivatives as steroid 5alpha-reductase inhibitors in the rat prostate
文献作者:Takami,H.; Kishibayashi,N.; Ishii,A.; Kumazawa,T.
参考来源:Bioorg Med Chem 1998,6(12),2441

VN-2222

Chemical Name: 1-(Benzothien-3-yl)-3-[4-(2-methoxyphenyl)-1-piperazinyl]-1-propanol hydrochloride
项目整合开发状态: Preclinical
项目研究机构: Vita (Originator)
合成路线:Mannich reaction of N-(2-methoxyphenyl)p...
参考文献标题:Cpds.derived from thiophene and benzothiophene,and related utilisation and compsn.
文献作者:Bosch Rovira,A.; Roca Acin,J.; Monge Vega,A.; Del Rio Zambrana,J.; Palop Cubillo,J.A.; Lasheras Aldaz,B.; Del Castillo Nieto,J.C.(Laboratorios Vita,SA)
参考来源:EP 1008594; ES 2128266; JP 2002511883; US 6262056; WO 9902516

Thiarubrine C

Chemical Name: 3-[3(Z),5-hexadien-1-ynyl]-6-(1-propynyl)-1,2-dithiine
项目整合开发状态: Biological Testing
项目研究机构: University of Michigan (Originator)
合成路线:The addition of 2-(trimethylsilyl)ethylmerc...
参考文献标题:Total synthesis and DNA-cleaving properties of thiarubrine C
文献作者:Wang,Y.M.; et al.
参考来源:J Org Chem 1998,63(24),8644

新产品编号:1463859

Chemical Name: 2-(3',5'-Diethoxybiphenyl-4-yl)propionic acid
项目整合开发状态: Biological Testing
项目研究机构: Merck Frosst (Originator)
合成路线:The acylation of 3,5-diethoxyphenol (I) with triflic anhydride...
参考文献标题:Biaryl-acetic acid derivs.and their use as COX-2 inhibitors
文献作者:Black,C.; Leger,S.; Bayly,C.I.; Ouimet,N.; Ouellet,M.; Percival,D.(Merck Frosst Canada Inc.)
参考来源:US 5994379; WO 9941224

新产品编号:1465441

Chemical Name: 2-(3',5'-Diethoxy-2-fluorobiphenyl-4-yl)propionic acid
项目整合开发状态: Biological Testing
项目研究机构: Merck Frosst (Originator)
合成路线:The acylation of 3,5-diethoxyphenol (I) with triflic ...
参考文献标题:Biaryl-acetic acid derivs.and their use as COX-2 inhibitors
文献作者:Black,C.; Leger,S.; Bayly,C.I.; Ouimet,N.; Ouellet,M.; Percival,D.(Merck Frosst Canada Inc.)
参考来源:US 5994379; WO 9941224

新产品编号:1467023

Chemical Name: 2-[4-(2-Methyl-1H-indol-5-yl)phenyl]propionic acid
项目整合开发状态: Biological Testing
项目研究机构: Merck Frosst (Originator)
合成路线:The acylation of 3,5-diethoxyphenol (I) with triflic anhy...
参考文献标题:Biaryl-acetic acid derivs.and their use as COX-2 inhibitors
文献作者:Black,C.; Leger,S.; Bayly,C.I.; Ouimet,N.; Ouellet,M.; Percival,D.(Merck Frosst Canada Inc.)
参考来源:US 5994379; WO 9941224

新产品编号:1468605

Chemical Name: 2-[5-[3-Cyclopentyloxy-4-methoxyphenyl]furan-2-yl]pyridine
项目整合开发状态: Preclinical
项目研究机构: Merck Frosst (Originator)
合成路线:The Grignard reaction of 3-(cyclopentyloxy)-4-methoxyben...
参考文献标题:Aryl furan derivs.as PDE IV inhibitors
文献作者:Young,R.N.; MacDonald,D.; Bayly,C.; Perrier,H.; Han,Y.; Giroux,A.(Merck Frosst Canada Inc.)
参考来源:EP 1021429; US 6020339; WO 9918095