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:1202829

Chemical Name:
项目整合开发状态: Preclinical
项目研究机构: St. Marianna University School Med. (Originator)
合成路线:Condensation of trimethylhydroquinone (I) with 4-chloro-1-butanol (II) in the presence of p...
参考文献标题:Synthesis of trimethylhydroquinone derivatives as anti-allergic agents with anti-oxidative actions
文献作者:Kawasaki,N.; Miyataka,H.; Nishiki,M.; Matsumoto,H.; Inagaki,N.; Nagai,H.; Satoh,T.
参考来源:Chem Pharm Bull 1999,47(2),177

DA-3797

Chemical Name:
项目整合开发状态: Biological Testing
项目研究机构:
合成路线:2-Benzyloxyaniline (I) was acylated with N-tert-butoxycarbonyl glycine (II) by means of 1-[3-(dimethylamino)propyl]-3-ethylcarbodiim...
参考文献标题:Synthesis of phenoxyacetic acid derivatives as highly potent antagonists of gastrin/cholecystokinin-B receptors
文献作者:Takeda,Y.; Kawagoe,K.; Yokomizo,A.; Yokomizo,Y.; Hosokami,T.; Ogihara,Y.; Honda,Y.; Yokohama,S.
参考来源:Chem Pharm Bull 1998,46(3),434-444

新产品编号:1204411

Chemical Name:
项目整合开发状态:
项目研究机构:
合成路线:Treatment of L-lyxose (I) with MeOH and H2SO4 afforded a 1:3 mixture of 1-O-methyl lyxopyranose (II) and 1-O-methyl lyxofuranose (III).This mixture wa...
参考文献标题:Design,synthesis,and antiviral activity of alpha-nucleosides: D- and L-isomers of lyxofuranosyl- and (5-deoxylyxofuranosyl) benzimidazoles
文献作者:Migawa,M.; Girardet,J.L.; Walker,J.A,II.; Koszalka,G.W.; Chamberlain,S.D.; Drach,J.C.; Townsend,L.B.
参考来源:J Med Chem 1998,41(8),1242

新产品编号:1205993

Chemical Name:
项目整合开发状态:
项目研究机构:
合成路线:The asymmetric 1,3-dipolar cycloaddition of the nitrile oxide resulting from 4-bromo-N-hydroxybenzenecarboximidoyl chloride (I) to allyl alcohol (II) ...
参考文献标题:Isoxazoline derivs.useful as antimicrobials
文献作者:Barbachyn,M.R.; Thomas,R.C.; Cleek,G.J.(Pharmacia & Upjohn AB)
参考来源:EP 0920421; US 5990136; WO 9807708

新产品编号:1207575

Chemical Name:
项目整合开发状态:
项目研究机构:
合成路线:2'-Deoxyadenosine (I) was protected as the diacetate (II) on treatment with acetic anhydride and a catalytic amount of dimethylaminopyridine.Then,reac...
参考文献标题:Deoxyadenosine bisphosphate derivatives as potent antagonists at P2Y1 receptors
文献作者:Camaioni,E.; Boyer,J.L.; Mohanram,A.; Harden,T.K.; Jacobson,K.A.
参考来源:J Med Chem 1998,41(1),183-190

新产品编号:1209157

Chemical Name:
项目整合开发状态:
项目研究机构:
合成路线:Amine (I) was alkylated with 4-nitrophenethyl bromide (II) in refluxing isopropanol to yield the tertiary amine (III).Hydrogenation of the nitro group...
参考文献标题:Novel antiarrhythmic cpds.
文献作者:Berzsenyi,P.; Druga,A.; P醫falusi,M.; Varga,I.; Rettegi,T.; Barlocco,D.; Moravcsik,I.; M醫yus,P.; Papp,G.; Varr? A.; Cignarella,G.; Simay,A.(Albert Szent-Gy鰎gyi Medical University ; Gyogyszerkutato Intezet Kft.)
参考来源:WO 9929655

新产品编号:1210739

Chemical Name:
项目整合开发状态:
项目研究机构:
合成路线:By chlorination of 2-chloro-2',3'-isopropylidene-N-methoxyadenosine (I) with SOCl2 and pyridine gives the 2,5'-dichloro derivative (II),which is depro...
参考文献标题:Chemical cpds.,their preparation and use
文献作者:Lau,J.; Knutsen,L.J.S.(Novo Nordisk A/S)
参考来源:EP 0719275; JP 1999511436; US 5589467; WO 9507921

新产品编号:1212321

Chemical Name:
项目整合开发状态:
项目研究机构:
合成路线:The reaction of 2,6-dichloro-9-(2',3',5'-tri-O-acetyl-beta-D-ribofuranosyl)-9H-purine (I) with O-methylhydroxylamine in hot dioxane gives 2',3',5'-tri...
参考文献标题:Novel N-alkoxyadenine derivs.acting as cytokine inhibitors
文献作者:Knutsen,L.; Olsen,U.B.; Roberts,S.M.; Varley,D.R.; Bowler,A.N.(Novo Nordisk A/S)
参考来源:WO 9801459

新产品编号:1213903

新产品编号:1215485

Chemical Name:
项目整合开发状态:
项目研究机构:
合成路线:A new synthesis of the title compound,very similar to that already published,is reported:The condensation of 6-(benzyloxy)-2,5,7,8-tetramethyl-3,4-dih...
参考文献标题:Cpds.having antidiabetic,hypolipidemic,antihypertensive properties,process for their preparation and pharmaceutical compsns.containing them
文献作者:Casturi,S.R.; Lohray,V.B.; Kallam,A.R.; Pingali,H.; Ramanujam,R.; Alla,S.R.(Dr.Reddy's Research Foundation)
参考来源:US 5925656