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

Dioscin

Chemical Name: (3beta,25R)-Spirost-5-en-3-yl 6-deoxy-alpha-L-mannopyranosyl-(1--2)-[6-deoxy-alpha-L-mannopyranosyl-(1--4)]-beta-D-glucopyranoside
项目整合开发状态: Biological Testing
项目研究机构:
合成路线:T...
参考文献标题:The synthesis of gracillin and dioscin: Two typical representatives of spirostanol glycosides
文献作者:Zou,C.-C.; Hou,S.-J.; Shi,Y.; Lei,P.-S.; Liang,X.-T.
参考来源:Carbohydr Res 2003,338(8),721

新产品编号:1648953

Chemical Name: N-[3-(4-Methoxyphenyl)-4-oxo-2,4-dihydroindeno[1,2-c]pyrazol-5-yl]urea
项目整合开发状态: Preclinical
项目研究机构: Bristol-Myers Squibb (Originator)
合成路线:Dimethyl 3-nitrophthalate (I) was hy...
参考文献标题:5-Aminoindeno(1,2-c)pyrazol-4-ones as anti-cancer and anti-proliferative agents
文献作者:Yue,E.W.; Carini,D.J.; Nugiel,D.A.; Dimeo,S.V.(DuPont Pharmaceuticals Co.)
参考来源:WO 9954308

新产品编号:1650535

Chemical Name: N-[3-(5-Chloro-3-thienyl)-4-oxo-2,4-dihydroindeno[1,2-c]pyrazol-5-yl]urea
项目整合开发状态: Preclinical
项目研究机构: Bristol-Myers Squibb (Originator)
合成路线:Dimethyl 3-nitrophthalate (I) was...
参考文献标题:5-Aminoindeno(1,2-c)pyrazol-4-ones as anti-cancer and anti-proliferative agents
文献作者:Yue,E.W.; Carini,D.J.; Nugiel,D.A.; Dimeo,S.V.(DuPont Pharmaceuticals Co.)
参考来源:WO 9954308

新产品编号:1652117

Chemical Name: 20(S)-Methoxy-7beta-methyl-4-aza-5alpha-pregn-1-en-3-one
项目整合开发状态: Preclinical
项目研究机构: Merck & Co. (Originator)
合成路线:Pregnenolone acetate (I) was reduced with NaBH4 to give alc...
参考文献标题:3-Oxo-4aza-5alpha-7beta-methylpregnan-20-ethers as inhibitors of human type 1 5alpha-reductase: Synthesis and structure-activity relationship
文献作者:Harris,G.S.; Tolman,R.L.; Ellsworth,K.P.; Rasmusson,G.H.; Chang,B.C.; Patel,G.F.; Bakshi,R.K.
参考来源:218th ACS Natl Meet (Aug 22 1999,New Orleans) 1999,Abst MEDI 226

新产品编号:1653699

Chemical Name: 1-[4-[4-(1H-Imidazol-1-yl)phenoxy]piperidin-1-ylsulfonyl]piperidine-2(R)-carbohydroxamic acid
项目整合开发状态: Biological Testing
项目研究机构: Agouron (Originator), Roche Bioscience (Originat...
参考文献标题:Novel sulfamides and sulfonamide inhibitors of matrix metalloproteases
文献作者:Mitchell,L.J.Jr.; Burke,B.; Dagostino,E.; et al.
参考来源:218th ACS Natl Meet (Aug 22 1999,New Orleans) 1999,Abst MEDI 76

A-241548

Chemical Name: N-(2,3-Dihydroxypropyl)-4-(4-methylphenylsulfanyl)thieno[2,3-c]pyridine-2-carboxamide
项目整合开发状态: Preclinical
项目研究机构: Abbott (Originator), Icos (Codevelopment)
合成路线:The formylati...
参考文献标题:Cell adhesion-inhibiting antiinflammatory cpds.
文献作者:Lartey,K.; Gunawardana,I.W.; Stout,D.M.; Bhatia,P.; Patel,M.V.; Staeger,M.A.; Boyd,S.A.; Mort,N.A.; Zhu,G.-D.; McCarty,C.M.; Stewart,A.O.; Arendsen,D.L.; Condroski,K.R.; Freeman,J.C.(Abbott Laboratories Inc.)
参考来源:WO 9962908

A-252444.0

Chemical Name: 4-(4-Chlorophenoxy)-N-methylthieno[2,3-c]pyridine-2-carboxamide
项目整合开发状态: Preclinical
项目研究机构: Abbott (Originator), Icos (Codevelopment)
合成路线:The formylation of 3,5-dichloropyri...
参考文献标题:Cell adhesion-inhibiting antiinflammatory cpds.
文献作者:Lartey,K.; Gunawardana,I.W.; Stout,D.M.; Bhatia,P.; Patel,M.V.; Staeger,M.A.; Boyd,S.A.; Mort,N.A.; Zhu,G.-D.; McCarty,C.M.; Stewart,A.O.; Arendsen,D.L.; Condroski,K.R.; Freeman,J.C.(Abbott Laboratories Inc.)
参考来源:WO 9962908

新产品编号:1655281

Chemical Name: N2-[4-(4-Bromophenoxy)phenylsulfonyl]-N1-hydroxy-D-tert-leucinamide
项目整合开发状态: Preclinical
项目研究机构: Agouron (Originator)
合成路线:Chlorosulfonation of 4-bromodiphenyl ether (I) in co...
参考文献标题:Metalloproteinase inhibitors,pharmaceutical compsns.containing them and their pharmaceutical uses
文献作者:Abreo,M.A.; Bender,S.L.(Agouron Pharmaceuticals,Inc.)
参考来源:EP 0973748; WO 9843963

新产品编号:1656863

Chemical Name: 2-(4-Bromophenyl)-6-chloro-8-methylquinoline-4-carboxylic acid
项目整合开发状态: Biological Testing
项目研究机构: Cubist (Originator)
合成路线:The title quinoline derivative was prepared by a Pf...
参考文献标题:Structure-activity relationship of quinoline analogs as inhibitors of C.albicans prolyl t-RNA synthetase
文献作者:Hill,J.M.; Kluge,A.F.; Silverman,J.; Yang,Y.; Yu,G.; Finn,J.; Keith,D.; Yu,X.Y.; Gallant,P.
参考来源:218th ACS Natl Meet (Aug 22 1999,New Orleans) 1999,Abst MEDI 289

新产品编号:1658445

Chemical Name: 2-(2',4'-Dichlorobiphenyl-4-yl)-6-fluoroquinoline-4-carboxylic acid
项目整合开发状态: Biological Testing
项目研究机构: Cubist (Originator)
合成路线:The title quinolinecarboxylic acid was synthes...
参考文献标题:Structure-activity relationship of biphenylquinoline analogs as inhbitors of S.aureus methionyl-TRNA synthetase
文献作者:Yu,X.Y.; et al.
参考来源:218th ACS Natl Meet (Aug 22 1999,New Orleans) 1999,Abst MEDI 296