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

BBR-2550, NSC-637823-T/1, Na[trans-RuCl4(DMSO)Im].2DMSO

Chemical Name: trans-(Dimethylsulfoxide)(imidazole)tetrachlororuthenium(III) sodium salt bis(dimethylsulfoxide)
项目整合开发状态: Preclinical
项目研究机构: Roche (Originator)
合成路线:The title complex can be ...
参考文献标题:Synthesis,molecular structure and chemical behavior of hydrogen trans-bis(DMSO)tetrachlororuthenate(III) and mer-trichlorotris(DMSO)ruthenium(III): The first full characterized chloride-dimethyl sulfoxide-ruthenium(III) complexes
文献作者:Attia,W.M.; Calligaris,M.; Costa,G.; Balducci,G.; Mestroni,G.; Alessio,E.
参考来源:Inorg Chem 1991,30(4),609-18

WAY-121006

Chemical Name: 2-[2-Fluoro-4'-(quinolin-2-ylmethoxy)biphenyl-4-yl]acetic acid
项目整合开发状态: Biological Testing
项目研究机构: Wyeth Pharmaceuticals (Originator)
合成路线:By condensation of 1-naphthol (I) wi...
参考文献标题:Conversion of a cyclooxygenase (CO) inhibitor into a 5-lipoxygenase (LO) inhibitor - A general route to novel antiinflammatory and antiallergy drugs
文献作者:Kreft,A.F.; Failli,A.; Musser,J.H.; et al.
参考来源:Drugs Exp Clin Res 1991,17381-387

ES-242-5

Chemical Name: 7,7',9,9'-Tetramethoxy-3,3'-dimethyl-5,5'-bi(3,4-dihydro-1H-naphtho[2,3-c]pyran)-4,10,10'-triol
项目整合开发状态: Biological Testing
项目研究机构: Kyowa Hakko (Originator)
合成路线:The title com...
参考文献标题:Synthesis and biological evaluation of the analogs of bioxanthracenes ES-242s,N-methyl-D-aspartate antagonists
文献作者:Tatsuta,K.; Yamazaki,T.; Yoshimoto,T.
参考来源:J Antibiot 1998,51(3),383

新产品编号:1016153

Chemical Name: 9-Cyclopropyl-6,8-difluoro-7-piperazino-2,3,4,9-tetrahydroisothiazolo[5,4-b]quinoline-3,4-dione methanesulfonate
项目整合开发状态: Biological Testing
项目研究机构: Abbott (Originator)
合成路线:T...
参考文献标题:Sulfonylurea signal transduction
文献作者:Aquilar-Bryan,L.; Bryan,J.; Boyd,A.E.III; et al.
参考来源:Recent Prog Horm Res 1991,47299-317

(-)-Salmeterol, (R)-Salmeterol

Chemical Name: (R)-(-)-2-(Hydroxymethyl)-4-[1-hydroxy-2-[6-(4-phenylbutoxy)hexylamino]ethyl]phenol; (R)-(-)-2-Hydroxy-5-[1-hydroxy-2-[6-(4-phenylbutoxy)hexylamino]ethyl]benzyl alcohol
项目整合开发状态: Bio...
参考文献标题:Phenethanolamine cpds.
文献作者:Evans,B.(GlaxoSmithKline plc)
参考来源:AU 9163901; EP 0422889; JP 1991133946

BBE

Chemical Name: trans-1,2-Bis(5-amidino-2-benzimidazolyl)ethene tetrahydrochloride; (E)-2,2'-Vinylenebis(benzimidazole-5-carboxamidine) tetrahydrochloride
项目整合开发状态: Preclinical
项目研究机构: University...
参考文献标题:Diarylamidine derivatives with one or both of the aryl moieties consisting of an indole or indole-like ring.Inhibitors of arginine-specific esteroproteases
文献作者:Tidwell,R.R.; Geratz,J.D.; Dann,O.; Volz,G.; Zeh,D.; Loewe,H.
参考来源:J Med Chem 1978,21(7),613-23

新产品编号:1017735

Chemical Name: 2,3,4-O-Triacetyl-1-O-(dl-alpha-tocopheryl)-beta-D-glucopyranuronic acid methyl ester; 2,3,4-O-Triacetyl-1-O-[dl-2,5,7,8-tetramethyl-2-(4,8,12-trimethyltridecyl)-2H-3,4-dihydrobenzo[b]p...
参考文献标题:Synthesis and structure activity relationships of anti-inflammatory 9,10-dihydro-9-oxo-2-acridine-alkanoic acids and 4-(2-carboxyphenyl)aminobenzenealkanoic acids
文献作者:Taraporewala,I.B.; Kauffman,J.M.
参考来源:J Pharm Sci 1990,79(2),173

alpha-Methyltryptophan, 1MT

Chemical Name: alpha-Methyl-L-tryptophan; 2(S)-Amino-3-(1H-indol-3-yl)-2-methylpropanoic acid
项目整合开发状态: Clinical
项目研究机构: McGill University (Originator)
合成路线:This compound has been obtained by...
参考文献标题:A facile method for the asymmetric synthesis of alpha-methyltryptophan
文献作者:Zhang,L.J.; Finn,J.M.
参考来源:J Org Chem 1995,60(17),5719

Org-13011

Chemical Name: 1-[4-[4-[4-(Trifluoromethyl)pyridin-2-yl]piperazin-1-yl]butyl]pyrrolidin-2-one fumarate
项目整合开发状态: Phase II
项目研究机构: Akzo Nobel (Originator), Organon (Originator)
合成路线:Alkylation...
参考文献标题:4-[4- or 6-(Trifluoromethyl-2-pyridinyl)]-1-piperazinyl-alkyl substd.lactams
文献作者:Carlier,P.; Combourieu,M.; Poisson,C.; Monteil,A.J.-C.(Akzo Nobel N.V.)
参考来源:EP 0482696; JP 1992282379; US 5180726

SDZ-266336

Chemical Name: (S)-2-[Hydroxy[2-(octadecyloxymethyl)tetrahydrofuran-2-ylmethoxy]phosphinyloxy]-N,N,N-trimethylethylaminium hydroxide inner salt
项目整合开发状态: Biological Testing
项目研究机构: Novartis (Ori...
参考文献标题:Enantiomers of 2-tetrahydrofuran derivs.,intermediates therefor and their preparation
文献作者:Estermann,H.; Houlihan,W.J.; Kapa,P.K.; Underwood,R.L.(Novartis AG; Novartis Deutschland GmbH)
参考来源:EP 0462935; JP 1992270276