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:1217067

Chemical Name:
项目整合开发状态:
项目研究机构:
合成路线:Addition of ethylmagnesium bromide to 3,4,5-trimethoxybenzaldehyde (I) gave secondary alcohol (II),which was converted into ketone (III) by Swern oxid...
参考文献标题:Potent antimitotic and cell growth inhibitory properties of substituted chalcones
文献作者:Ducki,S.; Forrest,R.; Hadfield,J.A.; Kendall,A.; Lawrence,N.J.; McGown,A.T.; Rennison,D.
参考来源:Bioorg Med Chem Lett 1998,8(9),1051

新产品编号:1218649

Chemical Name:
项目整合开发状态:
项目研究机构:
合成路线:Title compound was prepared by reductive alkylation of 3-phenylpropylamine (I) with 3'-methoxyacetophenone (II) using NaCNBH3 in the presence of titan...
参考文献标题:Calcium receptor active molecules
文献作者:Nemeth,E.F.; Van Wagenen,B.C.; Balandrin,M.F.(NPS Pharmaceuticals,Inc.)
参考来源:WO 9304373

新产品编号:1220231

Chemical Name:
项目整合开发状态: Phase II
项目研究机构:
合成路线:Addition of methylmagnesium iodide to nitrile (I),followed by hydrolytic treatment,provided ketone (II),which was brominated in CHCl3-MeOH to ...
参考文献标题:1-Arylcycloalkyl sulphides,sulphoxides and sulphones for the treatment of depression,anxiety and Parkinson's disease
文献作者:Harris,P.J.; Heal,D.J.(The Boots Company plc)
参考来源:EP 0715620; JP 1996510222; US 5652271; WO 9426704

新产品编号:1221813

Chemical Name:
项目整合开发状态:
项目研究机构:
合成路线:Coupling of isovanillin (I) with 3-hydroxytetrahyrofuran (II) in the presence of triphenyl phosphine and diisopropyl azodicarboxylate yielded the tetr...
参考文献标题:Novel 1,2,4-Triaminobenzene derivs.and process for their preparation
文献作者:Dieter,H.-R.; Engel,J.; Kutscher,B.; Polymeropoulos,E.; Szelenyi,S.; Nickel,B.(Asta Medica AG)
参考来源:DE 4200259; EP 0554543; JP 1993345752; US 5384330

新产品编号:1223395

Chemical Name:
项目整合开发状态:
项目研究机构:
合成路线:This compound has been obtained by two different ways:1) The condensation of 2-bromobenzyl alcohol (I) with cyclohexane-1,4-dione monoethyleneketal (I...
参考文献标题:Spirocyclic dopamine receptor subtype ligands
文献作者:Butler,T.W.; Fliri,A.F.J.(Pfizer Inc.)
参考来源:EP 0925291; JP 2000502360; WO 9808835

新产品编号:1224977

Chemical Name:
项目整合开发状态:
项目研究机构:
合成路线:The deprotection of the Boc-amino group of the aspartic acid of (X) allows its condensation with the protected S-(tetra-O-acetyl-beta-D-galactopyranos...
参考文献标题:A novel super-potent neurokinin A receptor antagonist containing dehydroalanine
文献作者:Lombardi,A.; D'Agostino,B.; Nastri,F.; D'Andrea,L.D.; Filippelli,A.; Rossi,F.; Pavone,V.
参考来源:Bioorg Med Chem Lett 1998,8(10),1153

新产品编号:1226559

Chemical Name:
项目整合开发状态:
项目研究机构:
合成路线:The optical resolution of 1-benzylazetidine-2-carboxamide (I) with L-tartaric acid in the usual way gave 1-benzylaetidine-2(R)-carboxamide (II),which ...
参考文献标题:7-(2-Aminomethyl-1-azetidinyl)-4-oxoquinoline-3-carboxylic acids as potent antibacterial agents: Design,synthesis,and antibacterial activity
文献作者:Fujita,M.; Chiba,K.; Tominaga,Y.; Hino,K.
参考来源:Chem Pharm Bull 1998,46(5),787

新产品编号:1228141

Chemical Name:
项目整合开发状态:
项目研究机构:
合成路线:Nitrophenoxyacetate (III) (prepared from 2-nitrophenol (I) and tert-butyl bromoacetate),was reduced with H2 in the presence of Pd/C to give aniline (I...
参考文献标题:Synthesis of dipeptide-type human immunodeficiency virus (HIV) protease inhibitors with a binding unit to GP120
文献作者:Asagarasu,A.; Takayanagi,N.; Achiwa,K.
参考来源:Chem Pharm Bull 1998,46(5),867

新产品编号:1229723

Chemical Name:
项目整合开发状态:
项目研究机构:
合成路线:The cyclization of L-serine (I) with pivalaldehyde (II) by means of LDA in THF gives the oxazolidine (III),which is acylated with formic and acetic an...
参考文献标题:Synthesis and biology of the conformationally restricted ACPD analogue,2-aminobicyclo[2.1.1]hexane-2,5-dicarboxylic acid-I,a potent mGluR agonist
文献作者:Kozikowski,A.P.; Steensma,D.; Araldi,G.L.; Tuckmantel,W.; Wang,S.; Pshenichkin,S.; Surina,E.; Wroblewski,J.T.
参考来源:J Med Chem 1998,41(10),1641

新产品编号:1231305

Chemical Name:
项目整合开发状态:
项目研究机构:
合成路线:The compound was prepared by esterification of the 7-hydroxyl group of 13-acetylbaccatin III (I) with 4-benzoylcinnamoyl chloride (II) in the presence...
参考文献标题:Taxoid reversal agents for drug-resistance in cancer chemotherapy and pharmaceutical compsns.thereof
文献作者:Bernacki,R.J.; Ojima,I.(State University of New York,Albany)
参考来源:EP 0966456; US 5811452; WO 9830553