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:2000157

Chemical Name: N,N'-Bis[3-(dimethylamino)propyl]dibenzo[b,j]-1,7-phenanthroline-2,10-dimethanamine
项目整合开发状态: Biological Testing
项目研究机构: CNRS (Originator)
合成路线:The title compound was prepared ...
参考文献标题:Telomerase inhibitors based on quadruplex ligands selected by a fluorescence assay
文献作者:Mergny,J.-L.; Lacroix,L.; Teulade-Frchou,M.-P.; Hounsou,C.; Guittat,L.; Hoarau,M.; Arimondo,P.B.; Vigneron,J.P.; Lehn,J.M.; Riou,J.F.; Garestier,T.; Helene,C.
参考来源:Proc Natl Acad Sci USA 2001,98(6),3062

(Ley)3-peptide-Pam3Cys

Chemical Name: N-Acetyl-O-(6-deoxy-alpha-L-galactopyranosyl)-(1--3)-(beta-D-galactopyranosyl)-(1--4)-[2-acetamido-2-deoxy-3-O-(6-deoxy-alpha-L-galactopyranosyl)-beta-D-glucopyranosyl]-(1--3)-(beta-D-g...
参考文献标题:Trimeric antigenic O-linked glycopeptide conjugates,methods of preparation and uses thereof
文献作者:Williams,L.; Chen,X.T.; Danishefsky,S.J.; Sames,D.; Schwartz,J.B.; Kuduk,S.; Kudryashov,V.; Livingston,P.O.; Ragupathi,G.; Hintermann,S.; Glunz,P.; Lloyd,K.O.(Sloan-Kettering Institute)
参考来源:WO 9948515

新产品编号:2001739

Chemical Name: N2-[3-[[1(R)-(Benzyloxycarbonylamino)-2-phenylethyl](hydroxy)phosphoryl]-2-(2-naphthylsulfanylmethyl)propionyl]-L-tryptophanamide
项目整合开发状态: Biological Testing
项目研究机构: University o...
参考文献标题:Convenient synthesis and diversification of dehydroalaninyl phosphinic peptide analogues
文献作者:Matziari,M.; Georgiadis,D.; Dive,V.; Yiotakis,A.
参考来源:Org Lett 2001,3(5),659

SZ-042

Chemical Name: 1-(4-Amino-2-methylquinazolin-6-yl)-N-[-3-fluoro-2'-(sulfamoyl)biphenyl-4-yl]-3-(trifluoromethyl)-1H-pyrazole-5-carboxamide
项目整合开发状态: Preclinical
项目研究机构: Bristol-Myers Squibb (Ori...
参考文献标题:Discovery of aminoquinazoline and aminoindazole P1 side chains as benzamidine mimics for FXa inhibitors
文献作者:Rossi,K.A.; Clark,C.G.; Li,R.; et al.
参考来源:221st ACS Natl Meet (April 1 2001,San Diego) 2001,Abst MEDI 50

GW-3995

Chemical Name: 1-[2-[1(S)-(4-Isopropyloxazol-2-yl)-2-[4-[2-(5-methyl-2-phenyloxazol-4-yl)ethoxy]phenyl]ethylamino]phenyl]-1-phenylmethanone
项目整合开发状态: Biological Testing
项目研究机构: GlaxoSmithKline (...
参考文献标题:Oxazole PPAR antagonists
文献作者:Cobb,J.E.; Shearer,B.G.; Lambert,M.H.III; Milburn,M.V.(Glaxo Group Ltd.)
参考来源:WO 0117994

GW-9765

Chemical Name: 1-[2-[2-[4-[2-(5-Methyl-2-phenyloxazol-4-yl)ethoxy]phenyl]-1(S)-(5-methyl-1,3,4-thiadiazol-2-yl)ethylamino]phenyl]-1-phenylmethanone
项目整合开发状态: Biological Testing
项目研究机构: GlaxoSmit...
参考文献标题:Oxazole PPAR antagonists
文献作者:Cobb,J.E.; Shearer,B.G.; Lambert,M.H.III; Milburn,M.V.(Glaxo Group Ltd.)
参考来源:WO 0117994

RHPS04, NSC-714187, RHPS4

Chemical Name: 3,11-Difluoro-6,8,13-trimethyl-8H-quino[4,3,2-kl]acridin-13-ium methylsulfate
项目整合开发状态: Preclinical
项目研究机构: Institute of Cancer Research (Originator), University of Nottingham (Or...
参考文献标题:Antitumor polycyclic acridines.8.Synthesis and telomerase-inhibitory activity of methylated pentacyclic acridinium salts
文献作者:Heald,R.A.; Modi,C.; Cookson,J.C.; Hutchinson,I.; Laughton,C.A.; Gowan,S.M.; Kelland,L.R.; Stevens,M.F.G.
参考来源:J Med Chem 2002,45(3),590

SCH-211803

Chemical Name: 2-[4-[4-(3-Chlorophenylsulfonyl)benzyl]-1,4'-bipiperidin-1'-ylcarbonyl]-6-methylphenylamine
项目整合开发状态: Phase I
项目研究机构: Schering-Plough (Originator)
合成路线:Treatment of piperidine ...
参考文献标题:Muscarinic antagonists
文献作者:Miller,M.W.; Clader,J.W.; McCombie,S.W.; Vice,S.F.; Kozlowski,J.A.(Schering Corp.)
参考来源:WO 0121590

BMS-250749

Chemical Name: 3,9-Difluoro-12-(4-deoxy-4-fluoro-beta-D-glucopyranosyl)-5,6,12,13-tetrahydroindolo[2,3- a]pyrrolo[3,4-c]carbazole-5,7-dione
项目整合开发状态: Preclinical
项目研究机构: Bristol-Myers Squibb (Or...
参考文献标题:Cytotoxic amino sugar and related sugar derivs.of indolopyrrolocarbazoles
文献作者:Saulnier,M.G.; Balasubramanian,N.; Frennesson,D.B.; St.Laurent,D.R.; Langley,D.R.(Bristol-Myers Squibb Co.)
参考来源:EP 0971717; JP 2000516250; WO 9807433

IK-264

Chemical Name: (8aS,12aR)-2-(2,4-Dichlorophenyl)-6,7,8a,9,10,11,12,12a-octahydro-5H-pyrido[3',4':4,5]pyrrolo[1,2,3-ef][1,5]benzothiazepine
项目整合开发状态: Preclinical
项目研究机构: Bristol-Myers Squibb (Ori...
参考文献标题:Synthesis and biological evaluation of novel,selective 5-HT2C receptor agonists for the treatment of obesity
文献作者:Robichaud,A.J.; Chen,W.; McClung,C.; et al.
参考来源:221st ACS Natl Meet (April 1 2001,San Diego) 2001,Abst MEDI 105