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:1777095

Chemical Name: 8-[3,7-Dimethyl-2(E),6-octadienyl]-3,5,7-trihydroxy-2-[3-(4-hydroxy-3-methoxyphenyl)-2-(hydroxymethyl)-2,3-dihydro-1,4-benzodioxin-6-yl]-4H-1-benzopyran-4-one
项目整合开发状态: Biological Te...
参考文献标题:The flavanolignan silybin and its hemisynthetic derivatives,a novel series of potential modulators of P-glycoprotein
文献作者:Maitrejean,M.; Comte,G.; Barron,D.; El Kirat,K.; Conseil,G.; Di Pietro,A.
参考来源:Bioorg Med Chem Lett 2000,10(2),157

新产品编号:1778677

Chemical Name: 2-[2(S)-Amino-3-(4-hydroxy-2,6-dimethylphenyl)propionyl]-7-(4-fluorophenyl)-1,2,3,4-tetrahydroisoquinoline-3(S)-carboxylic acid
项目整合开发状态: Biological Testing
项目研究机构: AstraZeneca (O...
参考文献标题:Novel Dmt-Tic dipeptide analogues as selective delta-opioid receptor antagonists
文献作者:Pag? D.; McGlory,A.; Mischki,T.; Schmidt,R.; Butterworth,J.; St-Onge,S.; Labarre,M.; Payza,K.; Brown,W.
参考来源:Bioorg Med Chem Lett 2000,10(2),167

Tamandarin B

Chemical Name: (3S,6S,10S,11R,14R,15R,18S,21S)-14-[N-[2(S)-Hydroxypropionyl]-L-prolyl-D-(N-methyl)leucylamino]-10-hydroxy-3-isobutyl-6,11-diisopropyl-18-(4-methoxybenzyl)-15,19-dimethyl-7,16-dioxa-1,4...
参考文献标题:Total synthesis of (-)-tamandarin B
文献作者:Joullie,M.M.; et al.
参考来源:Tetrahedron Lett 2000,41(49),9373

Neo-acridine, Neomycin-acridine

Chemical Name: O-2,6-Diamino-2,6-dideoxy-alpha-D-glucopyranosyl-(1--4)-O-[O-2,6-diamino-2,6-dideoxy-beta-L-idopyranosyl-(1--3)[5-[2-(acridin-9-ylamino)ethylsulfanyl]-5-deoxy-beta-D-ribofuranosyl-(1--5...
参考文献标题:Neomycin - Acridine conjugate: A potent inhibitor of Rev-RRE binding
文献作者:Kirk,S.R.; et al.
参考来源:J Am Chem Soc 2000,122(5),980

CTDP-31677

Chemical Name: 1-(3,4-Dichlorophenyl)-1-[4(S)-(3,4-dichlorophenyl)-4-hydroxy-1-methylpiperidin-3(R)-yl]methanone
项目整合开发状态: Preclinical
项目研究机构: Georgetown University (Originator), UT Medical Bran...
参考文献标题:Discovery of a novel dopamine transporter inhibitor,4-hydroxy-1-methyl-4-(4-methylphenyl)-3-piperidyl 4-methylphenyl ketone,as a potential cocaine antagonist through 3D-database pharmacophore searching.Molecular modeling,structure-activity relationshi
文献作者:Wang,S.; Sakamuri,S.; Enyedy,I.J.; Kozikowski,A.P.; Deschaux,O.; Bandyopadhyay,B.C.; Tella,S.R.; Zaman,W.A.; Johnson,K.M.
参考来源:J Med Chem 2000,43(3),351

新产品编号:1780259

Chemical Name: N-[3,3-Dimethyl-3-[2-[N-[2-(O-methylpolyethyleneglycol)acetyl]-L-alanyloxy]-4,6-dimethylphenyl]propionyl]daunorubicin
项目整合开发状态: Preclinical
项目研究机构: Enzon (Originator)
合成路线:Coup...
参考文献标题:Drug delivery systems based on trimethyl lock lactonization: Poly(ethylene glycol) prodrugs of amino-containing compounds
文献作者:Greenwald,R.B.; Choe,Y.H.; Conover,C.D.; Shum,K.; Wu,D.; Royzen,M.
参考来源:J Med Chem 2000,43(3),475

新产品编号:1781841

Chemical Name: N1,N1,N1,N21,N21,N21-Hexaethylhenicosane-1,21-diammonium dibromide
项目整合开发状态: Biological Testing
项目研究机构: CNRS (Originator)
合成路线:The title bis-ammonium salt was prepared by quate...
参考文献标题:Antimalarial activity of compounds interfering with Plasmodium falciparum phospholipid metabolism: Comparison between mono- and bisquaternary ammonium salts
文献作者:Calas,M.; Ancelin,M.L.; Cordina,G.; Portefaix,P.; Piquet,G.; Vidal-Sailhan,V.; Vial,H.
参考来源:J Med Chem 2000,43(3),505

MC-867

Chemical Name: 2-(Cyclopentylsulfanyl)-6-(2,6-difluorobenzyl)pyrimidin-4(3H)-one
项目整合开发状态: Biological Testing
项目研究机构: Idenix (Originator)
合成路线:The condensation of 2-(2,6-difluorophenyl)acetic...
参考文献标题:Selected non-nucleoside reverse transcriptase inhibitors (NNRTIs): the DABOs family
文献作者:Artico,M.
参考来源:Drugs Fut 2002,27(2),159

MC-922

Chemical Name: 2-(Cyclopentylsulfanyl)-6-(2,6-difluorobenzyl)-5-methylpyrimidin-4(3H)-one
项目整合开发状态: Biological Testing
项目研究机构: Idenix (Originator)
合成路线:The condensation of 2-(2,6-difluorophen...
参考文献标题:Selected non-nucleoside reverse transcriptase inhibitors (NNRTIs): the DABOs family
文献作者:Artico,M.
参考来源:Drugs Fut 2002,27(2),159

MC-1008

Chemical Name: 2-(Cyclopentylsulfanyl)-6-[1-(2,6-difluorophenyl)ethyl]pyrimidin-4(3H)-one
项目整合开发状态: Biological Testing
项目研究机构: Idenix (Originator)
合成路线:The condensation of 2-(2,6-difluorophen...
参考文献标题:Selected non-nucleoside reverse transcriptase inhibitors (NNRTIs): the DABOs family
文献作者:Artico,M.
参考来源:Drugs Fut 2002,27(2),159