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:1019317

Chemical Name: 5-Methoxy-3-[1-methylpyrrolidin-2(R)-ylmethyl]-1H-indole
项目整合开发状态: Biological Testing
项目研究机构: Pfizer (Originator)
合成路线:Alternatively,5-methoxyindole (III) was N-silylated emplo...
参考文献标题:Further studies on oxygenated tryptamines with LSD-like activity incorporating a chiral pyrrolidine moiety into the side chain
文献作者:Gerasimov,M.; Marona-Lewicka,D.; Kurrasch-Orbaugh,D.M.; Qandil,A.M.; Nichols,D.E.
参考来源:J Med Chem 1999,42(20),4257

GYKI-46903

Chemical Name: (+)-endo-6-(4-Fluorophenyl)-4-(propionyloxy)-1-azabicyclo[3.3.1]non-6-ene hydrochloride; (+)-(4R*,5S*)-6-(4-Fluorophenyl)-4-(propionyloxy)-1-azabicyclo[3.3.1]non-6-ene hydrochloride
...
参考文献标题:New 1-azabicycloalkane derivs.,pharmaceutical compsns.containing them and process for preparing same
文献作者:S髄yom,S.; Abraham,G.; Sz鰈sy,M.; Borsi,J.; Vit醠is,B.; Karimn?Tapfer,M.; Szab�?Bady,E.; Csuzdi,E.; Goldschmidtn?Horv醫h,K.; M�? G.; Ling,I.; Mikl髎n?Kov醕s,A.(Gyogyszerkutato Intezet Kft.)
参考来源:EP 0556342; JP 1994505706; WO 9207854

TAN-1251A

Chemical Name: (5S)-4-Methyl-2-[4-(3-methyl-2-butenyloxy)benzylidene]spiro[1,4-diazabicyclo[3.2.1]heptane-7,1'-cyclohexan]-4'-one
项目整合开发状态: Biological Testing
项目研究机构: Takeda (Originator)
合成路线...
参考文献标题:Total synthesis of (?-TAN1251A
文献作者:Nagumo,S.; et al.
参考来源:Tetrahedron Lett 1998,39(25),4493

TAN-1251B

Chemical Name: 3'-Hydroxy-4-methyl-2-[4-(3-methyl-2-butenyloxy)benzylidene]spiro[1,4-diazabicyclo[3.2.1]heptane-7,1'-cyclohexan]-4'-one
项目整合开发状态: Biological Testing
项目研究机构: Takeda (Originator) 参考文献标题:Biomimeric total syntheses of (-)-TAN1251A,(+)-TAN1251B,(+)-TAN1251C,and (+)-TAN1251D
文献作者:Snider,B.B.; Lin,H.
参考来源:Org Lett 2000,2(5),643

NLA-2

Chemical Name: N-[2-(2-Nitro-1H-imidazol-1-yl)ethyl]acridine-9-amine hydrochloride
项目整合开发状态: Biological Testing
项目研究机构: Stanford University (Originator), University of Auckland (Originator), Uni...
参考文献标题:Bis(nitro-1-imidazolyl alkylamine) platinum complexes useful in radiotheraphy or chemotherapy
文献作者:Adams,G.E.; Ahmed,I.; Stratford,I.J.(Gerald Edward Adams; Ian James Stratford; Israr Ahmed)
参考来源:GB 2131020

FR-143187

Chemical Name: 7-Methyl-3-[4-[2-methyl-5-(1H-tetrazol-5-yl)pyrrol-1-yl]benzyl]-2-propyl-3H-imidazo[4,5-b]pyridine hydrochloride
项目整合开发状态: Preclinical
项目研究机构: Fujisawa (Originator)
合成路线:The co...
参考文献标题:Pilot scale synthesis of a novel nonpeptide angiotensin II receptor antagonist
文献作者:Zanka,A.; et al.
参考来源:Org Process Res Dev 1998,2(4),230

2',2'-Dimethyl-PMEG

Chemical Name: 9-[2-Methyl-2-(phosphonomethoxy)propyl]guanine
项目整合开发状态: Preclinical
项目研究机构: Bristol-Myers Squibb (Originator)
合成路线:N6-Protected (S)-DHPA (II) was esterified with ClCH2P(O)Cl2,...
参考文献标题:Novel phosphonate nucleosides as antiviral agents
文献作者:Hwang,J.-T.; Choi,J.-R.
参考来源:Drugs Fut 2004,29(2),163

F-910754

Chemical Name: N-[4-(beta-D-Glucopyranuronosyloxy)-3-nitrobenzyloxycarbonyl]daunomycin
项目整合开发状态: Preclinical
项目研究机构: Aventis Pharma (Originator), Dade Behring Marburg (Originator), Institut Curi...
参考文献标题:Prodrugs of anthracyclines for use in antibody-directed enzyme prodrug therapy
文献作者:Florent,J.-C.; Dong,X.; Gaudel,G.; Mitaku,S.; Monneret,C.; Gesson,J.P.; Jacquesy,J.C.; Mondon,M.; Renoux,B.; Andrianomenjanahary,S.; Michel,S.; Koch,M.; Tillequin,F.; Gerken,M.; Czech,J.; Straub,R.; Bosslet,K.
参考来源:J Med Chem 1998,41(19),3572

CP-0467

Chemical Name: 7-[2-(5-Amino-1,2,4-thiadiazol-4-yl)-2(Z)-(methoxyimino)acetamido]-3-(benzothiazol-2-ylthio)-3-cephem-4-carboxylic acid sodium salt
项目整合开发状态: Preclinical
项目研究机构: Meiji Seika (Orig...
参考文献标题:Novel cephalosporin derivatives possessing a bicyclic heterocycle at the 3-position.Part I: Synthesis and biological activities of 3-(benzothiazol-2-yl)thiocephalosporin derivatives,CP0467 and related compounds
文献作者:Tsushima,M.; Iwamatsu,K.; Tamura,A.; Shibahara,S.
参考来源:Bioorg Med Chem 1998,6(7),1009

LY-274601((+)-enantiomer), LY-274600

Chemical Name: (-)-2(S)-(Propylamino)-8-(methylthio)-1,2,3,4-tetrahydronaphthalene hydrochloride
项目整合开发状态: Biological Testing
项目研究机构: Lilly (Originator)
合成路线:The cleavage of the butyrate grou...
参考文献标题:Syntheses of [C-11] and [H-3] LY274601,a serotonin(1A) receptor agonist
文献作者:Suehiro,M.; et al.
参考来源:J Label Compd Radiopharm 1998,41(8),725