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:1951115

Chemical Name: 5(S)-Ethyl-3-isopropoxy-5-methyl-4-[4-(methylsulfonyl)phenyl]-2,5-dihydrofuran-2-one
项目整合开发状态: Preclinical
项目研究机构: Merck & Co. (Originator)
合成路线:Dehydrohalogenation of bromo ke...
参考文献标题:Discovery of a potent and selective COX-2 inhibitor in the alkoxy lactone series with optimized metabolic profile
文献作者:Leblanc,Y.; Roy,P.; Wang,Z.; Li,C.S.; Chauret,N.; Nicoll-Griffith,D.A.; Silva,J.M.; Aubin,Y.; Yergey,J.A.; Chan,C.C.; Riendeau,D.; Brideau,C.; Gordon,R.; Xu,L.; Webb,J.; Visco,D.M.; Prasit,P.
参考来源:Bioorg Med Chem Lett 2002,12(22),3317

MAG-283

Chemical Name: 2(R)-[4-Amino-4-oxo-2(S)-sulfanylbutyl]sulfanyl]-N-[1(S)-benzyl-2-(methylamino)-2-oxoethyl]-4-methylpentanamide; N2-[2(R)-[4-Amino-4-oxo-2(S)-sulfanylbutylsulfanyl]-4-methylpentanoyl]-N...
参考文献标题:Mercaptosulfide metalloproteinase inhibitors
文献作者:Schwartz,M.A.; Wart,H.V.(Florida State University)
参考来源:WO 9509833

[Dmt1]DALDA, SUPER-DALDA

Chemical Name: 2,6-Dimethyl-L-tyrosyl-D-arginyl-L-phenylalanyl-L-lysinamide
项目整合开发状态: Preclinical
项目研究机构: AstraZeneca (Originator)
合成路线:The title peptide was prepared by solid-phase synthesis...
参考文献标题:DALDA analogs and their use
文献作者:Schiller,P.(AstraZeneca AB)
参考来源:WO 0055189

RPR-117824

Chemical Name: 9-(Carboxymethyl)-4-oxo-5,10-dihydro-4H-imidazo[1,2-a]indeno[1,2-e]pyrazine-2-carboxylic acid
项目整合开发状态: Preclinical
项目研究机构: Aventis Pharma (Originator)
合成路线:Heck coupling of 2-...
参考文献标题:5H,10H-Imidazo[1,2-a]indeno[1,2-e]pyrazine-4-one derivs.,preparation thereof,intermediates thereof and drugs containing same
文献作者:Aloup,J.-C.; Bouquerel,J.; Damour,D.; Hardy,J.-C.; Jimonet,P.; Manfre,M.; Mignani,S.; Nemecek,P.(Aventis Pharma SA)
参考来源:EP 0880522; FR 2743366; JP 2000505073; US 5990108; WO 9725328

PGE-3366466

Chemical Name: 7-[(1R,2R,3R,5S)-2-[3(R)-(Benzo[b]thien-2-yl)-3-hydroxypropyl]-3,5-dihydroxycyclopentyl]heptanoic acid; 15-(2-Benzothienyl)-13,14-dihydro-16,17,18,19,20-pentanorprostaglandin F1alpha 参考文献标题:C16 unsaturated FP-selective prostaglandins analogs
文献作者:deLong,M.A.; Soper,D.L.; De,B.; Wos,J.A.(The Procter & Gamble Co.)
参考来源:WO 0051980

UR-12715

Chemical Name: 3-(4-Aminophenyl)-1-[4-(2-methyl-1H-imidazo[4,5-c]pyridin-1-ylmethyl)piperidin-1-yl]-3-phenyl-2(Z)-propen-1-one
项目整合开发状态: Preclinical
项目研究机构: Uriach (Originator)
合成路线:4-(Aminom...
参考文献标题:Azo derivs.of 5-aminosalicylic acid for treatment of inflammatory bowel disease
文献作者:Carceller,E.; Jimenez,P.J.; Salas,J.; Almansa,C.; Bartroli,J.; Merlos,M.; Giral,M.; Balsa,D.; Ferrando,R.; Garcia-Rafanell,J.; Forn,J.(J.Uriach & C�?,SA)
参考来源:EP 0790998; ES 2104513; ES 2106682; JP 1999501939; US 5747477; WO 9709329

E-2050

Chemical Name: (-)-5-[4-[2-(4-Fluorophenoxy)ethyl]piperazin-1-yl]-2-isopropyl-2-phenylpentanenitrile
项目整合开发状态: Preclinical
项目研究机构: Eisai (Originator)
合成路线:Alkylation of 1-benzylpiperazine (V...
参考文献标题:N,N-Substd.cyclic amine derivs.
文献作者:Niidome,T.; Norimine,Y.; Teramoto,T.; Kawano,K.; Kimura,T.; Iimura,Y.; Yamamoto,N.; Suzuki,Y.; Ito,K.; Hatakeyama,S.; Nagato,S.; Komatsu,M.(Eisai Co.,Ltd.)
参考来源:EP 1099692; JP 2000169462; WO 0005210

WAY-170523

Chemical Name: N-[2-[4-[N-Benzyl-N-[2-(N-hydroxycarbamoyl)-4,6-dimethylphenyl]sulfamoyl]phenoxy]ethyl]-1-benzofuran-2-carboxamide
项目整合开发状态: Biological Testing
项目研究机构: Wyeth Pharmaceuticals (Orig...
参考文献标题:Preparation and use of orthosulfonamido aryl hydroxamic acids as matrix metalloproteinase and TACE inhibitors
文献作者:Gu,Y.; Nelson,F.C.; Zask,A.; Du,M.T.; Levin,J.I.; Venkatesan,M.(American Cyanamid Co.)
参考来源:US 5929097

RTI-362

Chemical Name: 3alpha-(4-Methylphenyl)nortropane-2beta-carboxylic acid methyl ester; 3endo-(4-Methylphenyl)-8-azabicyclo[3.2.1]octane-2exo-carboxylic acid methyl ester
项目整合开发状态: Biological Testing<...
参考文献标题:3alpha-(4'-Substituted phenyl)tropane-2beta-carboxylic acid methyl esters: Novel ligands with high affinity and selectivity at the dopamine transporter
文献作者:Holmquist,C.R.; Keverline-Frantz,K.I.; Abraham,P.; Boja,J.W.; Kuhar,M.J.; Carroll,F.I.
参考来源:J Med Chem 1996,39(21),4139

QF-1004B

Chemical Name: 6-[4-(6-Fluoro-1,2-benzisoxazol-3-yl)piperidin-1-ylmethyl]-6,7-dihydrobenzofuran-4(5H)-one
项目整合开发状态: Preclinical
项目研究机构: Universidad de Santiago de Compostela (Originator), Univer...
参考文献标题:Conformationally constrained butyrophenones with affinity for dopamine (D1,D2,D4) and serotonin (5-HT2A,5-HT2C) receptors: Synthesis of aminomethylbenzo[b]furanones and their evaluation as antipsychotics
文献作者:Ravi�? E.; Casariego,I.; Masaguer,C.F.; Fontenla,J.A.; Montenegro,G.Y.; Rivas,M.E.; Loza,M.I.; Enguix,M.J.; Villazon,M.; Cadavid,M.I.; Demontis,G.C.
参考来源:J Med Chem 2000,43(24),4678