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:1323061

Chemical Name: 2(S)-Allyl-3(R)-[N-[2-phenyl-1-(2-thienylcarbonyl)ethyl]carbamoyl]-5-methylhexanehydroxamic acid
项目整合开发状态: Biological Testing
项目研究机构: Abbott (Originator)
合成路线:Friedel Crafts ac...
参考文献标题:Aryl ketones as novel replacements for the C-terminal amide bond of succinyl hydroxamate MMP inhibitors
文献作者:Sheppard,G.S.; Florjancic,A.S.; Giesler,J.R.; Xu,L.; Guo,Y.; Davidsen,S.K.; Marcotte,P.A.; Elmore,I.; Albert,D.H.; Terrance,J.M.; Bouska,J.J.; Goodfellow,C.L.; Morgan,D.W.; Summers,J.B.
参考来源:Bioorg Med Chem Lett 1998,8(22),3251

新产品编号:1324643

Chemical Name: 2(S)-Allyl-3(R)-[N-[1-(oxazol-2-ylcarbonyl)-2-phenylethyl]carbamoyl]-5-methylhexanehydroxamic acid
项目整合开发状态: Biological Testing
项目研究机构: Abbott (Originator)
合成路线:Friedel Crafts ...
参考文献标题:Aryl ketones as novel replacements for the C-terminal amide bond of succinyl hydroxamate MMP inhibitors
文献作者:Sheppard,G.S.; Florjancic,A.S.; Giesler,J.R.; Xu,L.; Guo,Y.; Davidsen,S.K.; Marcotte,P.A.; Elmore,I.; Albert,D.H.; Terrance,J.M.; Bouska,J.J.; Goodfellow,C.L.; Morgan,D.W.; Summers,J.B.
参考来源:Bioorg Med Chem Lett 1998,8(22),3251

新产品编号:1326225

Chemical Name: [2R-(2alpha,3beta,4alpha,17abeta)]-4-Hydroxy-2-(hydroxymethyl)-3-methoxy-3,4,4a,11,12,17a-hexahydro-2H,10H-diindolo[1,2,3-de:3',2',1'-ij]pyrano[2,3-b]pyrrolo[3,4-g]quinoxaline-10,12-dio...
参考文献标题:Syntheses,biochemical and biological evaluation of staurosporine analogues from the microbial metabolite rebeccamycin
文献作者:Anizon,F.; Moreau,P.; Sancelme,M.; Voldoire,A.; Prudhomme,M.; Ollier,M.; Severe,D.; Riou,J.F.; Bailly,C.; Fabbro,D.; Meyer,T.; Aubertin,A.M.
参考来源:Bioorg Med Chem 1998,6(9),1597

2MD

Chemical Name: (20S)-1alpha,25-Dihydroxy-2-methylene-19-norvitamin D3
项目整合开发状态: Preclinical
项目研究机构: Wisconsin Alumni Research Foundation (Originator), Pfizer (Licensee), Deltanoid (Codevelopment...
参考文献标题:2-Alkylidene-19-nor-vitamin D cpds.
文献作者:DeLuca,H.F.; Sicinski,R.R.(Wisconsin Alumni Research Foundation)
参考来源:EP 0970047; JP 2001504135; US 5843928; WO 9841501

Kaitocephalin, PF-1191

Chemical Name: 2-[2(R)-Amino-2-carboxy-1(S)-hydroxyethyl]-5(R)-[2(S)-carboxy-2-(3,5-dichloro-4-hydroxybenzamido)ethyl]-L-proline
项目整合开发状态: Biological Testing
项目研究机构: Meiji Seika (Originator)
...
参考文献标题:The first synthesis of kaitocephalin based on the structure revision
文献作者:Watanabe,H.; Okue,M.; Kobayashi,H.; Kitahara,T.
参考来源:Tetrahedron Lett 2002,43(5),861

QM-96625

Chemical Name: 2-Benzyl-4-(2-chlorobenzyl)-3,4-dihydro-2H-thieno[3,4-e]-1,2,4-thiadiazin-3-one 1,1-dioxide
项目整合开发状态: Biological Testing
项目研究机构: CSIC (Originator), Katholieke Universiteit Leuven ...
参考文献标题:Novel 1,1,3-trioxo-2H,4H-thieno[3,4-e][1,2,4]thiadiazine derivatives as non-nucleoside reverse transcriptase inhibitors that inhibit human immunodeficiency virus type 1 replication
文献作者:Arranz,E.; D韆z,J.A.; Ingate,S.T.; Witvrouw,M.; Pannecouque,C.; Balzarini,J.; De Clercq,E.; Vega,S.
参考来源:J Med Chem 1998,41(21),4109

QM-96539

Chemical Name: 2-(3-Chlorobenzyl)-4-cyanomethyl-3,4-dihydro-2H-thieno[3,4-e]-1,2,4-thiadiazin-3-one 1,1-dioxide
项目整合开发状态: Biological Testing
项目研究机构: CSIC (Originator), Katholieke Universiteit Le...
参考文献标题:Novel 1,1,3-trioxo-2H,4H-thieno[3,4-e][1,2,4]thiadiazine derivatives as non-nucleoside reverse transcriptase inhibitors that inhibit human immunodeficiency virus type 1 replication
文献作者:Arranz,E.; D韆z,J.A.; Ingate,S.T.; Witvrouw,M.; Pannecouque,C.; Balzarini,J.; De Clercq,E.; Vega,S.
参考来源:J Med Chem 1998,41(21),4109

新产品编号:1327807

Chemical Name: trans-6-Hydroxy-1-(3-iodo-2-propenyl)-1,2,3,4,4a,5,10,10a-octahydrobenzo[g]quinoline
项目整合开发状态: Biological Testing
项目研究机构: University of Crete (Originator)
合成路线:Ketoester (II) w...
参考文献标题:N-(Iodopropenyl)-octahydrobenzo[f]- and -[g]quinolines: Synthesis and adrenergic and dopaminergic activity studies
文献作者:Tagmatarchis,N.; Thermos,K.; Katerinopoulos,H.E.
参考来源:J Med Chem 1998,41(21),4165

新产品编号:1329389

Chemical Name: 1alpha,24(R)-Dihydroxy-25-nitrovitamin D3
项目整合开发状态: Biological Testing
项目研究机构: Teijin (Originator)
合成路线:Condensation of aldehyde (I) with 2-nitropropane (II) using tert-butyldi...
参考文献标题:Synthesis and biological evaluation of 1alpha,24-dihydroxy-25-nitrovitamin D3
文献作者:Oshida,J.; Okamoto,M.; Ishizuka,S.; Azuma,S.
参考来源:Bioorg Med Chem Lett 1999,9(3),381

新产品编号:1330971

Chemical Name: 1alpha,24(S)-Dihydroxy-25-nitrovitamin D3
项目整合开发状态: Biological Testing
项目研究机构: Teijin (Originator)
合成路线:Condensation of aldehyde (I) with 2-nitropropane (II) using tert-butyldi...
参考文献标题:Synthesis and biological evaluation of 1alpha,24-dihydroxy-25-nitrovitamin D3
文献作者:Oshida,J.; Okamoto,M.; Ishizuka,S.; Azuma,S.
参考来源:Bioorg Med Chem Lett 1999,9(3),381