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:1614149

Chemical Name: (5R,5aR,8aS,9S)-9-[4-(1H-Benzimidazol-2-yl)phenylamino]-5-(4-hydroxy-3,5-dimethoxyphenyl)-5,8,8a,9-tetrahydrofuro[3',4':6,7]naphtho[2,3-d][1,3]dioxol-6(5aH)-one
项目整合开发状态: Preclinical...
参考文献标题:Antitumor agents.194.Synthesis and biological evaluations of 4-beta-mono-,-di-,and -trisubstituted aniline-4'-O-demethyl-podophyllotoxin and related compounds with improved pharmacological profiles
文献作者:Zhu,X.K.; Guan,J.; Tachibana,Y.; Bastow,K.F.; Cho,S.J.; Cheng,H.H.; Cheng,Y.C.; Gurwith,M.; Lee,K.H.
参考来源:J Med Chem 1999,42(13),2441

SRI-9643

Chemical Name: 6-(2-Chlorophenylaminomethyl)-5-methylpyrido[2,3-d]pyrimidine-2,4-diamine
项目整合开发状态: Preclinical
项目研究机构: Duquesne University (Originator), Indiana University (Originator)
合成路线:C...
参考文献标题:Pneumocystis carinii Toxoplasma gondii dihydrofolate reductase inhibitors and antitumor agents: Synthesis and biological activities of 2,4-diamino-5-methyl-6-[(monosubstituted anilino)methyl]-pyrido[2,3-d]pyrimidines
文献作者:Gangjee,A.; Adair,O.; Queener,S.F.
参考来源:J Med Chem 1999,42(13),2447

新产品编号:1615731

Chemical Name: N-[4-[3-[1(S),3-Dicarboxypropyl]ureido]benzyloxycarbonyl]doxorubicin
项目整合开发状态: Biological Testing
项目研究机构: Cancer Research UK (Originator)
合成路线:Coupling of 4-aminobenzyl alcohol...
参考文献标题:Self-immolative anthracycline prodrugs for suicide gene therapy
文献作者:Niculescu-Duvaz,I.; Niculescu-Duvaz,D.; Friedlos,F.; Spooner,R.; Martin,J.; Marais,R.; Springer,C.J.
参考来源:J Med Chem 1999,42(13),2485

S-32502-1

Chemical Name: N-tert-Butyl-N-(2-phenyl-1H-imidazol-4-ylmethylene)amine N-oxide; (Z)-N-tert-Butyl-alpha-(2-phenyl-1H-imidazol-4-yl)nitrone
项目整合开发状态: Preclinical
项目研究机构: Servier (Originator)
合...
参考文献标题:Nitrone derivs.,process for their preparation and pharmaceutical compsns.containing them
文献作者:Dhainaut,A.; Lestage,P.; Lockhart,B.; Tizot,A.; Goldstein,S.(ADIR et Cie.)
参考来源:CA 2274621; EP 0967207; FR 2780404; JP 2000026428; US 6034250

新产品编号:1617313

Chemical Name: N-[4-Hydroxy-3,5-bis(4-methylpiperazin-1-ylmethyl)phenyl]-2-(2-naphthyl)quinoline-4-amine
项目整合开发状态: Biological Testing
项目研究机构: Georgia State University (Originator), University of...
参考文献标题:Structure-activity relationship analysis of substituted 4-quinolinamines,antagonists of immunostimulatory CpG-oligodeoxynucleotides
文献作者:Strekowski,L.; Zegrocka,O.; Henary,M.; Say,M.; Mokrosz,M.J.; Kotecka,B.M.; Manzel,L.; Macfarlane,D.E.
参考来源:Bioorg Med Chem Lett 1999,9(13),1819

新产品编号:1618895

Chemical Name: 2-(1-Piperidinyl)acetic acid 2,5-dioxo-4,4-diphenylimidazolidin-1-ylmethyl ester hydrochloride
项目整合开发状态: Preclinical
项目研究机构: Universitat de Barcelona (Originator)
合成路线:Condensa...
参考文献标题:Synthesis of water-soluble phenytoin prodrugs
文献作者:Bosch,J.; Roca,T.; Domenech,J.; Suriol,M.
参考来源:Bioorg Med Chem Lett 1999,9(13),1859

新产品编号:1620477

Chemical Name: 7alpha-[4-[2-(1-Piperidinyl)ethoxy]benzylsulfanyl]-17alpha-3-oxopregn-4-ene-21,17-carbolactone
项目整合开发状态: Biological Testing
项目研究机构: Universit?Laval (Originator)
合成路线:Alkylation...
参考文献标题:Spironolactone-related inhibitors of type II 17beta-hydroxysteroid dehydrogenase: Chemical synthesis,receptor binding affinities,and proliferative/antiproliferative activities
文献作者:Tremblay,M.R.; Luu-The,V.; Leblanc,G.; Noel,P.; Breton,E.; Labrie,F.; Poirier,D.
参考来源:Bioorg Med Chem 1999,7(6),1013

NSC-656240

Chemical Name: 2-(Hydroxymethyl)benzo[1,2-b:5,4-b']dithiophene-4,8-dione
项目整合开发状态: Preclinical
项目研究机构: National Cancer Institute (Originator)
合成路线:Oxidation of 3-methyl-2-thiophenecarboxylic ...
参考文献标题:Synthesis and cytotoxicity of methyl-4,8-dihydrobenzol[1,2-b: 5,4-b']dithiophene-4,8-dione derivatives
文献作者:Chao,Y.H.; Kuo,S.C.; Ku,K.; Chiu,I.P.; Wu,C.H.; Mauger,A.; Wang,H.K.; Lee,K.H.
参考来源:Bioorg Med Chem 1999,7(6),1025

VP-365

Chemical Name: (R)-N-[4-(2,3,3a,4,5,10-Hexahydro-1H-pyrrolo[1,2-b][2,5]benzodiazepin-5-ylcarbonyl)phenyl]biphenyl-2-carboxamide
项目整合开发状态: Preclinical
项目研究机构: Wakamoto (Originator)
合成路线:The re...
参考文献标题:Biphenyl derivs.and medicinal compsns.
文献作者:Matsukawa,H.; Toyofuku,H.; Naito,A.; Ohtake,Y.; Saito,Y.; Naito,K.(Wakamoto Pharmaceutical Co.,Ltd.)
参考来源:EP 0987266; WO 9843976

QF-0510B

Chemical Name: 5-[2-[4-(6-Fluoro-1,2-benzisoxazol-3-yl)piperidin-1-yl]ethyl]-5,6-dihydro-4H-cyclopenta[b]thiophen-4-one dihydrochloride
项目整合开发状态: Preclinical
项目研究机构: Universidad de Santiago de C...
参考文献标题:Conformationally constrained butyrophenones with mixed dopaminergic (D(2)) and serotoninergic (5-HT(2A),5-HT(2C)) affinities: Synthesis,pharmacology,3D-QSAR,and molecular modeling of (aminoalkyl)benzo- and -thienocycloalkanones as putative atypical an
文献作者:Ravi�? E.; Negreira,J.; Cid,J.; Masaguer,C.F.; Rosa,E.; Rivas,M.E.; Fontenla,J.A.; Loza,M.I.; Tristan,H.; Cadavid,M.I.; Sanz,F.; Lozoya,E.; Carotti,A.; Carrieri,A.
参考来源:J Med Chem 1999,42(15),2774