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

TGP

Chemical Name: (-)-(2R,5S)-5-(Guanin-9-ylmethyl)tetrahydrofuran-2-ylphosphonic acid
项目整合开发状态: Preclinical
项目研究机构: GlaxoSmithKline (Originator), Shire BioChem (Originator)
合成路线:(S)-5-(Hydroxym...
参考文献标题:Anti-viral cpds.
文献作者:Kong,L.C.C.; Dionne,G.; Quimpere,M.; Brown,W.L.; Nguyen-Ba,N.
参考来源:US 5789394

VP-339

Chemical Name: (S)-N-[4-(10-Oxo-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...
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

VP-343

Chemical Name: (S,S)-N-[4-(2-Hydroxy-1,2,3,3a,4,5-hexahydropyrrolo[1,2-a]quinoxalin-5-ylcarbonyl)phenyl]-4'-methylbiphenyl-2-carboxmide
项目整合开发状态: Preclinical
项目研究机构: Wakamoto (Originator)
合成路...
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

FR-180102

Chemical Name: N-[2,4-Dichloro-3-(isoquinolin-5-yloxymethyl)phenyl]acetamide
项目整合开发状态: Biological Testing
项目研究机构: Fujisawa (Originator)
合成路线:Nitration of 2,6-dichlorobenzaldehyde (I) with 70%...
参考文献标题:A novel class of orally active non-peptide bradykinin B2 receptor antagonists.1.Construction of the basic framework
文献作者:Abe,Y.; Kayakiri,H.; Satoh,S.; Inoue,T.; Sawada,Y.; Imai,K.; Inamura,N.; Asano,M.; Hatori,C.; Katayama,A.; Oku,T.; Tanaka,H.
参考来源:J Med Chem 1998,41(4),564

新产品编号:1193337

Chemical Name:
项目整合开发状态: Preclinical
项目研究机构: Kyowa Hakko (Originator)
合成路线:The reaction of 4-bromothiophene-2-carbaldehyde (I) with triethyl orthoformate gives the corresponding acetal (II),...
参考文献标题:Synthesis and antitumor activity of duocarmycin derivatives: A-ring pyrrole compounds bearing 5-membered heteroarylacryloyl groups
文献作者:Amishiro,N.; Nagamura,S.; Kobayashi,E.; Okamoto,A.; Gomi,K.; Saito,H.
参考来源:Chem Pharm Bull 1999,47(10),1393

新产品编号:1194919

Chemical Name:
项目整合开发状态: Biological Testing
项目研究机构: Ishihara Sangyo (Originator)
合成路线:Phthalic anhydride (I) was condensed with 2,6-diisopropyl-aniline (II) to give the N-aryl phthalimide (I...
参考文献标题:Nonpeptide small-molecular inhibitors of dipeptidyl peptidase IV: N-Phenylphthalimide analogs
文献作者:Shimazawa,R.; Takayama,H.; Kato,F.; Kato,M.; Hashimoto,Y.
参考来源:Bioorg Med Chem Lett 1999,9(4),559

新产品编号:1196501

Chemical Name:
项目整合开发状态: Biological Testing
项目研究机构: National Institutes of Health (Originator), Rega Institute for Medical Research (Originator), University of Alberta (Originator), Wayne State...
参考文献标题:Cytotoxic activities of Mannich bases of chalcones and related compounds
文献作者:Dimmock,J.R.; Kandepu,N.M.; Hetherington,M.; Quail,J.W.; Pugazhenthi,U.; Sudom,A.M.; Chamankhah,M.; Rose,P.; Pass,E.; Allen,T.M.; Halleran,S.; Szydlowski,J.; Mutus,B.; Tannous,M.; Manavathu,E.K.; Myers,T.G.; De Clercq,E.; Balzarini,J.
参考来源:J Med Chem 1998,41(7),1014-1026

新产品编号:1198083

Chemical Name:
项目整合开发状态: Biological Testing
项目研究机构: Ohio State University (Originator)
合成路线:Nitration of 2-hydroxy-DL-phenylalanine (I) with nitronium tetrafluoroborate in cooled acetonitril...
参考文献标题:Design and synthesis of enantiomers of 3,5-dinitro-o-tyrosine: alpha-Amino-3-hydroxy-5-methyl-4-isoxazolepropanoic acid (AMPA) receptor antagonists
文献作者:Sun,G.; Slavica,M.; Uretsky,N.J.; Wallace,L.J.; Shams,G.; Weinstein,D.M.; Miller,J.C.; Miller,D.D.
参考来源:J Med Chem 1998,41(7),1034-1041

新产品编号:1199665

Chemical Name:
项目整合开发状态: Biological Testing
项目研究机构: University of Bath (Originator)
合成路线:Pechmann condensation of resorcinol (I) with ethyl 2-methylacetylacetate (II) in concentrated sulfuri...
参考文献标题:Steroidal and nonsteroidal sulfamates as potent inhibitors of steroid sulfatase
文献作者:Woo,L.W.C.; Howarth,N,M.; Purohit,A.; Hejaz,H.A.; Reed,M.J.; Potter,B.V.L.
参考来源:J Med Chem 1998,41(7),1068

新产品编号:1201247

Chemical Name:
项目整合开发状态: Biological Testing
项目研究机构: China Medical College (Originator), National Cancer Institute (Originator), University of North Carolina (Originator)
合成路线:The compound wa...
参考文献标题:Antitumor agents.181.Synthesis and biological evaluation of 6,7,2',3',4'-substituted-1,2,3,4-tetrahydro-2-phenyl-4-quinolones as a new class of antimitotic antitumor agents
文献作者:Xia,Y.; Yang,Z.Y..; Xia,P.; Bastow,K.F.; Tachibana,Y.; Kuo,S.C.; Hamel,E.; Hackl,T.; Lee,K.H.
参考来源:J Med Chem 1998,41(7),1155