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

GL-406349

Chemical Name: N,N'-Bis[2-[N-[2-(N2,N5-dimethyl-DL-lysylamino)ethyl]carbamoyl]-1H-indol-6-yl]-1H -indole-2,5-dicarboxamide
项目整合开发状态: Preclinical
项目研究机构: Genelabs (Originator)
合成路线:Reaction o...
参考文献标题:Discovery af a new class of broad-spectrum antifungal compounds that target the minor groove of DNA
文献作者:Roberts,C.; et al.
参考来源:28th Natl Med Chem Symp (June 8 2002,San Diego) 2002,Abst 67

新产品编号:2360853

Chemical Name: (3S,6R,7R)-N-[5-(N-Hydroxycarbamoyl)pentyl]-6-isobutyl-5,18-dioxo-12-oxa-4-azatricyclo[11.2.2.1(4,7)]octadeca-1(15),13,16-triene-3-carboxamide; 6-[(3S,6R,7R)-6-isobutyl-5,18-dioxo-12-ox...
参考文献标题:Succinimide hydroxamic acids as potent inhibitors of histone deacetylase (HDAC)
文献作者:Curtin,M.L.; et al.
参考来源:28th Natl Med Chem Symp (June 8 2002,San Diego) 2002,Abst 68

新产品编号:2362435

Chemical Name: N2-[2(S)-(3,5-Difluorophenyl)-2-hydroxyacetyl]-N1-[1(S)-(hydroxymethyl)-4-phenylbutyl]-L-alaninamide
项目整合开发状态: Biological Testing
项目研究机构: Elan (Originator), Lilly (Originator)
...
参考文献标题:A series of C-terminal amino alcohol dipeptide Abeta inhibitors
文献作者:Garofalo,A.W.; et al.
参考来源:28th Natl Med Chem Symp (June 8 2002,San Diego) 2002,Abst 11

新产品编号:2364017

Chemical Name: 7-Chloro-4-hydroxy-2-[3-(3-hydroxyphenyl)-1-methyl-2-propynyl]pyridazino[4,5-b]quinoline-1,10(2H,5H)-dione
项目整合开发状态: Biological Testing
项目研究机构: AstraZeneca (Originator)
合成路线:Co...
参考文献标题:Synthesis of 7-chloro-4-hydroxy-2-(3-(aryl/heteroaryl)prop-2-ynyl)1,2,5,10-tetrahydropyridazino[4,5-b]quinoline-1,10-diones (PQD I); potent oral glycine antagonists
文献作者:Horchler,C.L.; et al.
参考来源:28th Natl Med Chem Symp (June 8 2002,San Diego) 2002,Abst 19

新产品编号:2365599

Chemical Name: 2-O-[N-[4-[N-(2,4-Diaminopteridin-6-ylmethyl)-N-methylamino]benzoyl]-L-glutamyl]-3-O-[2-[(4Z,7Z,10Z,13Z,16Z,19Z)-docosa-4,7,10,13,16,19-hexaenoyloxy]-sn-glycero-3-O-phosphocholine inner...
参考文献标题:Synthesis of a novel phosphatidylcholine conjugated to docosahexaenoic acid and methotrexate that inhibits cell proliferation
文献作者:Zerouga,M.; Stillwell,W.; Jenski,L.J.
参考来源:Anti-Cancer Drugs 2002,13(3),301

新产品编号:2367181

Chemical Name: N-(4-Chlorophenyl)-4-(6,7-dimethoxyquinazolin-4-yl)piperazine-1-carboxamide
项目整合开发状态: Preclinical
项目研究机构: Kyowa Hakko (Originator), Millennium (Originator)
合成路线:The title urea ...
参考文献标题:Potent and selective inhibitors of platelet-derived growth factor receptor phosphorylation.1.Synthesis,structure-activity relationship,and biological effects of a new class of quinazoline derivatives
文献作者:Matsuno,K.; Ichimura,M.; Nakajima,T.; Tahara,K.; Fujiwara,S.; Kase,H.; Ushiki,J.; Giese,N.A.; Pandey,A.; Scarborough,R.M.; Lokker,N.A.; Yu,J.C.; Irie,J.; Tsukuda,E.; Ide,S.-i.; Oda,S.; Nomoto,Y.
参考来源:J Med Chem 2002,45(14),3057

新产品编号:2368763

Chemical Name: 2(R)-[4-(7-Bromoquinolin-2-yloxy)phenoxy]propionic acid
项目整合开发状态: Preclinical
项目研究机构: Karmanos Cancer Institute (Originator), Walker Cancer Research Institute (Originator), Wayne ...
参考文献标题:II.Synthesis and biological evaluation of some bioisosteres and congeners of the antitumor agent,2-{4-[(7-chloro-2-quinoxalinyl)oxy]phenox}propionic acid (XK469)
文献作者:Hazeldine,S.T.; Polin,L.; Kushner,J.; White,K.; Bouregeois,N.M.; Crantz,B.; Palomino,E.; Corbett,T.H.; Horwitz,J.P.
参考来源:J Med Chem 2002,45(14),3130

新产品编号:2370345

Chemical Name: 2-[4-(Allyloxy)-3-(trifluoromethoxy)phenyl]-4,5-dihydrooxazole-4-carbohydroxamic acid
项目整合开发状态: Biological Testing
项目研究机构: Chiron (Originator)
合成路线:Coupling of 4-allyloxy-3-tri...
参考文献标题:Potent,novel in vitro inhibitors of the Pseudomonas aeruginosa deacetylase LpxC
文献作者:Kline,T.; Andersen,N.H.; Harwood,E.A.; Bowman,J.; Malanda,A.; Endsley,S.; Erwin,A.L.; Doyle,M.; Fong,S.; Harris,A.L.; Mendelsohn,B.; Mdluli,K.; Raetz,C.R.H.; Stover,K.; Witte,P.R.; Yabannavar,A.; Zhu,S.
参考来源:J Med Chem 2002,45(14),3112

新产品编号:2371927

Chemical Name: N-[2-[4-(Methylsulfonamido)phenyl]ethyl]-N-[2-(naphthalen-1-yloxy)ethyl]acetamide
项目整合开发状态: Biological Testing
项目研究机构: China Pharmaceutical University (Originator), Chinese Academ...
参考文献标题:New p-methylsufonamido phenylamine analogues as class III antiarrhythmic agents: Design,synthesis,biological assay,and 3D-QSAR analysis
文献作者:Liu,H.; Ji,M.; Luo,X.D.; Shen,J.; Huang,X.-P.; Hua,W.; Jiang,H.J.; Chen,K.
参考来源:J Med Chem 2002,45(14),2953

2-IBPO

Chemical Name: 3-[5-[4-(2-Iodobenzyloxy)phenyl]-2-oxo-1,3,4-oxadiazol-3(2H)-yl]propanenitrile
项目整合开发状态: Preclinical
项目研究机构: Osaka University (Originator)
合成路线:Alkylation of ethyl 4-hydroxyben...
参考文献标题:Synthesis and characterization of radioiodinated MD-230254: A new ligand for potential imaging of monoamine oxidase B activity by single photon emission computed tomography
文献作者:Hirata,M.; Kagawa,S.; Yoshimoto,M.; Ohmomo,Y.
参考来源:Chem Pharm Bull 2002,50(5),609