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:1704323

Chemical Name: (5R,6S)-2-[6-(2-Aminopyridinium-1-ylmethyl)naphth-2-yl]-6-[1(R)-hydroxyethyl]carbapen-2-em-3-carboxylate inner salt
项目整合开发状态: Biological Testing
项目研究机构: Merck & Co. (Originator) 参考文献标题:2-Naphthyl-carbapenem antibacterial agents
文献作者:DiNinno,F.P.; Greenlee,M.L.(Merck & Co.,Inc.)
参考来源:EP 0466254; JP 1992253980; US 5032587

新产品编号:1705905

Chemical Name: 5-(4-Aminophenyl)-N-methyl-8-oxo-8,9-dihydro-7H-[1,3]dioxolo[4,5-h][2,3]benzodiazepine-7-carboxamide
项目整合开发状态: Preclinical
项目研究机构: Universit?degli Studi di Catanzaro (Originator),...
参考文献标题:Synthesis and anticonvulsant activity of novel and potent 2,3-benzodiazepine AMPA/kainate receptor antagonists
文献作者:Grasso,S.; De Sarro,G.; De Sarro,A.; Micale,N.; Zappala,M.; Pula,G.; Baraldi,M.; De Micheli,C.
参考来源:J Med Chem 1999,42(21),4414

SH-3/24

Chemical Name: cis-N-[3-[3,5-Dimethyl-4-(3-phenylpropyl)piperazin-1-yl]propyl]-N,N-diphenylamine hydrochloride
项目整合开发状态: Preclinical
项目研究机构: National Institute on Drug Abuse (Originator), Nation...
参考文献标题:Structure-activity relationships at the monoamine transporters and sigma receptors for a novel series of 9-[3-(cis-3,5-dimethyl-1-piperazinyl)-propyl]carbazole (rimcazole) analogues
文献作者:Husbands,S.M.; Izenwasser,S.; Kopajtic,T.; Bowen,W.D.; Vilner,B.J.; Katz,J.L.; Newman,A.H.
参考来源:J Med Chem 1999,42(21),4446

CGS-35066

Chemical Name: 3-(Dibenzo[b,d]furan-3-yl)-2(S)-(phosphonomethylamino)propionic acid
项目整合开发状态: Preclinical
项目研究机构: Novartis (Originator)
合成路线:Condensation of 1-formyl-2-isopropylhydrazine (I) ...
参考文献标题:Anti-inflammatory activity of 2-acyl-5(3)-hydroxytetrahydro-1H-pyrazole derivatives
文献作者:Zelenin,K.N.; et al.
参考来源:Arzneim-Forsch Drug Res 1999,49(2),843

新产品编号:1707487

Chemical Name: 2-Formyl-3-hydroxy-1-isopropyl-1-methylpyrazolidin-1-ium iodide
项目整合开发状态: Preclinical
项目研究机构: Military Medical Academy (Originator), St. Petersburg Chem.-Pharm. Acad (Originator)<...
参考文献标题:Anti-inflammatory activity of 2-acyl-5(3)-hydroxytetrahydro-1H-pyrazole derivatives
文献作者:Zelenin,K.N.; et al.
参考来源:Arzneim-Forsch Drug Res 1999,49(2),843

CGS-34043

Chemical Name: N-[2-(Dibenzo[b,d]furan-3-yl)-1(S)-(1H-tetrazol-5-yl)ethyl]aminomethylphosphonic acid
项目整合开发状态: Preclinical
项目研究机构: Novartis (Originator)
合成路线:The chiral amino acid (V) was pre...
参考文献标题:Potent and selective non-peptidic inhibitors of endothelin-converting enzyme-1 with sustained duration of action
文献作者:De Lombaert,S.; Blanchard,L.; Stamford,L.B.; Tan,J.; Wallace,E.M.; Satoh,Y.; Fitt,J.; Hoyer,D.; Simonsbergen,D.; Moliterni,J.; Marcopoulos,N.; Savage,P.; Chou,M.; Trapani,A.J.; Jeng,A.Y.
参考来源:J Med Chem 2000,43(3),488

新产品编号:1709069

Chemical Name: 9-Methoxy-2-(3,4,5-trimethoxyphenyl)-3,4-dihydro-2H-[1]benzopyrano[2,3-d]pyrimidin-4-one
项目整合开发状态: Biological Testing
项目研究机构: Cancer Research UK (Originator), De Montfort Universi...
参考文献标题:Synthesis and anticancer activities of 4-oxobenzopyrano[2,3-d]pyrimidines
文献作者:Hadfield,J.A.; Pavlidis,V.H.; Perry,P.J.; McGown,A.T.
参考来源:Anti-Cancer Drugs 1999,10(6),591

QYL-972

Chemical Name: 2(S)-[2-[(Z)-2-Amino-6-methoxy-9H-purin-9-ylmethylene]cyclopropylmethoxy(phenoxy)phosphorylamino]propionic acid methyl ester; (Z)-N-[2-(2-Amino-6-methoxypurin-9-ylmethylene)cyclopropylm...
参考文献标题:Synthesis and antiviral activity of phosphoralaninate derivatives of methylenecyclopropane analogues of nucleosides
文献作者:Kern,E.R.; Qiu,Y.-L.; Ptak,R.G.; Breitenbach,J.M.; Zemlicka,J.; Drach,J.C.; Cheng,Y.-C.; Lin,J.-S.
参考来源:Antivir Res 1999,43(1),37

TT-2

Chemical Name: 3-Methoxy-1,4,5,8,9,10-hexahydro-9,10[1',2']-benzenoanthracene-1,4,5,8-tetraone
项目整合开发状态: Biological Testing
项目研究机构: Kansas State University (Originator)
合成路线:The reduction of ...
参考文献标题:Triptycene analogs
文献作者:Hua,D.H.; Perchellet,J.-P.(Kansas State University)
参考来源:WO 0228808

TT-13

Chemical Name: 2-Bromo-3-methoxy-1,4,5,8,9,10-hexahydro-9,10[1',2']-benzenoanthracene-1,4,5,8-tetraone
项目整合开发状态: Biological Testing
项目研究机构: Kansas State University (Originator)
合成路线:The reduc...
参考文献标题:Triptycene analogs
文献作者:Hua,D.H.; Perchellet,J.-P.(Kansas State University)
参考来源:WO 0228808