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:1677429

Chemical Name: N-[1-Amidino-2-hydroxypiperidin-3(R)-yl]-3(S)-(benzylsulfonamido)-7-methoxy-2-oxo-2,3,4,5-tetrahydro-1H-1-benzazepine-1-acetamide trifluoroacetate
项目整合开发状态: Biological Testing
项目研...
参考文献标题:Novel benzo-fused lactam scaffolds as factor Xa inhibitors
文献作者:Tamura,S.Y.; Goldman,E.A.; Bergum,P.W.; Semple,J.E.
参考来源:Bioorg Med Chem Lett 1999,9(17),2573

新产品编号:1679011

Chemical Name: 4-Amino-5-chloro-2-methoxy-N-[1-[2-(methylsulfonamido)ethyl]piperidin-4-ylmethyl]benzamide oxalate
项目整合开发状态: Preclinical
项目研究机构: Mitsubishi Pharma (Originator)
合成路线:4-Amino-5-c...
参考文献标题:Synthesis and pharmacological evaluation of carboxamide derivatives as selective serotoninergic 5-HT4 receptor agonists
文献作者:Itoh,K.; kanzaki,K.; Ikebe,T.; Kuroita,T.; Tomozane,H.; Sonda,S.; Sato,N.; Haga,K.; Kawakita,T.
参考来源:Eur J Med Chem 1999,34(11),977

MC-03,971

Chemical Name: 3-[2-(L-Alanylamino)-4-(2-aminoethylsulfanylmethyl)thiazol-5-ylsulfanyl]-7-[2-(2-amino-4-chlorothiazol-5-yl)-2-(hydroxyimino)acetamido]-3-cephem-4-carboxylic acid inner salt
项目整合开发状态...
参考文献标题:Design,synthesis and in vitro antibacterial properties of novel 3-heteroarylthio cephems with anti-MRSA activity: Amino acid prodrug approach to solubility improvement
文献作者:Glinka,T.; Price,M.; Halas,S.; Calkins,T.; Frith,R.; Nudelman,G.; Whitehead,C.; Cho,A.; Hecker,S.; Ludwikow,M.; Chamberland,S.; Crawford,J.; Lee,V.
参考来源:39th Intersci Conf Antimicrob Agents Chemother (Sept 26 1999,San Francisco) 1999,Abst F391

MC-02,867

Chemical Name: (6R,7R)-3-[4-(2-Aminoethylsulfanylmethyl)-1,2,3-thiadiazol-5-ylsulfanyl]-7-[2-(6-aminopyridin-2-yl)-2-(hydroxyimino)acetamido]-3-cephem-4-carboxylic acid
项目整合开发状态: Preclinical
项目研...
参考文献标题:Design,synthesis,and SAR of water-soluble dibasic cephalosporins active against resistant Gram-positive bacteria
文献作者:Lee,V.J.; Price,M.; Zhang,Z.J.; Fan,A.; Glinka,T.; Chamberland,S.; Cho,A.; Ludwikow,M.; Hecker,S.J.; Liu,N.
参考来源:39th Intersci Conf Antimicrob Agents Chemother (Sept 26 1999,San Francisco) 1999,Abst F392

MC-03,260

Chemical Name: (6R,7R)-3-[4-(2-Aminoethylsulfanylmethyl)thiazol-5-ylsulfanyl]-7-[2-(6-aminopyridin-2-yl)-2-(hydroxyimino)acetamido]-3-cephem-4-carboxylic acid
项目整合开发状态: Preclinical
项目研究机构: Essen...
参考文献标题:Design,synthesis,and SAR of water-soluble dibasic cephalosporins active against resistant Gram-positive bacteria
文献作者:Lee,V.J.; Price,M.; Zhang,Z.J.; Fan,A.; Glinka,T.; Chamberland,S.; Cho,A.; Ludwikow,M.; Hecker,S.J.; Liu,N.
参考来源:39th Intersci Conf Antimicrob Agents Chemother (Sept 26 1999,San Francisco) 1999,Abst F392

LB-10827

Chemical Name: 7-[2-(2-Amino-5-chlorothiazol-4-yl)-2-(hydroxyimino)acetamido]-3-(2,6-diaminopyrimidin-4-ylsulfanylmethylsulfanyl)-3-cephem-4-carboxylic acid
项目整合开发状态: Preclinical
项目研究机构: LG Chem...
参考文献标题:Novel cephalosporin cpds.,processes for preparation thereof and antimicrobial compsns.containing the same
文献作者:Kim,M.Y.; Oh,S.H.; Kim,Y.Z.; Moon,K.Y.; Lee,C.S.; Ryu,E.J.; Paek,K.S.; Lee,S.H.(LG Chem Ltd.)
参考来源:WO 9958535

A-255916

Chemical Name: 1-Cyclopropyl-7-fluoro-9-methyl-4-oxo-8-(1,2,3,4-tetrahydro-7-isoquinolinyl)-4H-quinolizine-3-carboxylic acid hydrochloride
项目整合开发状态: Biological Testing
项目研究机构: Abbott (Originator...
参考文献标题:Synthesis and antibacterial activity of C-8 carbon-linked 2-pyridones
文献作者:Bui,M.; Nilius,A.; Nan,Y.; Marron,T.; Stone,G.; Baranowski,J.; Shen,L.; Schultz,C.C.; Raney,P.; Snyder,R.; Or,Y.S.
参考来源:39th Intersci Conf Antimicrob Agents Chemother (Sept 26 1999,San Francisco) 1999,Abst F560

新产品编号:1680593

Chemical Name: 1-[4-[N-(4-Benzyloxyphenyl)-N-(3-methylbut-2-enyl)amino]piperidin-1-yl]-1-[4-isopropyl-1-(3-methylbutyl)piperazin-2-yl]methanone
项目整合开发状态: Biological Testing
项目研究机构: Pfizer (Origi...
参考文献标题:Heterocyclic substd.aniline calcium channel blockers
文献作者:Ryder,T.R.; Rafferty,M.F.; Hu,L.-Y.(Pfizer Inc.)
参考来源:US 6251919; WO 9943658

新产品编号:1682175

Chemical Name: 4,4'-(Furan-2,5-diyl)bis[N-(4-fluorophenoxycarbonyl)benzamidine]
项目整合开发状态: Preclinical
项目研究机构: Georgia State University (Originator), University of North Carolina (Originator)
...
参考文献标题:Prodrugs for amidines: Synthesis and anti-Pneumocystis carinii activity of carbamates of 2,5-bis(4-amidinophenyl)furan
文献作者:Rahmathullah,S.M.; Hall,J.E.; Bender,B.C.; McCurdy,D.R.; Tidwell,R.R.; Boykin,D.W.
参考来源:J Med Chem 1999,42(19),3994

新产品编号:1683757

Chemical Name: 4-(6-Amino-4-oxo-3,4-dihydroquinazolin-3-yl)butanoic acid ethyl ester
项目整合开发状态: Preclinical
项目研究机构: University of California, San Diego (Originator)
合成路线:Condensation of 5-nitr...
参考文献标题:Substituted isoquinolines and quinazolines as potential antiinflammatory agents.Synthesis and biological of inhibitors of tumor necrosis factor alpha
文献作者:Chao,Q.; Deng,L.; Shih,H.; Leoni,L.M.; Genini,D.; Carson,D.A.; Cottam,H.B.
参考来源:J Med Chem 1999,42(19),3860