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:2413059

Chemical Name: N-[2-(1H-Indol-3-yl)ethyl]-3-[3-(2-thiazolyl)ureido]benzenesulfonamide; N-[3-[N-[2-(1H-Indol-3-yl)ethyl]sulfamoyl]phenyl]-N'-(2-thiazolyl)urea
项目整合开发状态: Preclinical
项目研究机构: Bayer ...
参考文献标题:Phenyl-thiazolylurea-sulfonamides as novel inhibitors of phenylalanine-tRNA synthetase
文献作者:Beyer,D.; Kroll,H.; Bauser,M.; Siegel,S.; Brotz,H.; Endermann,R.; Schiffer,G.; Ziegelbauer,K.; Habich,D.; Pohlmann,J.
参考来源:42nd Intersci Conf Antimicrob Agents Chemother (Sept 27 2002,San Diego) 2002,Abst F-756

PNU-293180

Chemical Name: N-[3-[3-Fluoro-4-(3-oxetanyl)phenyl]-2-oxooxazolidin-5(S)-ylmethyl]acetamide
项目整合开发状态: Preclinical
项目研究机构: Pfizer (Originator)
合成路线:Condensation of 2-fluoro-4-nitrotoluene (I) ...
参考文献标题:Synthesis and antibacterial activities of oxazolidinones incorporating C-ring oxetanes and thietanes
文献作者:Hao,Y.; Barbachyn,M.R.; Greene,M.L.; et al.
参考来源:42nd Intersci Conf Antimicrob Agents Chemother (Sept 27 2002,San Diego) 2002,Abst F-1321

A-00000762, A-762

Chemical Name: 2-(4-Nitrophenyl)benzo-1,4-quinone
项目整合开发状态: Biological Testing
项目研究机构: Arrow Therapeutics (Originator)
合成路线:Diazotization of 4-nitroaniline (I) with NaNO2 in cold concentrated...
参考文献标题:The identification of nanomolar 1,4-benzoquinone inhibitors of shikimate kinase
文献作者:Reynolds,K.; et al.
参考来源:42nd Intersci Conf Antimicrob Agents Chemother (Sept 27 2002,San Diego) 2002,Abst F-745

新产品编号:2414641

Chemical Name: N,N'-(4-Bromo-1,2-phenylene)bis(5-chlorothiophene-2-sulfonamide)
项目整合开发状态: Preclinical
项目研究机构: Arrow Therapeutics (Originator)
合成路线:Acylation of 4-bromo-2-nitroaniline (I) with...
参考文献标题:Bis(sulfonamides) as inhibitors of aroB.Unsymmetrical sulfonamide substitution and diamine core SAR
文献作者:Cockerill,G.S.; et al.
参考来源:42nd Intersci Conf Antimicrob Agents Chemother (Sept 27 2002,San Diego) 2002,Abst F-739

OPT-11

Chemical Name: 1-O,1'-O-(Butane-1,4-diyl)bis(methylimino)bis[1(S)-hydroxyethylene]bis(oxy)bis[4(R),6(S)-diamino-3(S)-hydroxycyclohexan-2(R),1(R)-diyl]bis(2,6-diamino-2,6-dideoxy-alpha-D-glucopyranose)...
参考文献标题:The synthesis and biological activity of multivalent aminoglycoside analogues of OPT-11
文献作者:Liang,C.; Duffield,J.J.; Marby,K.A.; Rabuka,D.; Romero,A.; Sgarbi,P.W.M.; Shue,Y.-K.; Sucheck,J.; Yao,S.; Zhang,Z.; Cheng,M.; Chan,F.K.; Hu,C.; Ng,S.P.; Hwang,S.-B.
参考来源:42nd Intersci Conf Antimicrob Agents Chemother (Sept 27 2002,San Diego) 2002,Abst F-1687

JNJ-10391849

Chemical Name: N-[3-[3-Fluoro-4-[2-(2-pyridyl)-5,7-dihydro-6H-pyrrolo[3,4-d]pyrimidin-6-yl]phenyl]-2-oxooxazolidin-5(S)-ylmethyl]acetamide
项目整合开发状态: Preclinical
项目研究机构: Johnson & Johnson (Origin...
参考文献标题:Antibacterial heterobicyclic substd.phenyl oxazolidinones
文献作者:Hlasta,D.; Paget,S.(Ortho-McNeil Pharmaceutical,Inc.)
参考来源:EP 1206469; US 6413981; WO 0142242

VRC-4334

Chemical Name: 3(R)-Amino-5(R)-hydroxy-6-(methylamino)hexanoic acid 2-(carboxymethyl)-2-methylhydrazide ; 2-[2-[3(R)-Amino-5(R)-hydroxy-6-(methylamino)hexanoyl]-1-methylhydrazino]acetic acid
项目整合开发...
参考文献标题:N- and C-terminal modifications of negamycin
文献作者:Raju,B.; Mortell,K.; O'Dowd,H.; et al.
参考来源:42nd Intersci Conf Antimicrob Agents Chemother (Sept 27 2002,San Diego) 2002,Abst F-1685

VRC-3885

Chemical Name: N-[3-[3-Fluoro-4-(1-oxothiomorpholin-4-yl)phenyl]-2-oxooxazolidin-5(S)-ylmethyl]-3-[4-(methoxyiminomethyl)phenyl]-2-propenamide
项目整合开发状态: Biological Testing
项目研究机构: Vicuron Pharma...
参考文献标题:Combinatorial lead optimization of oxazolidinones: In vitro activity of novel 5-amidomethyl thiomorpholine S-oxide and S,S-dioxide phenyloxazolidiones
文献作者:Zhou,J.; et al.
参考来源:42nd Intersci Conf Antimicrob Agents Chemother (Sept 27 2002,San Diego) 2002,Abst F-1319

DRF-8569

Chemical Name: N-[3-[4-[(E)-2-(2H-1,2,3-Benzotriazol-2-yl)-2-cyanovinyl]phenyl]-2-oxooxazolidin-5(S)-ylmethyl]thioacetamide
项目整合开发状态: Biological Testing
项目研究机构: Dr. Reddy's Laboratories (Origina...
参考文献标题:Geometrical and regioisomeric effects on biological activity of some novel stilbene-type oxazolidinones
文献作者:Das,J.; et al.
参考来源:42nd Intersci Conf Antimicrob Agents Chemother (Sept 27 2002,San Diego) 2002,Abst F-1325

DRL-11286

Chemical Name: N-[3-[(3aS)-2,3,3a,4-Tetrahydro-1H-pyrrolo[2,1-c][1,4]benzothiazin-7-yl]-2-oxooxazolidin-5(S)-ylmethyl]thiocarbamic acid O-methyl ester
项目整合开发状态: Biological Testing
项目研究机构: Dr. Re...
参考文献标题:SAR studies on certain conformationally constrained oxazolidinones
文献作者:Selvakumar,N.; Reddy,B.Y.; Kumar,G.S.; Khera,M.K.; Srinivas,D.; Kumar,M.S.; Das,J.; Iqbal,J.; Trehan,S.
参考来源:42nd Intersci Conf Antimicrob Agents Chemother (Sept 27 2002,San Diego) 2002,Abst F-1324