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

PNU-176798

Chemical Name: N-[3-[4-(5-Cyanothiazol-2-yl)-3-fluorophenyl]-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:Nitrile (II) was prepared from the ...
参考文献标题:Synthesis and antibacterial activity of azolylphenyl oxazolidinones having carbon-bound 1,3-thiazolyl rings
文献作者:Genin,M.J.; Grega,K.C.; Ford,C.W.; Barbachyn,M.R.; Walker,E.A.; Gadwood,R.C.; Thomasco,L.M.; Zurenko,G.E.
参考来源:38th Intersci Conf Antimicrob Agents Chemother (Sept 24 1998,San Diego) 1998,Abst F-139

ENC-22-HP

Chemical Name: 1-Cyclopropyl-7-[4-[2,2-bis(diethoxyphosphoryl)ethyl]piperazin-1-yl]-6-fluoro-4-oxo-1,4-dihydroquinoline-3-carboxylic acid
项目整合开发状态: Biological Testing
项目研究机构: ElizaNor Biopharmac...
参考文献标题:Diphosphonate derivs.of therapeutic agents
文献作者:Herczegh,P.; Sztaricskai,F.J.; Farcasiu,D.; Hartmann,J.F.(ElizaNor Biopharmaceuticals,Inc.)
参考来源:US 5880111; WO 9640190

ENC-41-HP

Chemical Name: 1-Cyclopropyl-7-[4-(2,2-diphosphonoethyl)piperazin-1-yl]-6-fluoro-4-oxo-1,4-dihydroquinoline-3-carboxylic acid
项目整合开发状态: Biological Testing
项目研究机构: ElizaNor Biopharmaceuticals (Or...
参考文献标题:Osteoadsorptive bisphosphonate derivatives of fluoroquinolone antibacterials
文献作者:Herczegh,P.; Buxton,T.B.; McPherson,J.C.III.; Kov醕s-Kulyassa,A.; Brewer,P.D.; Sztaricskai,F.; Stroebel,G.G.; Plowman,K.M.; Farcasiu,D.; Hartmann,J.F.
参考来源:J Med Chem 2002,45(11),2338

新产品编号:1297749

Chemical Name: (+)-cis-4-Methyl-5-pentylpyrrolidin-2-imine hydrochloride
项目整合开发状态: Preclinical
项目研究机构: Pfizer (Originator)
合成路线:Michael addition of 1-nitrohexane (I) to methyl crotonate (II) ...
参考文献标题:2-Iminopyrrolidines as potent and selective inhibitors of human inducible nitric oxide synthase
文献作者:Hagen,T.J.; Bergmanis,A.A.; Kramer,S.W.; Fok,K.F.; Schmelzer,A.E.; Pitzele,B.S.; Swenton,L.; Jerome,G.M.; Kornmeier,C.M.; Moore,W.M.; Branson,L.F.; Connor,J.R.; Manning,P.T.; Currie,M.G.; Hallinan,E.A.
参考来源:J Med Chem 1998,41(19),3675

新产品编号:1299331

Chemical Name: (3R*,5S*,9R* and9S*)-3-Carboxy-10-(3-chlorofluoren-9-yl)-3,5-dihydroxydecanoic acid
项目整合开发状态: Preclinical
项目研究机构: GlaxoSmithKline (Originator)
合成路线:1) Wittig reaction of 2,4-di...
参考文献标题:ATP-citrate lyase as a target for hypolipidemic intervention.2.Synthesis and evaluation of (3R*,5S*)-omega-substituted-3-carboxy-3,5-dihydroxyalkanoic acids and their gamma-lactone prodrugs as inhibitors of the enzyme in vitro and in vivo
文献作者:Gribble,A.D.; Ife,R.J.; Shaw,A.; McNair,D.; Novelli,C.E.; Bakewell,S.; Shah,V.P.; Dolle,R.E.; Groot,P.H.; Pearce,N.; Yates,J.; Tew,D.; Boyd,H.; Ashman,S.; Eggleston,D.S.; Haltiwanger,R.C.; Okafo,G.
参考来源:J Med Chem 1998,41(19),3582

新产品编号:1300913

Chemical Name: (3R,6S,8aS)-6-(Benzylsulfonamido)-N-(3-guanidinopropyl)-5-oxohexahydro-5H-thiazolo[3,2-a]pyridine-3-carboxamide bis(trifluoroacetate)
项目整合开发状态: Biological Testing
项目研究机构: Novartis...
参考文献标题:Rational design,synthesis,and X-ray structure of selective noncovalent thrombin inhibitors
文献作者:Wagner,J.; Kallen,J.; Ehrhardt,C.; Evenou,J.-P.; Wagner,D.
参考来源:J Med Chem 1998,41(19),3664

新产品编号:1302495

Chemical Name: 7-O-(4'-O-Acetyl-2',3',6'-trideoxy-3'-iodo-alpha-L-mannopyranosyl)daunomycinone
项目整合开发状态: Biological Testing
项目研究机构: Servier (Originator)
合成路线:Reduction of ketone (I) with NaBH...
参考文献标题:Design,synthesis and biological activity of 7-O-(4-O-acetyl-3-iodo-2,3,6-trideoxy-alpha-L-arabino-hexopyranosyl)daunomycinone and 7-O-(3-chloro-2,3,6-trideoxy-4-O-propanoyl-alpha-L-lyxo-hexopyranosyl)daunomycinone
文献作者:Aligiannis,N.; Pouli,N.; Marakos,P.; Mitaku,S.; Skaltsounis,A.L.; Leonce,S.; Pierre,A.; Atassi,G.
参考来源:Chem Pharm Bull 2000,48(1),150

新产品编号:1304077

Chemical Name: 2,3,4-Tri-O-acetyl-1-O-(3-butyl-3-ethyl-5-phenyl-2,3,4,5-tetrahydro-1,4-benzothiazepin-8-yl)-beta-D-glucopyranuronic acid methyl ester S,S-dioxide
项目整合开发状态: Biological Testing
项目研...
参考文献标题:Carbohydrate prodrugs: potential use for in situ activation and drug delivery
文献作者:Walker,E.H.; Palomino,E.; Blumenthal,S.L.
参考来源:Drugs Fut 1991,16(11),1029

新产品编号:1305659

Chemical Name: (1R,5S,6S)-2-[1,1-Dimethyl-2(S)-(piperazin-1-ylcarbonyl)pyrrolidinium-4(S)-ylsulfanyl]-6-[1(R)-hydroxyethyl]-1-methyl-1-carbapen-2-em-3-carboxylate hydrochloride
项目整合开发状态: Preclinica...
参考文献标题:Carbapenem derivs.having antibiotic activity,their preparation and their use
文献作者:Kawamoto,I.; Miyauchi,M.; Nakayama,E.; Endo,R.; Ohya,S.; Utsui,Y.(Sankyo Co.,Ltd.)
参考来源:EP 0443883; JP 1992211083; US 5310735

CGP-75254A

Chemical Name: 2-[N-[2-[N-(Ethoxycarbonylmethyl)-N-(2-hydroxybenzyl)amino]ethyl]-N-(2-hydroxybenzyl)amino]acetic acid sodium salt
项目整合开发状态: Preclinical
项目研究机构: Novartis (Originator)
合成路线:Este...
参考文献标题:IL-8 receptor antagonists
文献作者:Bryan,D.L.; Gleason,J.G.; Widdowson,K.L.(SmithKline Beecham plc)
参考来源:WO 9806398