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

J-109404

Chemical Name: 1,11-Dihydroxy-12-(beta-D-glucopyranosyl)-6-[2-hydroxy-1-(hydroxymethyl)ethylamino]-12,13-dihydro-4cH-indolo[2,3-a]pyrrolo[3,4-c]carbazole-5,7(6H,7aH)-dione
项目整合开发状态: Preclinical
...
参考文献标题:Synthesis and biological activities of topoisomerase I inhibitors,6-N-amino analogues of NB-506
文献作者:Ohkubo,M.; Kojiri,K.; Kondo,H.; Tanaka,S.; Kawamoto,H.; Nishimura,T.; Nishimura,I.; Yoshinari,T.; Arakawa,H.; Suda,H.; Morishima,H.; Nishimura,S.
参考来源:Bioorg Med Chem Lett 1999,9(9),1219

新产品编号:1561943

Chemical Name: 2-(6-Methoxy-3,4-dihydro-1-naphthyl)-4H-3,1-benzoxazin-4-one
项目整合开发状态: Preclinical
项目研究机构: Domp?(Originator)
合成路线:Condensation of of 2-iodoaniline (I) with vinyl triflate (II) ...
参考文献标题:Synthesis and in vitro and in vivo evaluation of the 2-(6'methoxy-3',4'-dihydro-1'-naphtyl)-4H-3,1-benzoxazin-4-one as a new potent substrate inhibitor of human leukocyte elastase
文献作者:Arcadi,A.; Asti,C.; Brandolini,L.; Caselli,G.; Marinelli,F.; Ruggieri,V.
参考来源:Bioorg Med Chem Lett 1999,9(9),1291

新产品编号:1563525

Chemical Name: 4-[1-[N-[2-(Dimethylamino)ethyl]-N-benzylamino]-1-phenylmethyl]-N,N-diethylbenzamide
项目整合开发状态: Preclinical
项目研究机构: Organon (Originator)
合成路线:4-Benzoylbenzoic acid (I) was reduc...
参考文献标题:Synthesis of novel analogues of the delta opioid ligand SNC-80 using AlCl3-promoted aminolysis
文献作者:Barn,D.R.; Bom,A.; Cottney,J.; Caulfield,W.L.; Morphy,J.R.
参考来源:Bioorg Med Chem Lett 1999,9(9),1329

GW-0072

Chemical Name: (?-(2S*,5S*)-4-[4-[5-[2-(Dibenzylamino)-2-oxoethyl]-2-heptyl-4-oxothiazolidin-3-yl]butyl]benzoic acid
项目整合开发状态: Preclinical
项目研究机构: Affymax (Originator), GlaxoSmithKline (Originat...
参考文献标题:PPARgamma ligands
文献作者:Willson,T.M.; Holmes,C.P.; Collins,J.L.; Lenhard,J.M.(Glaxo Group Ltd.)
参考来源:WO 0027832

新产品编号:1565107

Chemical Name: 1',2,3,3',4,4',5,5',6',7',7,8,8',9,9',10,10'-Heptadecahydro-6-mercapto-1,2'-bisdecaborate(4-) tetrasodium salt
项目整合开发状态: Preclinical
项目研究机构: Southwest Texas State University (Orig...
参考文献标题:Synthesis and in vivo murine evaluation of Na4[1-(1'-B10H9)-6-SHB10H8] as a potential agent for boron neutron capture therapy
文献作者:Feakes,D.A.; Waller,R.C.; Hathaway,D.K.; Morton,V.S.
参考来源:Proc Natl Acad Sci USA 1999,96(11),6406

ONO-4817

Chemical Name: N-[1(S)-(Ethoxymethoxymethyl)-4-(hydroxyamino)-3(S)-methyl-4-oxobutyl]-4-phenoxybenzamide
项目整合开发状态: Phase I
项目研究机构: Ono (Originator)
合成路线:Coupling of 4(S)-amino-4-carboxybutyri...
参考文献标题:Aminobutanoic acid derivs.
文献作者:Sugiura,T.; Takahashi,K.(Ono Pharmaceutical Co.,Ltd.)
参考来源:EP 1024134; WO 9919296

Me[18F]FBWAY

Chemical Name: 4-(18Fluoro)-3-methyl-N-[2-[4-(2-methoxyphenyl)piperazin-1-yl]ethyl]-N-(2-pyridinyl)benzamide
项目整合开发状态: Preclinical
项目研究机构: Lilly (Originator)
合成路线:Condensation of 4-(dimethyla...
参考文献标题:Development of fluorine-18-labeled 5-HT1A antagonists
文献作者:Lang,L.; Jagoda,E.; Schmall,B.; Vuong,B.K.; Adams,H.R.; Nelson,D.L.; Carson,R.E.; Eckelman,W.C.
参考来源:J Med Chem 1999,42(9),1576

S-22575, PMS-889

Chemical Name: 2-(4,5-Dihydro-1H-imidazol-2-yl)-1,4-bis(2-methylpropyl)piperazine
项目整合开发状态: Preclinical
项目研究机构: Servier (Originator)
合成路线:Alkylation of ethyl piperazine-2-carboxylate (I) with...
参考文献标题:Design and synthesis of imidazoline derivatives active on glucose homeostasis in a rat model of type II diabetes.2.Syntheses and biological activities of 1,4-dialkyl-,1,4-dibenzyl,and 1-benzyl-4-alkyl-2-(4',5'-dihydro-1'H-imidazol-2'-yl)piperazines an
文献作者:Le Bihan,G.; Rondu,F.; Pele-Tounian,A.; Wang,X.; Lidy,S.; Touboul,E.; Lamouri,A.; Dive,G.; Huet,J.; Pfeiffer,B.; Renard,P.; Guardiola-Lemaitre,B.; Manechez,D.; Penicaud,L.; Ktorza,A.; Godfroid,J.J.
参考来源:J Med Chem 1999,42(9),1587

新产品编号:1566689

Chemical Name: 1-(4-Chlorophenyl)-3-(hydroxymethyl)-9H-pyrido[3,4-b]indole
项目整合开发状态: Preclinical
项目研究机构: Central Drug Research Institute (Originator)
合成路线:Esterification of L-tryptophan (I) b...
参考文献标题:Potent 1,3-disubstituted-9H-pyrido[3,4-b]indoles as new lead compounds in antifilarial chemotherapy
文献作者:Srivastava,S.K.; Agarwal,A.; Chauhan,P.M.; Agarwal,S.K.; Bhaduri,A.P.; Singh,S.N.; Fatima,N.; Chatterjee,R.K.
参考来源:J Med Chem 1999,42(9),1667

新产品编号:1568271

Chemical Name: N-(Cyclopropylmethyl)-3-methoxy-6,7-didehydro-1'H-indolo[2',3':6,7]morphinan-4-ol
项目整合开发状态: Biological Testing
项目研究机构: National Institute on Drug Abuse (Originator), National Inst...
参考文献标题:delta Opioid affinity and selectivity of 4-hydroxy-3-methoxyindolomorphinan analogues related to naltrindole
文献作者:Coop,A.; Rothman,R.B.; Dersch,C.; Partilla,J.; Porreca,F.; Davis,P.; Jacobson,A.E.; Rice,K.C.
参考来源:J Med Chem 1999,42(9),1673