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:1332553

Chemical Name: 4(S)-[2(R)-Benzyl-5(S)-(cyclopentylsulfanylcarboxamido)-6-methyl-4-oxoheptanamido]-6-carbamoyl-2(E)-hexenoic acid ethyl ester
项目整合开发状态: Biological Testing
项目研究机构: Agouron (Origina...
参考文献标题:Structure-based design,synthesis,and biological evaluation of irreversible human rhinovirus 3C protease inhibitors.3.Structure-activity studies of ketomethylene-containing peptidomimetics
文献作者:Dragovich,P.S.; Prins,T.J.; Zhou,R.; Fuhrman,S.A.; Patick,A.K.; Matthews,D.A.; Ford,C.E.; Meador,J.W.III; Ferre,R.A.; Worland,S.T.
参考来源:J Med Chem 1999,42(7),1203

新产品编号:1334135

Chemical Name: 6-Carbamoyl-4(S)-[5(S)-(cyclopentylsulfanylcarboxamido)-6-methyl-2(R)-(4-methylbenzyl)-4-oxoheptanoyl]-2(E)-hexenoic acid ethyl ester
项目整合开发状态: Biological Testing
项目研究机构: Agouron ...
参考文献标题:Structure-based design,synthesis,and biological evaluation of irreversible human rhinovirus 3C protease inhibitors.3.Structure-activity studies of ketomethylene-containing peptidomimetics
文献作者:Dragovich,P.S.; Prins,T.J.; Zhou,R.; Fuhrman,S.A.; Patick,A.K.; Matthews,D.A.; Ford,C.E.; Meador,J.W.III; Ferre,R.A.; Worland,S.T.
参考来源:J Med Chem 1999,42(7),1203

新产品编号:1335717

Chemical Name: 6-Carbamoyl-4(S)-[5(S)-(cyclopentylsulfanylcarboxamido)-2(R)-(4-fluorobenzyl)-6-methyl-4-oxoheptanoyl]-2(E)-hexenoic acid ethyl ester
项目整合开发状态: Biological Testing
项目研究机构: Agouron ...
参考文献标题:Structure-based design,synthesis,and biological evaluation of irreversible human rhinovirus 3C protease inhibitors.3.Structure-activity studies of ketomethylene-containing peptidomimetics
文献作者:Dragovich,P.S.; Prins,T.J.; Zhou,R.; Fuhrman,S.A.; Patick,A.K.; Matthews,D.A.; Ford,C.E.; Meador,J.W.III; Ferre,R.A.; Worland,S.T.
参考来源:J Med Chem 1999,42(7),1203

新产品编号:1337299

Chemical Name: (3R,4R,5'S)-5'-Methylspiro[1-azabicyclo[2.2.1]octane-3,2'-tetrahydrofuran]-4'-one
项目整合开发状态: Biological Testing
项目研究机构: AstraZeneca (Originator)
合成路线:The Horner-Emmons reaction ...
参考文献标题:Synthesis and modeling studies of a potent conformationally rigid muscarinic agonist: 1-Azabicyclo[2.2.1]heptanespirofuranone
文献作者:Wu,E.S.C.; Kover,A.; Semus,S.F.
参考来源:J Med Chem 1998,41(22),4181

BuTAC

Chemical Name: (5R,6R)-3-(1-Azabicyclo[3.2.1]oct-6-yl)-4-(butylsulfanyl)-1,2,5-thiadiazole
项目整合开发状态: Preclinical
项目研究机构: Lilly (Originator), Novo Nordisk (Originator)
合成路线:Alkylation of ethyl...
参考文献标题:Heterocyclic cpds.and their preparation and use
文献作者:Sauerberg,P.; Olesen,P.H.(Novo Nordisk A/S)
参考来源:EP 0544779; JP 1994500542; US 5260314; US 5418240; US 5527813; US 5578602; WO 9203433

新产品编号:1338881

Chemical Name: (5R,6R)-3-(1-Azabicyclo[3.2.1]oct-6-yl)-4-(propylsulfanyl)-1,2,5-thiadiazole
项目整合开发状态: Preclinical
项目研究机构: Lilly (Originator), Novo Nordisk (Originator)
合成路线:Alkylation of ethy...
参考文献标题:Heterocyclic cpds.and their preparation and use
文献作者:Sauerberg,P.; Olesen,P.H.(Novo Nordisk A/S)
参考来源:EP 0544779; JP 1994500542; US 5260314; US 5418240; US 5527813; US 5578602; WO 9203433

新产品编号:1340463

Chemical Name: (5S,6S)-3-(1-Azabicyclo[3.2.1]oct-6-yl)-4-(propylsulfanyl)-1,2,5-thiadiazole
项目整合开发状态: Preclinical
项目研究机构: Lilly (Originator), Novo Nordisk (Originator)
合成路线:Alkylation of ethy...
参考文献标题:Heterocyclic cpds.and their preparation and use
文献作者:Sauerberg,P.; Olesen,P.H.(Novo Nordisk A/S)
参考来源:EP 0544779; JP 1994500542; US 5260314; US 5418240; US 5527813; US 5578602; WO 9203433

WHI-05

Chemical Name: 3'-Azido-5-bromo-5'-O-[4-methoxyphenoxy[1-(methoxycarbonyl)ethylamino]phosphoryl]-3'-deoxy-6-methoxy-5,6-dihydrothymidine
项目整合开发状态: Preclinical
项目研究机构: Parker Hughes Institute (Or...
参考文献标题:AZT derivs.exhibiting spermicidal and anti-viral activity
文献作者:Uckun,F.M.; Venkatachalam,T.; D'Cruz,O.(Parker Hughes Institute)
参考来源:WO 9948902

新产品编号:1342045

Chemical Name: 2-[(E)-2-(3,4-Dihydroxyphenyl)vinyl]-8-hydroxyquinoline-7-carboxylic acid
项目整合开发状态: Biological Testing
项目研究机构: CNRS (Originator)
合成路线:8-Hydroxyquinaldine (I) reacts with KOH in...
参考文献标题:Quinoline derivs.,having in particular antiviral properties,preparation and biological applications thereof
文献作者:Desmaele,D.; Auclair,C.; D'Angelo,J.; Subra,F.; Mouscadet,J.-F.; Mekouar,K.(CNRS (Centre National de la Recherche Scientifique))
参考来源:WO 9845269

S-34109

Chemical Name: 7-[3(R)-(Aminomethyl)-4(S)-(trifluoromethyl)pyrrolidin-1-yl]-1-cyclopropyl-6-fluoro-8-methoxy-4-oxo-1,4-dihydroquinoline-3-carboxylic acid hydrochloride
项目整合开发状态: Preclinical
项目研究...
参考文献标题:Synthesis and antibacterial activity of novel 7-(3-substituted-3 or 4-trifluoromethyl-1-pyrrolidinyl)-8-methoxyfluoroquinolones
文献作者:Fukui,H.; Shibata,T.; Naito,T.; Nakano,J.; Maejima,T.; Senda,H.; Iwatani,W.; Tatsumi,Y.; Suda,M.; Arika,T.
参考来源:Bioorg Med Chem Lett 1998,8(20),2833