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

SB-T-1250

Chemical Name: [2aR-[2alpha,4beta,4abeta,6beta,9alpha(2R,3S),11beta,12alpha,12aalpha,12balpha]]-6,12b-Diacetoxy-12-benzoyloxy-9-[3-(tert-butoxycarbonylamino)-3-[2,2-dimethyl-1(R)-cyclopropyl]-2-hydrox...
参考文献标题:Syntheses and biological activity of advanced second-generation taxoids
文献作者:Lin,S.; et al.
参考来源:216th ACS Natl Meet (Aug.23-27,Boston) 1998,Abst MEDI 315

SB-T-1251

Chemical Name: [2aR-[2alpha,4beta,4abeta,6beta,9alpha(2R,3S),11beta,12alpha,12aalpha,12balpha]]-12b-Acetoxy-12-benzoyloxy-9-[3-(tert-butoxycarbonylamino)-3-[2,2-dimethyl-1(R)-cyclopropyl]-2-hydroxypro...
参考文献标题:Syntheses and biological activity of advanced second-generation taxoids
文献作者:Lin,S.; et al.
参考来源:216th ACS Natl Meet (Aug.23-27,Boston) 1998,Abst MEDI 315

SNAP-6145-(+), (+)-SNAP-6145

Chemical Name: (+)-1-[3-[4-(3,4-Difluorophenyl)-2,5-dioxo-1,2,3,4,5,7-hexahydrofuro[3,4-d]pyrimidin-3-ylcarboxamido]propyl]-4-phenylpiperidine-4-carboxylic acid methyl ester
项目整合开发状态: Preclinical 参考文献标题:Synthesis and evaluation of furo[3,4-d]pyrimidinones as selective alpha1a-adrenergic receptor antagonists
文献作者:Lagu,B.; Tian,D.; Chiu,G.; Nagarathnam,D.; Fang,J.; Shen,Q.; Forray,C.; Ransom,R.W.; Chang,R.S.; Vyas,K.P.; Zhang,K.; Gluchowski,C.
参考来源:Bioorg Med Chem Lett 2000,10(2),175

新产品编号:1147459

Chemical Name: (cis)-1,1-Dichloro-2-(4-methoxyphenyl)-3-phenylcyclopropane
项目整合开发状态: Biological Testing
项目研究机构: National Cancer Institute (Originator), University of Pittsburgh (Originator)
合...
参考文献标题:Synthesis and biological evaluation of a series of gem-dichlorocyclopropanes as antitumor agents
文献作者:Griffin,M.T.; et al.
参考来源:Anti-Cancer Drug Des 1992,7(1),49

新产品编号:1149041

Chemical Name: 11-Dichloro-2-(4-fluorophenyl)-3-(4-methoxyphenyl)cyclopropane
项目整合开发状态: Biological Testing
项目研究机构: National Cancer Institute (Originator), University of Pittsburgh (Originator) 参考文献标题:Synthesis and biological evaluation of a series of gem-dichlorocyclopropanes as antitumor agents
文献作者:Griffin,M.T.; et al.
参考来源:Anti-Cancer Drug Des 1992,7(1),49

新产品编号:1150623

Chemical Name: 1beta-(2,6,7-Trichloro-1H-naphtho[2,3-d]imidazol-1-yl)-D-ribofuranose
项目整合开发状态: Biological Testing
项目研究机构: University of Michigan (Originator)
合成路线:The hydrolysis of 6,7-dichlo...
参考文献标题:Synthesis of 2,6,7-trichloro-1-(beta-D-ribofuranosyl)naphtho[2,3-d]imidazole: A linear dimensional analogue of the antiviral agent TCRB
文献作者:Zhu,Z.J.; et al.
参考来源:J Org Chem 1998,63(4),977

新产品编号:1152205

Chemical Name: (+)-3,10-Dibromo-8-chloro-11-[1-[2-(1-oxidopyridin-4-yl)acetyl]piperidin-4-ylidene]-5,6-dihydro-11H-benzo[5,6]cyclohepta[1,2-b]pyridine
项目整合开发状态: Preclinical
项目研究机构: Schering-Plou...
参考文献标题:(+)-4-[2-[4-(8-Chloro-3,10-dibromo-6,11-dihydro-5H-benzo[5,6]cyclohepta[1,2-b]pyridin-11(R)-yl)-1-piperidinyl]-2-oxo-ethyl]-1-piperidinecarboxamide (SCH-66336): A very potent farnesyl protein transferase inhibitor as a novel antitumor agent
文献作者:Njoroge,F.G.; Taveras,A.G.; Kelly,J.; Remiszewski,S.; Mallams,A.K.; Wolin,R.; Afonso,A.; Cooper,A.B.; Rane,D.F.; Liu,Y.-T.; Wong,J.; Vibulbhan,B.; Pinto,P.; Deskus,J.; Alvarez,C.S.; del Rosario,J.; Connolly,M.; Wang,J.; Desai,J.; et al.
参考来源:J Med Chem 1998,41(24),4890

新产品编号:1153787

Chemical Name: (+)-4-[2-[4-(3,10-Dibromo-8-chloro-5,6-dihydro-11H-benzo[5,6]cyclohepta[1,2-b]pyridin-11-ylidene)piperidin-1-yl]-2-oxoethyl]piperidin-1-carboxamide
项目整合开发状态: Preclinical
项目研究机构: S...
参考文献标题:(+)-4-[2-[4-(8-Chloro-3,10-dibromo-6,11-dihydro-5H-benzo[5,6]cyclohepta[1,2-b]pyridin-11(R)-yl)-1-piperidinyl]-2-oxo-ethyl]-1-piperidinecarboxamide (SCH-66336): A very potent farnesyl protein transferase inhibitor as a novel antitumor agent
文献作者:Njoroge,F.G.; Taveras,A.G.; Kelly,J.; Remiszewski,S.; Mallams,A.K.; Wolin,R.; Afonso,A.; Cooper,A.B.; Rane,D.F.; Liu,Y.-T.; Wong,J.; Vibulbhan,B.; Pinto,P.; Deskus,J.; Alvarez,C.S.; del Rosario,J.; Connolly,M.; Wang,J.; Desai,J.; et al.
参考来源:J Med Chem 1998,41(24),4890

PD-166309

Chemical Name: 3-[5-[4-(1,3-Benzodioxol-5-yl)-2-hydroxy-2-(4-methoxyphenyl)-5-oxo-2,5-dihydrofuran-3-ylmethyl]-2,3-dimethoxyphenoxy]propane-1-sulfonic acid sodium salt
项目整合开发状态: Preclinical
项目研究...
参考文献标题:Butenolide endothelin antagonists with improved aqueous solubility
文献作者:Patt,W.C.; Cheng,X.-M.; Repine,J.T.; Lee,C.; Reisdorph,B.R.; Massa,M.A.; Doherty,A.M.; Welch,K.M.; Bryant,J.W.; Flynn,M.A.; Walker,D.M.; Schroeder,R.L.; Haleen,S.J.; Keiser,J.A.
参考来源:J Med Chem 1999,42(12),2162

PNU-109230

Chemical Name: N-[3-[3-Fluoro-4-[4-(2-hydroxy-1-oxoethyl)piperazin-1-yl]phenyl]-2-oxooxazolidin-5(S)-ylmethyl]-2,2-dichloroacetamide
项目整合开发状态: Preclinical
项目研究机构: Pfizer (Originator)
合成路线:Hyd...
参考文献标题:Synthesis and biological activity of N-acetyl modified analogs of oxazolidinone anticancer agents linezolid and eperezolid
文献作者:Ulanowicz,D.A.; et al.
参考来源:37th Intersci Conf Antimicrob Agents Chemother (Sept 28-Oct 1,Toronto) 1997,Abst F-21