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

ODE-CDV

Chemical Name: 2-(4-Amino-2-oxo-1,2-dihydropyrimidin-1-yl)-1(S)-(hydroxymethyl)ethoxymethylphosphonic acid 2-(octadecyloxy)ethyl monoester
项目整合开发状态: Preclinical
项目研究机构: University of Alabama at...
参考文献标题:Phosphonate cpds.
文献作者:Hostetler,K.Y.; Kini,G.D.; Beadle,J.R.(University of California,San Diego)
参考来源:EP 1233770; WO 0139724

NSC-711616

Chemical Name: (E)-3-(2-Chloro-5-methoxy-6-methyl-1H-indol-3-ylmethylidene)-2,3-dihydro-1H-indol-2-one
项目整合开发状态: Preclinical
项目研究机构: Lithuanian Institute of Cardiology (Originator), Universit?de...
参考文献标题:Synthesis and antitumor activity of 1,5,6-substituted E-3-(2-chloro-3-indolylmethylene)-1,3-dihydroindol-2-ones
文献作者:Andreani,A.; Granaiola,M.; Leoni,A.; Locatelli,A.; Morigi,R.; Rambaldi,M.; Garaliene,V.
参考来源:J Med Chem 2002,45(12),2666

新产品编号:2346615

Chemical Name: 1-(4-Fluorophenyl)-1-[1-[2-(4-fluorophenyl)ethyl]piperidin-4-yl]methanol
项目整合开发状态: Biological Testing
项目研究机构: Harvard Medical School (Originator), Massachusetts General Hospital (...
参考文献标题:Synthesis,receptor potency,and selectivity of halogenated diphenylpiperidines as serotonin 5-HT2A ligands for PET or SPECT brain imaging
文献作者:Fu,X.; Tan,P.-Z.; Kula,N.S.; Baldessarini,R.; Tamagnan,G.; Innis,R.B.; Baldwin,R.M.
参考来源:J Med Chem 2002,45(11),2319

RPR-238677

Chemical Name: trans-N-(Cyclopropylmethyl)-4-[4-(4-fluorophenyl)-2-[5-methyl-5-(4-methylpiperazin-1-ylcarbonyl)-1,3-dioxan-2-yl]-1H-imidazol-5-yl]pyrimidin-2-amine
项目整合开发状态: Preclinical
项目研究机构: ...
参考文献标题:An algorithm-directed two-component library synthesized via solid-phase methodology yielding potent and orally bioavailable p38 MAP kinase inhibitors
文献作者:McKenna,J.M.; Halley,F.; Souness,J.E.; McLay,I.M.; Pickett,S.D.; Collis,A.J.; Page,K.; Ahmed,I.
参考来源:J Med Chem 2002,45(11),2173

新产品编号:2348197

Chemical Name: 4-(10,11-Dihydro-5H-dibenzo[a,d]cyclohepten-5-yl)-1-[4-[2-[N-[2-[N-[3-(dimethylamino)propyl]-N-methylamino]ethyl]carbamoyl]-1H-pyrrol-1-ylsulfonyl]-2-nitrophenyl]semicarbazide
项目整合开发...
参考文献标题:Nonpeptide bradykinin B2 receptor antagonists: Conversion of rodent-selective bradyzide analogues into potent,orally-active human bradykinin B2 receptor antagonists
文献作者:Dziadulewicz,E.K.; Ritchie,T.J.; Hallett,A.; Snell,C.R.; Davies,J.W.; Wrigglesworth,R.; Dunstan,A.R.; Bloomfield,G.C.; Drake,G.S.; McIntyre,P.; Brown,M.C.; Burgess,G.M.; Lee,W.; Davis,C.; Yaqoob,M.; Phagoo,S.B.; Phillips,E.; et al.
参考来源:J Med Chem 2002,45(11),2160

[18F]-N-Me-FAMP

Chemical Name: 3-([18F]Fluoro)-2-methyl-2-(methylamino)propionic acid
项目整合开发状态: Preclinical
项目研究机构: Emory University (Originator)
合成路线:The nonradioactive aminoacid is prepared as follows.The ...
参考文献标题:Radiolabeled amino acids for tumor imaging with PET: Radiosynthesis and biological evaluation of 2-amino-3[18F]fluoro-2-methylpropanoic acid and 3-[18F]fluoro-2-methyl-2-(methylamino)propanoic acid
文献作者:McConathy,J.; Martarello,L.; Malveaux,E.J.; Camp,V.M.; Simpson,N.E.; Simpson,C.P.; Bowers,G.D.; Olson,J.J.; Goodman,M.M.
参考来源:J Med Chem 2002,45(11),2240

新产品编号:2349779

Chemical Name: N'-(2-Chlorophenyl)-N-(3-ethynylphenyl)-2-oxopropanehydrazonamide
项目整合开发状态: Biological Testing
项目研究机构: Bristol-Myers Squibb (Originator)
合成路线:2-Chloroaniline (I) is diazotized ...
参考文献标题:Arylamidrazones as novel corticotropin releasing factor receptor antagonists
文献作者:Wilson,D.M.; Termin,A.P.; Mao,L.; Ramirez-Weinhouse,M.M.; Molteni,V.; Gootenhuis,P.D.J.; Miller,K.; Keim,S.; Wise,G.
参考来源:J Med Chem 2002,45(11),2123

新产品编号:2351361

Chemical Name: 5-Bromo-2-[N-[4-(2-butynyloxy)phenylsulfonyl]-N-methylamino]-3-(4-methylpiperazin-1-ylmethyl)benzohydroxamic acid
项目整合开发状态: Preclinical
项目研究机构: Amgen (Originator), Wyeth Pharmaceu...
参考文献标题:Anthranilate sulfonamide hydroxamate TACE inhibitors.Part 2: SAR of the acetylenic P1' group
文献作者:Levin,J.I.; Chen,J.M.; Du,M.T.; Nelson,F.C.; Killar,L.M.; Skala,S.; Sung,A.; Jin,G.; Cowling,R.; Barone,D.; March,C.J.; Mohler,K.M.; Black,R.A.; Skotnicki,J.S.
参考来源:Bioorg Med Chem Lett 2002,12(8),1199

99mTc-EC-AMDP

Chemical Name: [1-[N-[2-[1(R)-Carboxy-2-sulfanylethylamino]ethyl]-L-cysteinylamino]methyl-1,1-diphosphonic acid]oxo[99mTc]technetium(V) complex; [[(5R,10R)-1,1-Dihydroxy-5,10-bis(mercaptomethyl)-1-oxi...
参考文献标题:Development of a conjugate of 99mTc-EC with aminomethylenediphosphonate in the search for a bone tracer with fast clearance from soft tissue
文献作者:Verbeke,K.; et al.
参考来源:Bioconjugate Chem 2002,13(1),16

FA-FdUMP[10]

Chemical Name: 2'-Deoxy-5-fluorocytidylyl-(3'-5')-2'-deoxy-5-fluorocytidylyl-(3'-5')-2'-deoxy-5-fluorocytidylyl-(3'-5')-2'-deoxy-5-fluorocytidylyl-(3'-5')-2'-deoxy-5-fluorocytidylyl-(3'-5')-2'-deoxy-5...