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。
如有产品相关项目调研推广服务, 请致函联系我们

客户展示

新项目整合精选

新产品编号:2394075

Chemical Name: N-(3,5-Dimethylisothiazol-4-ylmethyl)-3-[2(S)-hydroxy-4(R)-[N-[3(S)-hydroxy-3,4-dihydro-2H-1-benzopyran-4(S)-yl]carbamoyl]-5-phenylpentanoyl]-5,5-dimethylthiazolidine-4(R)-carboxamide 参考文献标题:Synthesis of highly potent HIV protease inhibitors with activity against protease resistant virus
文献作者:Bohn,J.; Lu,Z.; Raghavan,S.; Charest,M.; Stahlhut,M.; Rutkowski,C.A.; Himmelberger,A.L.; Olsen,D.B.; Scheleif,W.A.; Carella,A.; Gabryelski,L.; Jin,L.; Lin,J.H.; Tata,J.R.; Chapman,K.
参考来源:224th ACS Natl Meet (Aug 18 2002,Boston) 2002,Abst MEDI 205

新产品编号:2395657

Chemical Name: 3,5-Dichloro-N-[1(S)-[2-(2-chloropyridin-3-ylamino)-3,4-dioxo-1-cyclobuten-1-ylamino]-2,2-dimethylpropyl]benzamide
项目整合开发状态: Preclinical
项目研究机构: Abbott (Originator)
合成路线:Conden...
参考文献标题:Aminal diones as potassium channel openers
文献作者:Basha,F.Z.; Carroll,W.A.; Kort,M.E.; Gregg,R.J.; Dinges,J.; Perez Medrano,A.(Abbott Laboratories Inc.)
参考来源:US 2002165264; US 6495576; WO 0262761

新产品编号:2397239

Chemical Name: 4-[4-[3-[4(R)-Methyl-2,5-dioxo-3-phenylimidazolidin-1-yl]propoxy]phenylsulfonyl]tetrahydro-2H-pyran-4-carbohydroxamic acid
项目整合开发状态: Biological Testing
项目研究机构: Pfizer (Originator)...
参考文献标题:Design and synthesis of potent and selective 4,4-disubstituted alpha-sulphones hydroxamates as MMP inhibitors
文献作者:Becker,D.P.; Villamil,C.; Barta,T.E.; et al.
参考来源:224th ACS Natl Meet (Aug 18 2002,Boston) 2002,Abst MEDI 309

新产品编号:2398821

Chemical Name: 4-Fluoro-N-[1-[3-[6-[1-methyl-1-(methylsulfonyl)ethyl]quinolin-8-yl]phenyl]ethyl]-N-[4-(methylsulfonyl)phenyl]benzamide
项目整合开发状态: Preclinical
项目研究机构: Merck Frosst (Originator)
...
参考文献标题:Heteroatom-bridged substituted 8-arylquinolines as potent PDE IV inhibitors
文献作者:Lacombe,P.; Dub? D.; Deschenes,D.; et al.
参考来源:224th ACS Natl Meet (Aug 18 2002,Boston) 2002,Abst MEDI 328

新产品编号:2400403

Chemical Name: 6-[1-[6-Cyano-2'-(trifluoromethyl)biphenyl-3-yl]-1-(1-methyl-1H-imidazol-5-yl)methoxymethyl]-2-(3-hydroxypiperidin-1-yl)pyridine-3-carbonitrile
项目整合开发状态: Biological Testing
项目研究机构...
参考文献标题:Lead optimization of imidazole-containing inhibitors of farnesyl transferase
文献作者:Wang,G.T.; et al.
参考来源:224th ACS Natl Meet (Aug 18 2002,Boston) 2002,Abst MEDI 130

新产品编号:2401985

Chemical Name: 3-[4-[3-(trifluoromethyl)phenyl]-1H-imidazol-2-yl]pyridine
项目整合开发状态: Preclinical
项目研究机构: Schering-Plough (Originator)
合成路线:3-Cyanopyridine (I) is converted into amidine (II),wh...
参考文献标题:2,4-Diarylimidazoles as neuropeptide Y Y5 receptor antagonists
文献作者:Boyle,C.D.; et al.
参考来源:ACS Natl.Meet.2002,Abst MEDI 335

GW-500580X

Chemical Name: 5-[(E)-(2,4-Dioxothiazolidin-5-ylidenemethyl)-N-[1(S)-phenylethyl]-2-propoxybenzamide
项目整合开发状态: Preclinical
项目研究机构: GlaxoSmithKline (Originator)
合成路线:5-Formylsalicylic acid (I)...
参考文献标题:Aryl 1,3-thiazolidine-2,4-diones acting as KATP channel agonists as a class of potent antidiabetic agents
文献作者:Allen,S.H.; Pfohl,J.L.; Wallace,E.; Truax,J.F.; Worley,J.K.; Townsend,C.; Peat,A.J.; Garrido,D.M.; McKay,C.
参考来源:224th ACS Natl Meet (Aug 18 2002,Boston) 2002,Abst MEDI 364

新产品编号:2403567

Chemical Name: 5-(3-Chlorophenyl)-6-[1-(4-cyanophenyl)-1-(1-methyl-1H-imidazol-5-yl)methoxymethyl]-2-oxo-1,2-dihydropyridine-3-carbonitrile
项目整合开发状态: Preclinical
项目研究机构: Abbott (Originator)
合...
参考文献标题:Design and synthesis of pyridone farnesyltransferase inhibitors
文献作者:Hasvold,L.A.; et al.
参考来源:224th ACS Natl Meet (Aug 18 2002,Boston) 2002,Abst MEDI 126

ST-1863

Chemical Name: 2-[3-[2-(4-Chlorophenyl)ethoxy]benzyl]malonic acid dimethyl diester
项目整合开发状态: Preclinical
项目研究机构: Sigma-Tau (Originator)
合成路线:Knoevenagel condensation of 4-hydroxybenzaldehyde ...
参考文献标题:New phenylalkylcarboxylate derivatives as hypoglycemic and hypolipidemic agents
文献作者:Catini,R.; Brunetti,T.; Arduini,A.; et al.
参考来源:Drugs Fut 2002,27(Suppl.A),

3,4,3-LI(1,2-Me-3,2-HOPO)

Chemical Name: N,N'-(1,4-Butylene)bis[N-(1-hydroxy-6-oxo-1,6-dihydropyridin-2-ylcarbonyl)imino]bis(1,3-propylene)bis(3-hydroxy-1-methyl-2-oxo-1,2-dihydropyridine-4-carboxamide)
项目整合开发状态: Preclinica...
参考文献标题:Synthesis and initial evaluation for in vivo chelation of Pu(IV) of a mixed octadentate spermine-based ligand containing 4-carbamoyl-3-hydroxy-1-methyl-2(1H)-pyridinone and 6-carbamoyl-1-hydroxy-2(1H)-pyridinone
文献作者:Xu,J.; Durbin,P.W.; Kullgren,B.; Ebbe,S.N.; Uhlir,L.C.; Raymond,K.N.
参考来源:J Med Chem 2002,45(18),3963