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:1123729

Chemical Name: 2,8-Dihydroxy-5-[4-[2-(1-piperidinyl)ethoxy]phenyl]-5,6-dihydrobenzo[c]phenanthridine
项目整合开发状态: Preclinical
项目研究机构: Lilly (Originator)
合成路线:Imine (III) was prepared by condensa...
参考文献标题:Photochemical synthesis of N-arylbenzophenanthridine selective estrogen receptor modulators (SERMs)
文献作者:Grese,T.A.; Adrian,M.D.; Phillips,D.L.; Shetler,P.K.; Short,L.L.; Glasebrook,A.L.; Bryant,H.U.
参考来源:J Med Chem 2001,44(17),2857

Sch-59948

Chemical Name: 8-Chloro-11-[1-[2-(4-pyridyl)acetyl]piperidin-4-yl]-6,11-dihydro-5H-benzo[5,6]cyclohepta[1,2-b]pyridin-6-one oxime
项目整合开发状态: Biological Testing
项目研究机构: Schering-Plough (Originator...
参考文献标题:Benzocycloheptapyridine farnesyl protein transferase inhibitors: Effects of substitution at position 5 and 6 on enzyme inhibition
文献作者:del Rosario,J.D.; et al.
参考来源:213th ACS Natl Meet (April 13-17,San Francisco) 1997,Abst MEDI 198

新产品编号:1125311

Chemical Name: N-(6-Ethyl-7-nitro-2,3-dioxo-1,2,3,4-tetrahydroquinoxalin-5-ylmethyl)-N-methylglycine
项目整合开发状态: Biological Testing
项目研究机构: Pfizer (Originator)
合成路线:Hofmann degradation of tetra...
参考文献标题:Design and synthesis of novel quinoxaline-2,3-dione AMPA/GlyN receptor antagonists: Amino acid derivatives
文献作者:Nikam,S.S.; Cordon,J.J.; Ortwine,D.F.; Heimbach,T.H.; Blackburn,A.C.; Vartanian,M.G.; Nelson,C.B.; Schwarz,R.D.; Boxer,P.A.; Rafferty,M.F.
参考来源:J Med Chem 1999,42(12),2266

LY-335580

Chemical Name: 2-[5-[2-(2,4-Diamino-5,6,7,8-tetrahydropyrido[2,3-d]pyrimidin-6-yl)ethyl]thien-2-ylcarbonyl]-L-glutamic acid
项目整合开发状态: Biological Testing
项目研究机构: Lilly (Originator)
合成路线:Pyrido...
参考文献标题:The synthesis and biological activity of a series of 2,4-diaminopyrido[2,3-d]pyrimidine based antifolates as antineoplastic and antiarthritic agents
文献作者:Gossett,L.S.; Habeck,L.L.; Shackelford,K.A.; Mendelsohn,L.G.; Gates,S.B.; Worzalla,J.F.; Self,T.D.; Theobald,K.S.; Andis,S.L.; Schultz,R.M.; Shih,C.
参考来源:Bioorg Med Chem Lett 1999,9(1),75

LY-335738

Chemical Name: 2-[5-[2-(2,4-Diamino-5,6,7,8-tetrahydropyrido[2,3-d]pyrimidin-6-yl)ethyl]furan-2-ylcarbonyl]-L-glutamic acid
项目整合开发状态: Biological Testing
项目研究机构: Lilly (Originator)
合成路线:Pyrido...
参考文献标题:The synthesis and biological activity of a series of 2,4-diaminopyrido[2,3-d]pyrimidine based antifolates as antineoplastic and antiarthritic agents
文献作者:Gossett,L.S.; Habeck,L.L.; Shackelford,K.A.; Mendelsohn,L.G.; Gates,S.B.; Worzalla,J.F.; Self,T.D.; Theobald,K.S.; Andis,S.L.; Schultz,R.M.; Shih,C.
参考来源:Bioorg Med Chem Lett 1999,9(1),75

MEN-11149

Chemical Name: (1R,2S)-2-(1H-Indol-3-ylcarboxamido)-N-[1-[N-methyl-2-(4-methylphenyl)acetamido]-2-(2-naphthyl)ethyl]cyclohexanecarboxamide
项目整合开发状态: Preclinical
项目研究机构: Malesci (Originator), Men...
参考文献标题:Tachykinin antagonists
文献作者:Sisto,A.; Fincham,C.; Potier,E.; Manzini,S.; Arcamone,F.; Lombardi,P.(Malesci Ist.Farmacobiol.SpA; Menarini Industrie Farma Riunite srl)
参考来源:EP 0731790; JP 1997506348; US 5760248; WO 9515311

新产品编号:1126893

Chemical Name: 3-[3-Carboxy-2-methyl-1-[(E)-5,5,8,8-tetramethyl-5,6,7,8-tetrahydroanthracen-2-ylmethylene]-2(Z)-propenyl]benzoic acid; 4-(3-Carboxyphenyl)-3-methyl-5-(5,5,8,8-tetramethyl-5,6,7,8-tetra...
参考文献标题:Alicyclic phospholipase A2 inhibitors
文献作者:Bronson,J.J.; Carroll,F.I.; Greene,K.M.; Lewin,A.; Mansuri,M.M.; D'Andrea,S.V.(Bristol-Myers Squibb Co.)
参考来源:CA 2125802; EP 0629604; JP 1995017913; US 5436369

新产品编号:1128475

Chemical Name: 3-(3,4-Difluorophenoxy)-5,5-dimethyl-4-[4-(methylsulfonyl)phenyl]furan-2(5H)-one
项目整合开发状态: Preclinical
项目研究机构: Merck Frosst (Originator)
合成路线:The Friedel Crafts condensation of...
参考文献标题:(Methylsulfonyl)phenyl-2-(5H)-furanones as COX-2 inhibitors
文献作者:Belley,M.; Gauthier,J.Y.; Grimm,E.; Leblanc,Y.; Li,C.-S.; Therien,M.; Lau,C.-K.; Prasit,P.; Roy,P.(Merck Frosst Canada Inc.)
参考来源:EP 0863891; JP 1999500146; US 5981576; WO 9714691

新产品编号:1130057

Chemical Name: 1-O-[4-[3(R)-[3(S)-Acetoxy-3-(4-fluorophenyl)propyl]-1-(4-fluorophenyl)-4-oxoazetidin-2(S)-yl]phenyl]-2,3,4-tri-O-acetyl-beta-D-glucopyranuronic acid methyl ester
项目整合开发状态: Biologica...
参考文献标题:Synthesis and structure activity relationships of anti-inflammatory 9,10-dihydro-9-oxo-2-acridine-alkanoic acids and 4-(2-carboxyphenyl)aminobenzenealkanoic acids
文献作者:Taraporewala,I.B.; Kauffman,J.M.
参考来源:J Pharm Sci 1990,79(2),173

PNU-167532

Chemical Name: 2-Benzyl-4-(3,4-difluorophenyl)-4-oxobutyric acid
项目整合开发状态: Biological Testing
项目研究机构: Pfizer (Originator)
合成路线:Conjugate addition of benzylmagnesium chloride (II) to unsaturat...
参考文献标题:4-Phenyl-4-oxo-butanoic acid derivatives inhibitors of kynurenine 3-hydroxylase
文献作者:Giordani,A.; Pevarello,P.; Cini,M.; Bormetti,R.; Greco,F.; Toma,S.; Speciale,C.; Varasi,M.
参考来源:Bioorg Med Chem Lett 1998,8(20),2907