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:1046211

Chemical Name: 6-Chloro-5-(methylsulfanyl)-N-(3-pyridyl)indoline-1-carboxamide
项目整合开发状态: Biological Testing
项目研究机构: GlaxoSmithKline (Originator)
合成路线:The heating of nicotinoyl azide (I) in re...
参考文献标题:Indoline derivs.as 5HT2C antagonists
文献作者:Ham,P.; Jones,G.E.; Forbes,I.T.(SmithKline Beecham plc)
参考来源:EP 0707581; JP 1996512299; US 5834494; WO 9501976

新产品编号:1047793

Chemical Name: (3R,4S,5R,6R,8R,9R,10E,12E,15R)-5-[4-O-(4-O-Butyryl-2,6-dideoxy-3-O,3-C-dimethyl-alpha-L-altropyranosyl)-3,6-dideoxy-3-(dimethylamino)-beta-D-glucopyranosyloxy]-3,9-dihydroxy-6-(formylm...
参考文献标题:Cladinose analogues of sixteen-membered macrolide antibiotics.VI.Synthesis of metabolically programmed,highly potent analogues of sixteen-membered macrolide antibiotics
文献作者:Kurihara,K.; Ajito,K.; Shibahara,S.; Hara,O.; Araake,M.; Omoto,S.; Inouye,S.
参考来源:J Antibiot 1998,51(8),771

新产品编号:1049375

Chemical Name: 2-[6-(4-Amidino-2-fluorobenzamido)-1-oxo-1,2,3,4-tetrahydronaphthalen-2-yl]acetic acid trifluoroacetate
项目整合开发状态: Preclinical
项目研究机构: Lilly (Originator)
合成路线:The known amino te...
参考文献标题:Fused bicyclic Gly-Asp beta-turn mimics with potent affinity for GPIIb-IIIa.Exploration of the arginine isostere
文献作者:Fisher,M.J.; Giese,U.; Harms,C.S.; Kinnick,M.D.; Lindstrom,T.D.; McCowan,J.R.; Mest,H.J.; Morin,J,M.Jr.; Mullaney,J.T.; Paal,M.; Rapp,A.; Ruhter,G.; Ruterbories,K.J.; Sall,D.J.; Scarborough,R.M.; Schotten,T.; Stenzel,W.; et al.
参考来源:Bioorg Med Chem Lett 2000,10(4),385

SR-10208

Chemical Name: N-([1]Benzothieno[3,2-h]isoquinolin-6-yl)-2,2,2-trifluoroacetamide
项目整合开发状态: Preclinical
项目研究机构: SRI (Originator)
合成路线:3-(Chloromethyl)benzothiophene (II) was prepared by conde...
参考文献标题:Novel benzothiophene analogs as antiviral agents
文献作者:Reist,E.J.(SRI International)
参考来源:EP 0712404; JP 1997500386; US 5424315; WO 9504059

S-18204(racemate), S-18886

Chemical Name: 3-[6-(4-Chlorophenylsulfonamido)-2-methyl-5,6,7,8-tetrahydronaphth-1-yl]propionic acid sodium salt
项目整合开发状态: Phase III
项目研究机构: Servier (Originator)
合成路线:Reductive amination of ...
参考文献标题:1,2,3,4-Tetrahydronaphthalene,chroman and thiochroman derivs.as antithrombotic agents
文献作者:Lavielle,G.; Dubuffet,T.; Muller,O.; Laubie,M.; Verbeuren,T.; Simonet,S.; Descombes,J.-J.(ADIR et Cie.)
参考来源:CA 2118102; EP 0648741; FR 2711139; JP 1995188155

新产品编号:1050957

Chemical Name: 6-O-Demethyl-6-O-(N-methylcarbamoyl)galanthamine; (4aS,6R,8aS)-6-Hydroxy-11-methyl-3-(N-methylcarbamoyloxy)-5,6,9,10,11,12-hexahydro-4aH-benzofuro[3a,3,2-ef][2]benzazepine
项目整合开发状态: ...
参考文献标题:Galanthamine derivatives for the treatment of Alzeimer's disease
文献作者:Bores,G.M.; Kosley,R.W.Jr.
参考来源:Drugs Fut 1996,21(6),621

TBC-10950, IPI-950

Chemical Name: N-(4-Bromo-3-methylisoxazol-5-yl)-4'-methylbiphenyl-4-sulfonamide
项目整合开发状态: Biological Testing
项目研究机构: Encysive Pharmaceuticals (Originator), Wellstat Therapeutics (Originator) 参考文献标题:The discovery and structure-activity relationships of nonpeptide,low molecular weight antagonists selective for the endothelin ETB receptor
文献作者:Chan,M.F.; Kois,A.; Verner,E.J.; Raju,B.G.; Castillo,R.S.; Wu,C.; Okun,I.; Stavros,F.D.; Balaji,V.N.
参考来源:Bioorg Med Chem 1998,6(12),2301

TBC-10894, IPI-894

Chemical Name: N-(4-Bromo-3-methylisoxazol-5-yl)-5-(4-methylphenyl)thiophene-2-sulfonamide
项目整合开发状态: Biological Testing
项目研究机构: Encysive Pharmaceuticals (Originator)
合成路线:4-Bromobenzenesulfon...
参考文献标题:The discovery and structure-activity relationships of nonpeptide,low molecular weight antagonists selective for the endothelin ETB receptor
文献作者:Chan,M.F.; Kois,A.; Verner,E.J.; Raju,B.G.; Castillo,R.S.; Wu,C.; Okun,I.; Stavros,F.D.; Balaji,V.N.
参考来源:Bioorg Med Chem 1998,6(12),2301

Korupensamine A

Chemical Name: (S-biar)-6,8-Dihydroxy-5-(4-hydroxy-5-methoxy-7-methyl-1-naphthyl)-1(R),3(R)-dimethyl-1,2,3,4-tetrahydroisoquinoline
项目整合开发状态: Biological Testing
项目研究机构: US Department of Health &...
参考文献标题:Total synthesis of michellamines A-C,korupensamines A-D,and ancistrobrevine B
文献作者:Hoye,T.R.; et al.
参考来源:J Org Chem 1999,64(19),7184

新产品编号:1052539

Chemical Name: 6-O-Demethyl-3-O-(isobutyryl)-6-O-(N-methylcarbamoyl)galanthamine; (4aS,6R,8aS)-6-(Isobutyryloxy)-11-methyl-3-(N-methylcarbamoyloxy)-5,6,9,10,11,12-hexahydro-4aH-benzofuro[3a,3,2-ef][2]...
参考文献标题:Galanthamine derivatives for the treatment of Alzeimer's disease
文献作者:Bores,G.M.; Kosley,R.W.Jr.
参考来源:Drugs Fut 1996,21(6),621