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

CRL-8275

Chemical Name: 2,2,2-Trifluoro-N-[2-(6-methoxy-5,10-dioxo-5,10-dihydropyrido[3,2-g]quinolin-4-yl)phenyl]acetamide
项目整合开发状态: Preclinical
项目研究机构: Lafon (Originator)
合成路线:The cyclization of quin...
参考文献标题:Pharmaceutical compsn.based on polyaromatic cpds.
文献作者:Kiss,R.; Bontemps-Subielos,N.; Frydman,A.; Darro,F.; Bastide,J.; Deflourne,E.(Laboratoires L.Lafon)
参考来源:FR 2790954; WO 0055160

CRL-8277

Chemical Name: N-[2-(5,10-Dioxo-5,10-dihydropyrido[3,2-g]quinolin-4-yl)phenyl]-2,2,2-trifluoroacetamide
项目整合开发状态: Preclinical
项目研究机构: Lafon (Originator)
合成路线:The cyclization of quinoline-5,8-...
参考文献标题:Pharmaceutical compsn.based on polyaromatic cpds.
文献作者:Kiss,R.; Bontemps-Subielos,N.; Frydman,A.; Darro,F.; Bastide,J.; Deflourne,E.(Laboratoires L.Lafon)
参考来源:FR 2790954; WO 0055160

RHPS03, NSC-714186, RHPS3

Chemical Name: 3,6,8,11,13-Pentamethyl-8H-quino[4,3,2-kl]acridin-13-ium methylsulfate
项目整合开发状态: Biological Testing
项目研究机构: Institute of Cancer Research (Originator), University of Nottingham (Or...
参考文献标题:Antitumor polycyclic acridines.8.Synthesis and telomerase-inhibitory activity of methylated pentacyclic acridinium salts
文献作者:Heald,R.A.; Modi,C.; Cookson,J.C.; Hutchinson,I.; Laughton,C.A.; Gowan,S.M.; Kelland,L.R.; Stevens,M.F.G.
参考来源:J Med Chem 2002,45(3),590

DA-3003-1, NSC-663284

Chemical Name: 6-Chloro-7-[2-(4-morpholinyl)ethylamino]-5,8-dihydroquinoline-5,8-dione
项目整合开发状态: Biological Testing
项目研究机构: National Cancer Institute (Originator), University of Pittsburgh (Orig...
参考文献标题:Discovery and biological evaluation of a new family of potent inhibitors of the dual specificity protein phosphatase Cdc25
文献作者:Lazo,J.S.; Aslan,D.C.; Southwick,E.C.; Cooley,K.A.; Ducruet,A.P.; Joo,B.; Vogt,A.; Wipf,P.
参考来源:J Med Chem 2001,44(24),4042

DA-3003-2

Chemical Name: 7-Chloro-6-[2-(4-morpholinyl)ethylamino]-5,8-dihydroquinoline-5,8-dione
项目整合开发状态: Biological Testing
项目研究机构: National Cancer Institute (Originator), University of Pittsburgh (Orig...
参考文献标题:Discovery and biological evaluation of a new family of potent inhibitors of the dual specificity protein phosphatase Cdc25
文献作者:Lazo,J.S.; Aslan,D.C.; Southwick,E.C.; Cooley,K.A.; Ducruet,A.P.; Joo,B.; Vogt,A.; Wipf,P.
参考来源:J Med Chem 2001,44(24),4042

新产品编号:2009649

Chemical Name: N-[5-[2-[1-[4-(2,4-Dioxothiazolidin-5-ylmethyl)phenyl]piperidin-4-ylamino]-1(R)-hydroxyethyl]-2-hydroxyphenyl]methanesulfonamide
项目整合开发状态: Preclinical
项目研究机构: Wyeth Pharmaceutical...
参考文献标题:2,4-Thiazolidinediones as potent and selective human beta3 agonists
文献作者:Hu,B.; Ellingboe,J.; Gunawan,I.; Han,S.; Largis,E.; Li,Z.; Malamas,M.S.; Mulvey,R.; Oliphant,A.; Sum,F.W.; Tillett,J.; Wong,V.
参考来源:Bioorg Med Chem Lett 2001,11(6),757

新产品编号:2011231

Chemical Name: (6aR,aS)-3-Methyl-2-[6-methyl-5,6,6a,7-tetrahydro-4H-dibenzo[de,g]quinolin-11-yl]benzonitrile
项目整合开发状态: Biological Testing
项目研究机构: ACADIA (Originator), AstraZeneca (Originator) 参考文献标题:Atropisomeric derivatives of 2',6'-disubstituted (R)-11-phenylaporphine: Selective serotonin 5-HT7 receptor antagonist
文献作者:Linnanen,T.; Brisander,M.; Unelius,L.; Rosqvist,S.; Nordvall,G.; Hacksell,U.; Johansson,A.M.
参考来源:J Med Chem 2001,44(9),1337

WAY-174231

Chemical Name: N-[4-[4-[2(R)-Hydroxy-2-[4-hydroxy-3-(methylsulfonamido)phenyl]ethylamino]piperidin-1-yl]benzoyl]-L-leucine
项目整合开发状态: Preclinical
项目研究机构: Wyeth Pharmaceuticals (Originator)
合成路...
参考文献标题:(4-Piperidin-1-yl)phenyl amides: Potent and selective human beta3 agonists
文献作者:Hu,B.; Ellingboe,J.; Han,S.; Largis,E.; Mulvey,R.; Oliphant,A.; Sum,F.W.; Tillett,J.
参考来源:J Med Chem 2001,44(9),1456

新产品编号:2012813

Chemical Name: 2-Acetyl-N-benzyl-1-(2-thiazolyl)hydrazinecarboxamide
项目整合开发状态: Preclinical
项目研究机构: National Institutes of Health (Originator), University of Houston (Originator), University of N...
参考文献标题:Synthesis and structural studies of aza analogues of functionalized amino acids: New anticonvulsant agents
文献作者:Andurkar,S.V.; Beguin,C.; Stables,J.P.; Kohn,H.
参考来源:J Med Chem 2001,44(9),1475

TU-753

Chemical Name: 17-(2-Methyl-2-propenyl)-4,5alpha-epoxy-3,14-dihydroxy-6,7-didehydroindolo[2',3':6,7]morphinan; (4bS,8R,8aS,14bR)-7-(2-Methyl-2-propenyl)-6,7,8,9,14,14b-hexahydro-5H-4,8-methano[1]benzo...
参考文献标题:Effect of N-alkyl and N-alkenyl substituents in noroxymorphindole,17-substituted-6,7-dehydro-4,5alpha-epoxy-3,14-dihydroxy-6,7:2',3'-indolomorphinans on opioid receptor affinity,selectivity,and efficacy
文献作者:McLamore,S.; Ullrich,T.; Rothman,R.B.; Xu,H.; Dersch,C.; Coop,A.; Davis,P.; Porreca,F.; Jacobson,A.E.; Rice,K.C.
参考来源:J Med Chem 2001,44(9),1471