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

WP-769

Chemical Name: 7-O-(4-O-Benzyl-2,6-dideoxy-alpha-L-galactopyranosyl)-4-demethoxyadriamycinone hydrochloride
项目整合开发状态: Preclinical
项目研究机构: M.D. Anderson Cancer Center (Originator)
合成路线:Hydroly...
参考文献标题:Methods and compsns.for the manufacture of C-3' and C-4' anthracycline antibiotics
文献作者:Fokt,I.; Skibicki,P.; Priebe,W.; Perez-Soler,R.; Grynkiewicz,G.; Krawczyk,M.; Przewloka,T.
参考来源:WO 0056267

新产品编号:1838793

Chemical Name: N-[4-[2-[2(R)-Hydroxy-2-(3-pyridyl)ethylamino]ethyl]phenyl]-4-[4-[4-(trifluoromethyl)benzyl]-2H-1,2,3-triazol-2-yl]benzenesulfonamide
项目整合开发状态: Preclinical
项目研究机构: Merck & Co. (Or...
参考文献标题:Human beta3 adrenergic receptor agonists containing 1,2,3-triazole-substituted benzenesulfonamides
文献作者:Brockunier,L.L.; Parme,E.R.; Ok,H.O.; et al.
参考来源:219th ACS Natl Meet (March 26 2000,San Francisco) 2000,Abst MEDI 252

新产品编号:1840375

Chemical Name: N-(1,3-Benzodioxol-5-ylmethyl)-3(S)-[N2-(benzylsulfonyl)-L-arginyl-N2-methylglycinamido]-4-(cyclohexyl)-2-oxobutyramide
项目整合开发状态: Biological Testing
项目研究机构: Corvas (Originator) 参考文献标题:Novel,potent,and selective factor Xa inhibitors featuring a hydrophobic P1-ketoamide moiety
文献作者:Semple,J.E.; et al.
参考来源:219th ACS Natl Meet (March 26 2000,San Francisco) 2000,Abst MEDI 193

SMA-41

Chemical Name: N-(3-Methylphenyl)-6-(3-methyltriazen-1-yl)quinazolin-4-amine
项目整合开发状态: Preclinical
项目研究机构: McGill University (Originator)
合成路线:Coupling of chloroquinazoline (I) with 3-bromoan...
参考文献标题:Tyrosine kinase inhibitors.5.Synthesis and structure-activity relationships for 4-[(phenylmethyl)amino]- and 4-(phenylamino)quinazolines as potent adenosine 5'-triphosphate binding site inhibitors of the tyrosine kinase domain of the epidermal growth f
文献作者:Rewcastle,G.W.; Denny,W.A.; Bridges,A.J.; Zhou,H.; Cody,D.R.; McMichael,A.; Fry,D.W.
参考来源:J Med Chem 1995,38(18),3482

新产品编号:1841957

Chemical Name: N-(2,6-Diisopropylphenyl)-N'-[1-methyl-2-[3-(trifluoromethyl)phenyl]ethyl]urea
项目整合开发状态: Preclinical
项目研究机构: Elan (Originator), Pfizer (Originator)
合成路线:The title urea derivati...
参考文献标题:Synthesis and biological evaluation of substituted alpha-methyl-3-(trifluoromethyl)benzeneethanamine derivatives as novel N-type calcium channel blockers
文献作者:Warmus,J.; Weber,M.l.; Stoehr,S.; Downing,D.; Kornberg,B.E.; Rock,D.M.; Rafferty,M.F.; Szoke,B.G.; Nikam,S.S.
参考来源:219th ACS Natl Meet (March 26 2000,San Francisco) 2000,Abst MEDI 260

新产品编号:1843539

Chemical Name: N-(4,5-Dihydrothiazol-2-yl)-N-(2-phenyl-3,4-dihydro-2H-1-benzothiopyran-4-yl)amine
项目整合开发状态: Biological Testing
项目研究机构: AstraZeneca (Originator)
合成路线:2-Phenyl-3,4-dihydro-2H-1-...
参考文献标题:Selective alpha2C-adrenoceptor agonist activity of imidazole,imidazoline,and imidazoline-related derivatives
文献作者:Lewis,J.J.; Bare,T.M.; Horchler,C.L.; et al.
参考来源:219th ACS Natl Meet (March 26 2000,San Francisco) 2000,Abst MEDI 268

Pyroxamide, NSC-696085

Chemical Name: N'-Hydroxy-N-(3-pyridyl)octane-1,8-diamide
项目整合开发状态: Phase I
项目研究机构: National Cancer Institute (Originator)
合成路线:Monomethyl suberate (I) is treated with isobutyl chloroformate ...
参考文献标题:A phase I dose escalation and bioavailability study of oral sodium phenylbutyrate in patients with refractory solid tumor malignancies
文献作者:Gilbert,J.; Baker,S.D.; Bowling,M.K.; Grochow,L.; Figg,W.D.; Zabelina,Y.; Donehower,R.C.; Carducci,M.A.
参考来源:Clin Cancer Res 2001,7(8),2292

E-7820, ER-68203-00

Chemical Name: 3-Cyano-N-(3-cyano-4-methyl-1H-indol-7-yl)benzenesulfonamide
项目整合开发状态: IND Filed
项目研究机构: Eisai (Originator)
合成路线:The synthesis of intermediate (VIII) can be achieved by followi...
参考文献标题:Sulfonamide-containing indole cpds.
文献作者:Kamata,J.; Semba,T.; Nara,K.; Ohwa,T.; Hata,N.; Haneda,T.; Funahashi,Y.; Hamaoka,S.; Tsuruoka,A.; Ueda,N.; Wakabayashi,T.; Ozawa,Y.; Yamamoto,Y.; Okabe,T.; Takahashi,K.; Tsukahara,N.(Eisai Co.,Ltd.)
参考来源:EP 1074542; JP 2000247949; WO 0050395

CGP-79807

Chemical Name: trans-3-[9-Ethyl-2-(4-hydroxycyclohexylamino)-9H-purin-6-ylamino]benzonitrile
项目整合开发状态: Preclinical
项目研究机构: Novartis (Originator)
合成路线:Condensation between dichloropurine (I) a...
参考文献标题:Chemistry and biological characterization of CGP79807,a highly selective CDK1/2 inhibitor
文献作者:Br黦gen,J.; Caravatti,G.; Capraro,H.-G.; et al.
参考来源:221st ACS Natl Meet (April 1 2001,San Diego) 2001,Abst MEDI 150

新产品编号:1845121

Chemical Name: 2(S)-(3,5-Dimethylisoxazol-4-ylsulfonamido)-3-[3-(4-pyridinyl)-3-azaspiro[5.5]undec-9-ylcarboxamido]propionic acid
项目整合开发状态: Preclinical
项目研究机构: Millennium (Originator), Lilly (Co...
参考文献标题:Pyridyl-containing spirocyclic cpds.as inhibitors of fibrinogen-dependent platelet aggregation
文献作者:Smyth,M.; Pandey,A.; Mehrota,M.; Scarborough,R.M.(COR Therapeutics,Inc.)
参考来源:WO 0130780