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

DuP-991

Chemical Name: 3-(2-Chlorophenyl)-2-(2,4-difluorophenyl)-1-(1H-1,2,4-triazol-1-yl)-3-buten-2-ol methanesulfonate
项目整合开发状态: Preclinical
项目研究机构: BTG (Technology Transfer), Bristol-Myers Squibb (Or...
参考文献标题:Antifungal carbinols
文献作者:Cuomo,J.; Greenberg,R.S.; Olson,R.E.(DuPont Pharmaceuticals Co.)
参考来源:EP 0251086; JP 1988060975

Febrifugine

Chemical Name: 3-[3-[3(S)-Hydroxypiperidin-2(R)-yl]-2-oxopropyl]-3,4-dihydroquinazolin-4-one
项目整合开发状态: Preclinical
项目研究机构: Okayama University (Originator), University of Tokyo (Originator)
合成...
参考文献标题:Febrifugine and isofebrifugine and processes for the preparation of both
文献作者:Kobayashi,S.; Kim,H.-S.; Wataya,Y.(Japan Science and Technology Corp.)
参考来源:EP 1076057; WO 0052005

Isofebrifugine

Chemical Name: 3-[(3aS,7aS)-2-Hydroxyperhydrofuro[3,2-b]pyridin-2-ylmethyl]-3,4-dihydroquinazolin-4-one
项目整合开发状态: Preclinical
项目研究机构: Okayama University (Originator), University of Tokyo (Origin...
参考文献标题:Febrifugine and isofebrifugine and processes for the preparation of both
文献作者:Kobayashi,S.; Kim,H.-S.; Wataya,Y.(Japan Science and Technology Corp.)
参考来源:EP 1076057; WO 0052005

AL-8810

Chemical Name: 7-[2(R)-[3(R)-(2,3-dihydro-1H-inden-2-yl)-3-hydroxy-1(E)-propenyl]-3(S)-fluoro-5(S)-hydroxy-1(R)-cyclopentyl]-5(Z)-heptenoic acid; 9(S),15(R)-Dihydroxy-11(S)-fluoro-15-(2-indanyl)-16,17...
参考文献标题:11-Halo prostaglandins for the treatment of glaucoma or ocular hypertension
文献作者:Sallee,V.L.; Hellberg,M.R.; Klimko,P.G.; Zinke,P.W.(Alcon Laboratories,Inc.)
参考来源:WO 9820880

新产品编号:1671101

Chemical Name: N-[2-[2-[Bis(4-fluorophenyl)methoxy]ethylamino]ethyl]-3-(4-bromophenyl)-2(E)-propenamide
项目整合开发状态: Preclinical
项目研究机构: Massachusetts General Hospital (Originator), Northeastern Un...
参考文献标题:Design,synthesis,and biological evaluation of novel non-piperazine analogues of 1-[2-(diphenylmethoxy]ethyl]- and 1-[2-[bis(4-fluorophenyl)methoxy]ethyl]4-(3-phenylpropyl)piperazines as dopamine transporter inhibitors
文献作者:Choi,S.W.; Elmaleh,D.R.; Hanson,R.N.; Fischman,A.J.
参考来源:J Med Chem 1999,42(18),3647

JK-1624SO2

Chemical Name: 23-(tert-Butylsulfonyl)-16,17-dehydro-1alpha-hydroxy-24,25,26,27-tetranorvitamin D3
项目整合开发状态: Preclinical
项目研究机构: Johns Hopkins University (Originator), M.D. Anderson Cancer Cente...
参考文献标题:Conceptually new sulfone analogues of the hormone 1alpha,25-dihydroxyvitamin D3: Synthesis and preliminary biological evaluation
文献作者:Posner,G.H.; Wang,Q.; Han,G.; Lee,J.K.; Crawford,K.; Zand,S.; Brem,H.; Peleg,S.; Dolan,P.; Kensler,T.W.
参考来源:J Med Chem 1999,42(18),3425

新产品编号:1672683

Chemical Name: N-(5-Aminosulfonyl-1,3,4-thiadiazol-2-yl)-2-(N1-methylguanidino)acetamide trifluoroacetate
项目整合开发状态: Preclinical
项目研究机构: Universit?degli Studi di Firenze (Originator)
合成路线:The ...
参考文献标题:Carbonic anhydrase inhibitors: Synthesis of water-soluble,aminoacyl/dipeptidyl sulfonamides possessing long-lasting intraocular pressure-lowering properties via the topical route
文献作者:Scozzafava,A.; Briganti,F.; Mincione,G.; Menabuoni,L.; Mincione,F.; Supuran,C.T.
参考来源:J Med Chem 1999,42(18),3690

新产品编号:1674265

Chemical Name: N-(5-Aminosulfonyl-1,3,4-thiadiazol-2-yl)-3-[2-(N1-methylguanidino)acetamido]propionamide trifluromethanesulfonate
项目整合开发状态: Preclinical
项目研究机构: Universit?degli Studi di Firenze (...
参考文献标题:Carbonic anhydrase inhibitors: Synthesis of water-soluble,aminoacyl/dipeptidyl sulfonamides possessing long-lasting intraocular pressure-lowering properties via the topical route
文献作者:Scozzafava,A.; Briganti,F.; Mincione,G.; Menabuoni,L.; Mincione,F.; Supuran,C.T.
参考来源:J Med Chem 1999,42(18),3690

GW-9578

Chemical Name: 2-[4-[2-[3-(2,4-Difluorophenyl)-1-heptylureido]ethyl]phenylsulfanyl]-2-methylpropionic acid
项目整合开发状态: Preclinical
项目研究机构: GlaxoSmithKline (Originator)
合成路线:4-Bromothiophenol (I...
参考文献标题:A ureido thiosobutyric acid (GW9578) is a subtype selective PPARalpha agonist with potent lipid lowering activity
文献作者:Brown,P.J.; Winegar,D.A.; Plunket,K.D.; Moore,L.B.; Lewis,M.C.; Wilson,J.G.; Sundseth,S.S.; Koble,C.S.; Wu,Z.; Chapman,J.M.; Lehmann,J.M.; Kliewer,S.A.; Willson,T.M.
参考来源:J Med Chem 1999,42(19),3785

新产品编号:1675847

Chemical Name: 3,5-Dichloro-2-(3,5-dichloro-2-hydroxyphenylsulfonamido)-N-[4-(6-ethoxybenzothiazol-2-ylsulfanyl)phenyl]benzamide
项目整合开发状态: Biological Testing
项目研究机构: Bayer (Originator)
合成路线:T...
参考文献标题:Synthesis and structure activity relationships of novel small molecule cathepsin D inhibitors
文献作者:Dumas,J.; Britelli,D.; Chen,J.; Dixon,B.; Hatoum-Mokdad,H.; K鰊ig,G.; Sibley,R.; Witowsky,J.; Wong,S.
参考来源:Bioorg Med Chem Lett 1999,9(17),2531