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:1356283

Chemical Name: 4-[4-(4-Acetylphenyl)piperazin-1-yl]-7,9-diphenylpyrido[3',2':4,5]thieno[3,2-d]pyrimidine; 4-[4-(7,9-Diphenylpyrido[3',2':4,5]thieno[3,2-d]pyrimidin-4-yl)piperazin-1-yl]acetophenone
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参考文献标题:Synthesis and antiallergic activity of pyridothienopyrimidines
文献作者:Quintela,J.M.; Peinador,C.; Veiga,C.; Gonzalez,L.; Botana,L.M.; Alfonso,A.; Riguera,R.
参考来源:Bioorg Med Chem 1998,6(10),1911

KNI-684

Chemical Name: 3'-Azido-5'-O-[3-[N-[1(S)-benzyl-2(S)-[4(R)-(N-tert-butylcarbamoyl)-5,5-dimethylthiazolidin-3-ylcarbonyl]-2-hydroxyethyl]carbamoyl]-2,2-dimethylpropionyl]-3'-deoxythymidine
项目整合开发状态:...
参考文献标题:A new class of potent anti-HIV agents,conjugates of HIV protease inhibitors containing carboxylic acid with reverse transcriptase inhibitor
文献作者:Kiso,Y.; Kimura,T.; Akaji,K.; Matsuda,T.; Matsumoto,H.; Hamawaki,T.
参考来源:Symp Med Chem 1998,Abst 1-P-17

KNI-685

Chemical Name: 3'-Azido-5'-O-[3-[N-[1(S)-benzyl-2(S)-[4(R)-(N-tert-butylcarbamoyl)-5,5-dimethylthiazolidin-3-ylcarbonyl]-2-hydroxyethyl]carbamoyl]-2-methylbutyryl]-3'-deoxythymidine
项目整合开发状态: Biolo...
参考文献标题:A new class of potent anti-HIV agents,conjugates of HIV protease inhibitors containing carboxylic acid with reverse transcriptase inhibitor
文献作者:Kiso,Y.; Kimura,T.; Akaji,K.; Matsuda,T.; Matsumoto,H.; Hamawaki,T.
参考来源:Symp Med Chem 1998,Abst 1-P-17

Thionisoxetine-(R), (R)-Thionisoxetine, LY-368975

Chemical Name: (R)-N-Methyl-3-[2-(methylsulfanyl)phenoxy]-3-phenylpropylamine hydrochloride
项目整合开发状态: Preclinical
项目研究机构: Lilly (Originator)
合成路线:Reduction of 3-chloropropiophenone (I) with N...
参考文献标题:N-Alkyl-3-phenyl-3-(2-alkylthiophenoxy)propylamines
文献作者:Gehlert,D.R.; Robertson,D.W.; Wong,D.T.(Eli Lilly and Company)
参考来源:EP 0591581

新产品编号:1357865

Chemical Name: 8(S)-Bromomethyl-6-[3-(2-methoxypyrimidin-5-yl)-2(E)-propenoyl]-2-methyl-4-(4-methyl-1-piperazinylcarbonyloxy)-3,6,7,8-tetrahydropyrrolo[3,2-e]indole-1-carboxylic acid methyl ester hydr...
参考文献标题:New water-soluble duocarmycin derivatives: Synthesis and antitumor activity of A-ring pyrrole compounds bearing beta-heteroarylacryloyl groups
文献作者:Amishiro,N.; Nagamura,S.; Kobayashi,E.; Gomi,K.; Saito,H.
参考来源:J Med Chem 1999,42(4),669

新产品编号:1359447

Chemical Name: (?-1,1-Difluoro-1-[(1R*,2S*)-2-[2-(6-oxo-1,6-dihydro-9H-purin-9-yl)ethyl]cyclopropyl]methylphosphonic acid; (?-1,1-Difluoro-1-[(1R*,2S*)-2-[2-(hypoxanthin-9-yl)ethyl]cyclopropyl]methylp...
参考文献标题:Synthesis of novel nucleotide analogues possessing difluoromethylene phosphonate pharmacophore.Evaluation of the inhibitory activities of PNPases
文献作者:Shimeno,H.; Suemune,K.; Abe,H.; Yokomatsu,T.; Kihara,T.; Sato,M.; Soeda,S.; Shibuya,S.
参考来源:Symp Med Chem 1998,Abst 1-P-06

新产品编号:1361029

Chemical Name: 5-Amino-2-[3(R)-methyl-2,6-dioxohexahydro-3-pyridinyl]-1H-isoindole-1,3(2H)-dione
项目整合开发状态: Biological Testing
项目研究机构: Massachusetts Institute of Technology (Originator), Universi...
参考文献标题:Tumor necrosis factor-alpha production enhancing activity of substituted 3'-methylthalidomide: Influence of substituents at the phthaloyl moiety on the activity and stereoselectivity
文献作者:Miyachi,H.; Koiso,Y.; Shirai,R.; Niwayama,S.; Liu,J.O.; Hashimoto,Y.
参考来源:Chem Pharm Bull 1998,46(7),1165

新产品编号:1362611

Chemical Name: 5-Amino-2-[3(S)-methyl-2,6-dioxohexahydro-3-pyridinyl]-1H-isoindole-1,3(2H)-dione
项目整合开发状态: Biological Testing
项目研究机构: Massachusetts Institute of Technology (Originator), Universi...
参考文献标题:Tumor necrosis factor-alpha production enhancing activity of substituted 3'-methylthalidomide: Influence of substituents at the phthaloyl moiety on the activity and stereoselectivity
文献作者:Miyachi,H.; Koiso,Y.; Shirai,R.; Niwayama,S.; Liu,J.O.; Hashimoto,Y.
参考来源:Chem Pharm Bull 1998,46(7),1165

新产品编号:1364193

Chemical Name: 3-[3-(Benzothiazol-6-yl)ureido]-1-[3-(3-isopropylureido)benzyl]-2,3,4,5-tetrahydro-1H-1-benzazepin-2-one
项目整合开发状态: Biological Testing
项目研究机构: Shionogi (Originator)
合成路线:Treatme...
参考文献标题:1,3-Disubstituted benzazepines as novel,potent,selective neuropeptide Y Y1 receptor antagonists
文献作者:Murakami,Y.; Hara,H.; Okada,T.; Hashizume,H.; Kii,M.; Ishihara,Y.; Ishikawa,M.; Shimamura,M.; Mihara,S.; Kato,G.; Hanasaki,K.; Hagishita,S.; Fujimoto,M.
参考来源:J Med Chem 1999,42(14),2621

新产品编号:1365775

Chemical Name: (6R,8R,9R)-N-[4-Amino-9-(tert-butyldimethylsilyloxy)-6-(tert-butyldimethylsilyloxymethyl)-1,7-dioxa-2-thiaspiro[4.4]-3-nonen-8-yl]-N'-(2-methylpropenoyl)urea S,S-dioxide
项目整合开发状态: Bi...
参考文献标题:Abasic analogues of TSAO-T as the first sugar derivatives that specifically inhibit HIV-1 reverse transcriptase
文献作者:Vel醶quez,S.; Chamorro,C.; Perez-Perez,M.J.; Alvarez,R.; Jimeno,M.L.; Martin-Domenech,A.; Perez,C.; Gago,F.; De Clercq,E.; Balzarini,J.; San-Felix,A.; Camarasa,M.J.
参考来源:J Med Chem 1998,41(23),4636