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:1090507

Chemical Name: 1-[4-(3,5-Dibromo-8-chloro-11H-benzo[5,6]cyclohepta[1,2-b]pyridin-11-yl)piperidin-1-yl]-2-(1-oxidopyridin-4-yl)ethanone
项目整合开发状态: Biological Testing
项目研究机构: Schering-Plough (Origi...
参考文献标题:Potent,selective,and orally bioavailable tricyclic pyridyl acetamide N-oxide inhibitors of farnesyl protein transferase with enhanced in vivo antitumor activity
文献作者:Njoroge,F.G.; Vibulbhan,B.; Pinto,P.; Bishop,W.R.; Bryant,M.S.; Nomeir,A.A.; Lin,C.C.; Liu,M.; Doll,R.J.; Girijavallabhan,V.; Ganguly,A.K.
参考来源:J Med Chem 1998,41(10),1561

新产品编号:1092089

Chemical Name: 20-(Hydroxyimino)-4,16-pregnadien-3-one
项目整合开发状态: Biological Testing
项目研究机构: University of Maryland (Originator)
合成路线:Title compound was obtained by Oppenauer oxidation of 3-be...
参考文献标题:Synthesis and in vitro activity of some epimeric 20alpha-hydroxy,20-oxime and aziridine pregnene derivatives as inhibitors of human 17alpha-hydroxylase/C17,20-lyase and 5alpha-reductase
文献作者:Ling,Y.-Z.; Li,J.S.; Kato,K.; Liu,Y.; Wang,X.; Klus,G.T.; Marat,K.; Nnane,I.P.; Brodie,A.M.
参考来源:Bioorg Med Chem 1998,6(10),1683

SNO-Yohimbine, S-Nitrosylated yohimbine, NMI-187

Chemical Name: (1R,2S,4aR,13bS,14aS)-13-Acetyl-2-[3-methyl-3-(nitrososulfanyl)butanoyloxy]-1,2,3,4,4a,5,7,8,13,13b,14,14a-dodecahydrobenz[g]indolo[2,3-a]quinolizine-1-carboxylic acid methyl ester
项...
参考文献标题:Nitrosated and nitrosylated alpha-adrenergic receptor antagonist cpds.,compsns.and their uses
文献作者:Saenz de Tejada,I.; Schroeder,J.D.; Carvey,D.S.(NitroMed Inc.)
参考来源:JP 2000505424; WO 9727749

新产品编号:1093671

Chemical Name: N-(4-Methoxy-2,3-dihydro-1H-phenalen-2-yl)acetamide
项目整合开发状态: Biological Testing
项目研究机构: ADIR (Originator)
合成路线:2-Methoxynaphthalene (I) was condensed with bis(N-phenyl-chlorom...
参考文献标题:Melatonergic properties of the (+)- and (-)-enanti
文献作者:Jellimann,C.; Mathe-Allainmat,M.; Andrieux,J.; Renard,P.; Delagrange,P.; Langlois,M.
参考来源:J Med Chem 1999,42(6),1100

新产品编号:1095253

Chemical Name: 2-[2-(1,3-Benzodioxol-5-yl)acetyl]-N-(4-chloro-3-methylisoxazol-5-yl)thiophene-3-sulfonamide
项目整合开发状态: Biological Testing
项目研究机构: Encysive Pharmaceuticals (Originator)
合成路线:5-A...
参考文献标题:Sulfonamides and derivs.thereof that modulate the activity of endothelin
文献作者:Chan,M.F.; Raju,B.G.; Kois,A.; Verner,E.J.; Wu,C.; Castillo,R.S.; Yalamoori,V.; Balaji,V.N.; Ramnarayan,K.(ImmunoPharmaceutics,Inc.)
参考来源:EP 0699191; EP 0870764; GB 2285625; JP 1996510744; US 5464853; WO 9427979

HSP-117

Chemical Name: (2S,3S)-3-(5-Isopropyl-2,3-dihydrobenzofuran-7-ylmethylamino)-2-phenylpiperidine dihydrochloride
项目整合开发状态: Preclinical
项目研究机构: Hisamitsu (Originator)
合成路线:Reductive condensatio...
参考文献标题:Piperidine derivs.
文献作者:Tanaoue,Y.; Beppu,K.; Okayama,A.; Sakamoto,O.(Hisamitsu Pharmaceutical Co.,Ltd.)
参考来源:EP 0826684; US 5886011; WO 9630367

KP-21

Chemical Name: 3'-Azido-3'-deoxy-5'-O-(4-oxatetradecanoyl)thymidine
项目整合开发状态: Biological Testing
项目研究机构: University of Alberta (Originator)
合成路线:Acid chloride (II) prepared from 4-oxatetradec...
参考文献标题:Synthesis,in vitro anti-human immunodeficiency virus structure-activity relationships and biological stability of 5'-O-myristoyl analogue derivatives of 3'-azido-2',3'-dideoxythymidine (AZT) as potential prodrugs
文献作者:Parang,K.; Wiebe,L.I.; Knaus,E.E.
参考来源:Antivir Chem Chemother 1998,9(4),311-323

新产品编号:1096835

Chemical Name: 5-Methyl-5H-indazolo[2,3-b]isoquinolinium hydrogensulfate
项目整合开发状态: Biological Testing
项目研究机构: Hungarian Academy of Sciences (Originator)
合成路线:3-Hydroxyisoquinoline (I) was con...
参考文献标题:Synthesis of novel ellipticine analogues and their inhibition of moloney leukaemia reverse transcriptase
文献作者:Messmer,A.; Nacsa,J.; Tim醨i,G.; Haj�? G.; Moln�? J.; So�? T.
参考来源:Bioorg Med Chem Lett 1996,6(21),2831-2836

UCS1006-S15, KF-25706

Chemical Name: 13-Chloro-5(S),6(S)-epoxy-14,16-dihydroxy-11-(hydroxyimino)-3(R)-methyl-3,4,5,6,11,12-hexahydro-1H-2-benzoxacyclotetradecin-1-one
项目整合开发状态: Preclinical
项目研究机构: Kyowa Hakko (Origin...
参考文献标题:Radicicol derivs.
文献作者:Agatsuma,T.; Saitoh,Y.; Yamashita,Y.; Mizukami,T.; Akinaga,S.; Gomi,K.; Akasaka,K.; Takahashi,I.(Kyowa Hakko Kogyo Co.,Ltd.)
参考来源:EP 0823429; US 5977165; WO 9633989

HSR-113

Chemical Name: endo-4-[3-(4-Amino-5-chloro-2-methoxybenzamido)-9-azabicyclo[3.3.1]non-9-yl]butyric acid ethyl ester
项目整合开发状态: Phase I
项目研究机构: Abbott (Originator)
合成路线:4-Acetylamino-2-methoxyb...
参考文献标题:Benzamide deriv.
文献作者:Ito,Y.; Kato,H.; Yasuda,S.; Iwasaki,N.; Nishino,H.; Takeshita,M.(Hokuriku Seiyaku Co.,Ltd.)
参考来源:EP 0640601; US 5395832; US 5500422; WO 9214705