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

S-3304

Chemical Name: N-[5-(4-Methylphenylethynyl)thien-2-ylsulfonyl]-D-tryptophan
项目整合开发状态: Phase I/II
项目研究机构: Shionogi (Originator)
合成路线:The sulfonation of D-tryptophan tert-butyl ester (I) with 4...
参考文献标题:Sulfonated amino acid derivs.and metalloproteinase inhibitors containing the same
文献作者:Watanabe,F.; Tsuzuki,H.; Ohtani,M.(Shionogi & Co.Ltd.)
参考来源:EP 0950656; JP 2001316254; US 6207698; US 6235768; US 6441021; WO 9727174

新产品编号:1180681

Chemical Name: N-[2,2-Dimethyl-1(S)-(N-methylcarbamoyl)propyl]-2(R)-[2(S)-hydroxy-3-sulfanylpropyl]nonanamide
项目整合开发状态: Biological Testing
项目研究机构: Wyeth Pharmaceuticals (Originator)
合成路线:The ...
参考文献标题:The asymmetric synthesis and in vitro characterization of succinyl mercaptoalcohol and mercaptoketone inhibitors of matrix metalloproteinases
文献作者:Levin,J.I.; DiJoseph,J.F.; Killar,L.M.; Sharr,M.A.; Skotnicki,J.S.; Patel,D.V.; Xiao,X.-Y.; Shi,L.; Navre,M.; Campbell,D.A.
参考来源:Bioorg Med Chem Lett 1998,8(10),1163

新产品编号:1182263

Chemical Name: N-(3,5-Dichloropyridinyl-4-yl)-4-methoxy-2-(methoxymethyl)-1H-benzimidazole-7-carboxamide
项目整合开发状态: Preclinical
项目研究机构: Aventis Pharma (Originator)
合成路线:The title compound was ...
参考文献标题:2-Substituted-4-methoxybenzimidazole-based PDE4 inhibitors
文献作者:Regan,J.; Bruno,J.; McGarry,D.; Poli,G.; Hanney,B.; Bower,S.; Travis,J.; Sweeney,D.; Miller,B.; Souness,J.; Djuric,S.
参考来源:Bioorg Med Chem Lett 1998,8(19),2737

Cryptophycin 52, LY-355703

Chemical Name: [3S-(3alpha,10beta,13E,16beta)]-10-(3-Chloro-4-methoxybenzyl)-16-[2(R*),3(R*)-epoxy-1(R)-methyl-3-phenylpropyl]-3-isobutyl-6,6-dimethyl-1,4-dioxa-8,11-diazacyclohexadec-13-ene-2,5,9,12-...
参考文献标题:Stereoselective process for producing antineoplastic agents
文献作者:Zmijewski,M.J.J.; Zhang,T.Y.; Aikins,J.A.; Briggs,B.S.(Eli Lilly and Company; University of Hawaii; Wayne State University)
参考来源:WO 0023429

SM-20220

Chemical Name: N-(1-Methyl-1H-indol-2-ylcarbonyl)guanidine methanesulfonate
项目整合开发状态: Preclinical
项目研究机构: Sumitomo Pharmaceuticals (Originator)
合成路线:The methylaion of 4-methyl-1H-indole-2-car...
参考文献标题:Indoloylguanidine derivs.as inhibitors of sodium-hydrogen exchange
文献作者:Kojima,A.; Kitano,M.; Miyagishi,A.; Noguchi,T.; Yagi,H.; Nakano,K.; Ohashi,N.(Sumitomo Pharmaceuticals Co.,Ltd.)
参考来源:CA 2121391; EP 0622356; JP 1995010839

AH-1058

Chemical Name: 4-(5H-Dibenzo[a,d]cyclohepten-5-ylidene)-1-[3-(3-methoxy-2-nitrophenyl)-2(E)-propenyl]piperidine hydrochloride
项目整合开发状态: Preclinical
项目研究机构: Ajinomoto (Originator)
合成路线:Treatme...
参考文献标题:Piperidine derivs.and their use as antiarrhythmic agents
文献作者:Hirasawa,A.; Shoji,M.; Yoshimoto,R.; Gyotoku,Y.; Eguchi,C.(Ajinomoto Co.,Inc.)
参考来源:EP 0479601; JP 1993025044; US 5229400

DB-480

Chemical Name: 4,4'-(Furan-2,4-diyl)bis(N1-isopropylbenzamidine) dihydrochloride
项目整合开发状态: Preclinical
项目研究机构: University of Georgia (Originator), University of North Carolina (Originator)
合成...
参考文献标题:2,4-Bis (4-amidino)phenyl furans as anti-Pneumocystis carinii agents
文献作者:Boykin,D.W.; Francesconi,I.; Tidwell,R.R.; Wilson,D.W.(Georgia State University; University of North Carolina)
参考来源:EP 0941991; GB 2334716; US 6008247

tRA-96023, SB-RA-31012

Chemical Name: [2aR-(2aalpha,4beta,4abeta,6beta,9alpha,11beta,12alpha,12aalpha,12balpha)]-6,9,12b-Triacetoxy-12-benzoyloxy-4-[3-(4-benzoylphenyl)-2(E)-propenoyloxy]-11-hydroxy-4a,8,13,13-tetramethyl-2...
参考文献标题:Taxoid reversal agents for drug-resistance in cancer chemotherapy and pharmaceutical compsns.thereof
文献作者:Bernacki,R.J.; Ojima,I.(State University of New York,Albany)
参考来源:EP 0966456; US 5811452; WO 9830553

OPC-28326

Chemical Name: N-[2,6-Dimethyl-4-[4-[N-methyl-N-(2-phenylethyl)amino]piperidin-1-ylcarbonyl]phenyl]propionamide hydrochloride monohydrate
项目整合开发状态: Phase II
项目研究机构: Otsuka (Originator)
合成路线:C...
参考文献标题:Peripheral vasodilating agent containing N-acylated 4-amino piperidine derivs.as active ingredients
文献作者:Fujioka,T.; Teramoto,S.; Tanaka,M.; Shimizu,H.; Tabusa,F.; Tominaga,M.(Otsuka Pharmaceutical Co.,Ltd.)
参考来源:EP 0650476; JP 1994340627; US 5656642; US 5760058; US 6136826; WO 9422826

PKI-75166, PKI-166, CGP-75166

Chemical Name: 4-[4-[1(R)-Phenylethylamino]-7H-pyrrolo[2,3-d]pyrimidin-6-yl]phenol
项目整合开发状态: Discontinued
项目研究机构: Novartis (Originator)
合成路线:The cyclization of 4-methoxyphenacyl bromide (I) w...
参考文献标题:Pyrrolopyrimidines and processes for the preparation thereof
文献作者:Traxler,P.; Bold,G.; Brill,W.K.-D.; Frei,J.(Novartis AG)
参考来源:EP 0836605; JP 1999508570; US 6140332; WO 9702266