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

LY-438434

Chemical Name: 2-Methylalanyl-5-phenyl-D-norvalyl-4-amino-1H-imidazol-1-ylacetyl-N1-benzyl-L-prolinamide; N-[2-[4-[2(R)-(2-amino-2-methylpropanamido)-5-phenylpentanamido]-1H-imidazol-1-yl]acetyl]-L-pr...
参考文献标题:Growth hormone secretagogues
文献作者:Jungheim,L.N.; Palkowitz,A.D.; Trankle,W.G.; Lugar,C.W.III; Muehl,B.S.; Ratz,A.M.; Copp,J.D.; Jones,S.A.; Kennedy,J.H.; Shepherd,T.A.; Alt,C.A.; Fahey,K.J.; Thrasher,K.J.; Cohen,J.D.; Gritton,W.H.; et al.(Eli Lilly and Company)
参考来源:EP 0933365; WO 9908699

BPDZ-42

Chemical Name: 3-(2-Butylamino)-4H-pyrido[4,3-e]-1,2,4-thiadiazine 1,1-dioxide
项目整合开发状态: Preclinical
项目研究机构: Universit?Libre de Bruxelles (Originator), University of Li鑗e (Originator)
合成路线:Th...
参考文献标题:Preparation and pharmacological evaluation of the R- and S-enantiomers of 3-(2'-butylamino)-4H- and 3-(3'-methyl-2'-butylamino)-4H-pyrido[4,3-e]-1,2,4-thiadiazine 1,1-dioxide,two tissue selective ATP-sensitive potassium channel openers
文献作者:Khelili,S.; de Tullio,P.; Lebrun,P.; Fillet,M.; Antoine,M.H.; Ouedraogo,R.; Dupont,L.; Fontaine,J.; Felekidis,A.; Leclerc,G.; Delarge,J.; Pirotte,B.
参考来源:Bioorg Med Chem 1999,7(8),1513

AGR-129

Chemical Name: N-(3-Chlorobenzyl)-2-cyano-3-[2-[3-(1H-imidazol-2-ylsulfanyl)propoxy]phenyl]-2(E)-propenamide
项目整合开发状态: Biological Testing
项目研究机构: Hebrew University (Originator)
合成路线:Salicylal...
参考文献标题:alpha-Cyanocinnamide derivatives: A new family of non-peptide,non-sulfhydryl inhibitors of Ras farnesylation
文献作者:Poradosu,E.; Gazit,A.; Reuveni,H.; Levitzki,A.
参考来源:Bioorg Med Chem 1999,7(8),1727

新产品编号:1660027

Chemical Name: 2(R)-[2,6-Dibromo-4-(6-bromobenzo[b]naphtho[2,3-d]furan-11-yl)phenoxy]-3-phenylpropionic acid
项目整合开发状态: Preclinical
项目研究机构: Wyeth Pharmaceuticals (Originator)
合成路线:Condensation...
参考文献标题:11-Aryl-benzo[b]naphtho[2,3-d]furans and 11-aryl-benzo[b]naphtho[2,3-d]thiophenes useful in the treatment of insulin resistance and hyperglycemia
文献作者:Dietrich,A.J.; Wrobel,J.E.; Li,Z.(American Home Products Corp.)
参考来源:WO 9958521

新产品编号:1661609

Chemical Name: 2-(3-Pentyl-3H-1,2-diaziren-3-yl)ethanol
项目整合开发状态: Preclinical
项目研究机构: Harvard Medical School (Originator), Massachusetts General Hospital (Originator), UCLA School of Medicine (O...
参考文献标题:Synthesis and properties of 3-(2-hydroxyethyl)-3-N-pentyldiazirine,a photoactivable general anesthetic
文献作者:Husain,S.S.; Forman,S.A.; Kloczewiak,M.A.; Addona,G.H.; Olsen,R.W.; Pratt,M.B.; Cohen,J.B.; Miller,K.W.
参考来源:J Med Chem 1999,42(17),3300

新产品编号:1663191

Chemical Name: 12-Amino-9-ethyl-3-methyl-6,7,10,11-tetrahydro-7(S),11(S)-methanocycloocta[b]quinoline
项目整合开发状态: Biological Testing
项目研究机构: Medichem (Originator)
合成路线:Condensation of diketone ...
参考文献标题:Polycyclic aminopyridine cpds.which are acetylcholinesterase inhibitors,process for preparing them and their use
文献作者:Contreras Lascorz,J.; El Achab,R.; Camps Garcia,P.; Ba駉s Diez,J.E.; Mu駉z-Torrero Lopez-Ibarra,D.; Badia Sancho,A.; Morral Cardoner,J.; Simon Fornell,M.; G鰎big Romeu,M.; Vivas,N.M.(Medichem SA)
参考来源:EP 0796849; ES 2100129; US 5965569; WO 9713754

新产品编号:1664773

Chemical Name: 3,5,11,11a-Tetrahydrothiazolo[2,3-c]-1,4-benzothiazepine-5,11(2H)-dione
项目整合开发状态: Biological Testing
项目研究机构: Achillion (Originator), National Institutes of Health (Originator), US...
参考文献标题:Thiazepine inhibitors of HIV-1 integrase
文献作者:Garofalo,A.; Pommier,Y.; Neamati,N.; Nacci,V.(US Department of Health & Human Services)
参考来源:WO 0068235

新产品编号:1666355

Chemical Name: 2-Azaspiro[4.5]decane-4(R)-carboxylic acid hydrochloride
项目整合开发状态: Preclinical
项目研究机构: Pfizer (Originator)
合成路线:The condensation of cyclohexanone (I) with ethyl cyanacetate (II...
参考文献标题:Conformationally constrained amino acid cpds.having affinity for the alpha2delta subunit of a calcium channel
文献作者:Horwell,D.C.; Bryans,J.S.; Receveur,J.-M.(Pfizer Inc.)
参考来源:WO 9961424

新产品编号:1667937

Chemical Name: N-[1(S)-Benzyl-3-[2-[5-(3-cyanophenyl)-2-thienylsulfonamido]ethylamino]-2,3-dioxopropyl]-2,6-dichlorobenzamide
项目整合开发状态: Biological Testing
项目研究机构: Cephalon (Originator)
合成路线:E...
参考文献标题:Peptidyl-containing alpha-ketoamide cysteine and serine protease inhibitors
文献作者:Wells,G.J.; Mallamo,J.P.; Chatterjee,S.; Bihovsky,R.(Cephalon,Inc.)
参考来源:US 6150378

新产品编号:1669519

Chemical Name: (1R,5S,6S)-2-[5(S)-[3(S),4(S)-Dihydroxypyrrolidin-1-ylcarbonyl]pyrrolidin-3(S)-ylsulfanyl]-6-[1(R)-hydroxyethyl]-1-methyl-1-carba-2-penem-3-carboxylic acid
项目整合开发状态: Preclinical
项...
参考文献标题:Synthesis and biological evaluation of novel 1beta-methylcarbapenems having a new moiety at C-2
文献作者:Kang,Y.K.; Shin,K.J.; Yoo,K.H.; Seo,K.J.; Park,S.Y.; Kim,D.J.; Park,S.W.
参考来源:Bioorg Med Chem Lett 1999,9(16),2385