项目整合精选

聚焦新型临床类新产品的整合与转化. 在创新药研发领域，传统的“单一产品、单打独斗”模式正在被一种更系统化的“项目整合”思维所取代。项目整合的核心，在于将散落在研发早期、中期的创新资产，通过资金、临床资源、产业生态等多维度要素的有机组合，实现从“科学发现”到“临床价值”，再到“商业成功”的跨越。研发与商业的战略整合：从“资产思维”到“组合思维”它要求我们超越单个分子的视野，拥抱一个由技术创新、临床需求、资本支持和商业洞察共同构成的复杂网络。在这个网络中，成功的标准不再是单一的“获批上市”，而是能否通过高效的整合，将科学上的突破，转化为临床上真正可及、商业上可持续、能够惠及患者的解决方案。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，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。
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项目整合精选

[18F]FCWAY

Chemical Name: trans-4-(18Fluoro)-N-[2-[4-(2-methoxyphenyl)piperazin-1-yl]ethyl]-N-(2-pyridinyl)cyclohexanecarboxamide
CAS No. 223699-98-7
项目整合开发状态: Preclinical
项目研究机构: Lilly (Originator)
...
参考文献标题:Synthesis of a series of stromelysin-selective thiadiazole urea matrix metalloproteinase inhibitors
文献作者:Jacobsen,E.J.; Mitchell,M.A.; Hendges,S.K.; Belonga,K.L.; Skaletzky,L.L.; Stelzer,L.S.; Lindberg,T.J.; Fritzen,E.L.; Schostarez,H.J.; O'Sullivan,T.J.; Maggiora,L.L.; Stuchly,C.W.; Laborde,A.L.; Kubicek,M,F.; Poorman,R.A.; et al.
参考来源:J Med Chem 1999,42(9),1525

SKK-60060

Chemical Name: 2-Tetradecylhexadecyl 2-O-(3-O-sulfo-6-deoxy-alpha-L-galactopyranosyl)-3-O-sulfo-beta-D-galactopyranoside disodium salt
CAS No. 190443-07-3
项目整合开发状态: Preclinical
项目研究机构: Sanwa ...
参考文献标题:Sulfated and phosphated saccharide derivs.,process for the preparation of the same and use thereof
文献作者:Usui,T.; Igami,T.; Kakigami,T.; Hamashima,H.; Jomori,T.; Tashita,A.; Ishiwatari,Y.; Yokochi,S.; Mitani,T.; Suzuki,Y.; Hasegawa,A.(Sanwa Kagaku Kenkyusho Co.,Ltd.)
参考来源:EP 0771815; JP 1997183789; US 5869460

AMG-126737

Chemical Name: N,N'-(Pentane-1,5-diyl)bis(oxy)bis(1,4-phenylene)bis(methylene)bis(3-amidinobenzenesulfonamide)
CAS No. 224054-76-6
项目整合开发状态: Preclinical
项目研究机构: Array BioPharma (Originator), ...
参考文献标题:Cpds.which inhibit tryptase activity
文献作者:Burgess,L.; Rizzi,J.P.(Array BioPharma,Inc.)
参考来源:WO 9924395

GT-2204, VUF-5297

Chemical Name: (1S,2S)-2-(1H-Imidazol-4-yl)cyclopropylamine
CAS No. 186194-74-1 (trans-isomer), 24160-41-6 (undefined isomer)
项目整合开发状态: Preclinical
项目研究机构: Gliatech (Originator), Vrije Univer...
参考文献标题:Characterization of the binding site of the histamine H3 receptor.1.Various approaches to the synthesis of 2-(1H-imidazol-4-yl)cyclopropylamine and histaminergic activity of (1R,2R)- and (1S,2S)-2-(1H-imidazol-4-yl)-cyclopropylamine
文献作者:De Esch,I.J.; Vollinga,R.C.; Goubitz,K.; Schenk,H.; Appelberg,U.; Hacksell,U.; Lemstra,S.; Zuiderveld,O.P.; Hoffmann,M.; Leurs,R.; Menge,W.M.; Timmerman,H.
参考来源:J Med Chem 1999,42(7),1115

新产品编号:233063

Chemical Name: 1-Benzyl-3-(benzyloxymethyl)-3,4-dihydro-1H-1,3-benzothiadiazin-4-one S,S-dioxide
CAS No. 190835-51-9
项目整合开发状态: Biological Testing
项目研究机构: CSIC (Originator), Rega Institute for...
参考文献标题:Novel potential agents for human cytomegalovirus infection: Synthesis and antiviral activity evaluation of benzothiadiazine dioxide acyclonucleosides
文献作者:Martinez,A.; Esteban,A.I.; Castro,A.; Gil,C.; Conde,S.; Andrei,G.; Snoeck,R.; Balzarini,J.; De Clercq,E.
参考来源:J Med Chem 1999,42(7),1145

新产品编号:560537

Chemical Name: (Z)-2-(1-Azabicyclo[2.2.2]oct-3-ylidene)-1-[4-(4-bromobenzoyl)phenyl]ethanone
CAS No. 223726-07-6
项目整合开发状态: Preclinical
项目研究机构: AstraZeneca (Originator)
合成路线:Addition of lit...
参考文献标题:Quinuclidine inhibitors of 2,3-oxidosqualene cyclase-lanosterol synthase: Optimization from lipid profiles
文献作者:Brown,G.R.; Hollinshead,D.M.; Stokes,E.S.; Clarke,D.S.; Eakin,M.A.; Foubister,A.J.; Glossop,S.C.; Griffiths,D.; Johnson,M.C.; McTaggart,F.; Mirrlees,D.J.; Smith,G,J.; Wood,R.
参考来源:J Med Chem 1999,42(7),1306

beta-L-2'-Fd4FC

Chemical Name: 1-(2,3-Dideoxy-2-fluoro-beta-L-glycero-pent-2-enofuranosyl)-5-fluorocytosine
CAS No. 181785-91-1
项目整合开发状态: Biological Testing
项目研究机构: Emory University (Originator), University ...
参考文献标题:Synthesis and anti-HIV and anti-HBV activities of 2'-fluoro-2',3'-unsaturated L-nucleosides
文献作者:Lee,K.; Choi,Y.; Gullen,E.; Schlueter-Wirtz,S.; Schinazi,R.F.; Cheng,Y.C.; Chu,C.K.
参考来源:J Med Chem 1999,42(7),1320

LR-172

Chemical Name: N-[2-(3,4-Dichlorophenyl)ethyl]-N-methylhexahydro-1H-azepine-1-ethanamine
CAS No. 138356-42-0
项目整合开发状态: Preclinical
项目研究机构: National Institutes of Health (Originator), Pfizer (...
参考文献标题:N-(Arylethyl)-N-alkyl-2-(1-pyrrolidinyl)ethylamine derivs.for CNS disorders
文献作者:De Costa,B.R.; Radesca,L.; Bowen,W.; Long,J.; Walker,J.M.; Rice,K.C.; Gray,N.M.; Contreras,P.C.(Pharmacia Corp.)
参考来源:EP 0518216; WO 9222279

新产品编号:280523

Chemical Name: trans-3-Propyl-5,6,6a,7,8,12b-hexahydronaphtho[1,2-f][1,7]naphthyridine-10,11-diol
CAS No. 197007-99-1, 197007-53-7 (diHBr)
项目整合开发状态: Biological Testing
项目研究机构: Abbott (Origina...
参考文献标题:Trans-2,6-,3,6- and 4,6-diaza-5,6,6a,7,8,12b-hexahydrobenzo[c]phenanthrene cpds.as dopamine agonists
文献作者:Michaelides,M.; Gu,Y.G.; Shiosaki,K.(Abbott Laboratories Inc.)
参考来源:US 5668141; WO 9736902

新产品编号:236227

Chemical Name: N-[7-(Hydroxymethyl)-3,11,15-trimethylhexadeca-2(E),6(Z),10(E),14-tetraenyl]-N'-(2-phenylethyl)thiourea
CAS No. 191042-72-5
项目整合开发状态: Biological Testing
项目研究机构: Sankyo (Origina...
参考文献标题:A highly stereoselective synthesis of plaunotol and its thiourea derivatives as potent antibacterial agents against Helicobacter pylori
文献作者:Kogen,H.; Tago,K.; Arai,M.; Minami,E.; Masuda,K.; Akiyama,T.
参考来源:Bioorg Med Chem Lett 1999,9(10),1347