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

RO-1169132/238

Chemical Name: 4-(3,4-Dichlorobenzyl)-1-methyl-1-[3-methyl-2(R)-[3-(3,4,5-trimethoxyphenyl)ureido]butyl]piperidinium chloride
CAS No. 270572-42-4
项目整合开发状态: Preclinical
项目研究机构: Roche Bioscienc...
参考文献标题:Piperidine CCR-3 receptor antagonists
文献作者:Kertesz,D.J.; Smith,D.B.; Hirschfeld,D.R.(F.Hoffmann-La Roche AG)
参考来源:DE 19955793; EP 1131290; GB 2343894; JP 2002530375; US 6342509; WO 0031033

AD-101, SCH-350581

Chemical Name: 4-[1-(2,4-Dimethyl-3-pyridinylcarbonyl)-4-methyl-4-piperidinyl}-2(S)-methyl-1-[1(S)-[4-(trifluoromethyl)phenyl]ethyl]piperazine
CAS No. 306293-36-7
项目整合开发状态: Preclinical
项目研究机构...
参考文献标题:Piperazine derivs.useful as CCR5 antagonists
文献作者:Labroli,M.A.; Smith,E.M.; Baroudy,B.M.; Gilbert,E.; Tagat,J.R.; Josien,H.B.; Steensma,R.; Laughlin,M.A.; Miller,M.W.; Clader,J.W.; McKittrick,B.A.; Neustadt,B.R.; Palani,A.; McCombie,S.W.; Vice,S.F.(Schering Corp.)
参考来源:EP 1175401; WO 0066558

新产品编号:334311

Chemical Name: N,N-Dimethyl-N'-[1-(10H-pyrazino[2,3-b][1,4]benzothiazin-8-ylmethyl)piperidin-4-yl]sulfamide
CAS No. 203648-51-5
项目整合开发状态: Preclinical
项目研究机构: Eisai (Originator)
合成路线:Displa...
参考文献标题:Benzopiperidine derivs.
文献作者:Kaneko,T.; Clark,R.; Ohi,N.; Ozaki,F.; Kawahara,T.; Kamada,A.; Okano,K.; Yokohama,H.; Muramoto,K.; Arai,T.; Ohkuro,M.; Takenaka,O.; Sonoda,J.(Eisai Co.,Ltd.)
参考来源:EP 0934941; WO 9806720

SNJ-1558

Chemical Name: N1-[1(S)-[2-(Dimethylamino)acetylhydrazonomethyl]-3-methylbutyl]-N2-(4-fluorophenylsulfonyl)-L-valinamide
CAS No. 438003-89-5
项目整合开发状态: Preclinical
项目研究机构: Senju (Originator) 参考文献标题:Exploration of peptidyl hydrazones as water-soluble calpain inhibitors
文献作者:Nakamura,M.; Inoue,J.
参考来源:Bioorg Med Chem Lett 2002,12(12),1603

新产品编号:826313

Chemical Name: 1-(3-Fluoronaphthalen-2-yl)-3-methyl-N-(2'-sulfamoylbiphenyl-4-yl)-1H-pyrazole-5-carboxamide
CAS No. 330801-94-0
项目整合开发状态: Preclinical
项目研究机构: Millennium (Originator)
合成路线:3...
参考文献标题:Benzamides and related inhibitors of factor Xa
文献作者:Wang,L.; Zhu,B.-Y.; Li,W.; Zhang,P.; Huang,W.; Song,Y.; Goldman,E.; Zuckett,J.; Scarborough,R.(Millennium Pharmaceuticals,Inc.)
参考来源:EP 1216228; EP 1216231; WO 0119788; WO 0119798

新产品编号:824731

Chemical Name: trans-1-[4-(4-Methylpiperazin-1-yl)cyclohexyl]-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine
CAS No. 330786-01-1, 330786-02-2 (maleate), 330792-60-4 (stereoisomer), 330786-...
参考文献标题:Pyrazolopyrimidines as therapeutic agents
文献作者:Hirst,G.C.; Rafferty,P.; Ritter,K.; Arnold,L.D.; Wishart,N.; Calderwood,D.; Friedman,M.M.(BASF AG)
参考来源:EP 1212327; WO 0119829

新产品编号:902249

Chemical Name: cis-2-[3,5-Bis(trifluoromethyl)phenyl]-N-[4-(2-oxa-8-azaspiro[4.5]dec-8-yl)-1-phenylcyclohexyl]propionamide
CAS No. 374791-95-4, 374791-96-5 (stereoisomer)
项目整合开发状态: Preclinical 参考文献标题:Cyclohexane derivs.and their use as therapeutic agents
文献作者:Elliott,J.M.; Castro Pineiro,J.L.; Swain,C.J.; Hollingworth,G.J.; Dinnell,K.; Shaw,D.E.(Merck Sharp & Dohme Ltd.)
参考来源:WO 0187838

新产品编号:695007

Chemical Name: L-Tyrosyl-D-penicillaminyl-glycyl-L-phenylalanyl-D-cysteine cyclic (2-5)-thioether; (3S,6S,12S)-6-Benzyl-13,13-dimethyl-5,8,11-trioxo-12-(L-tyrosylamino)-1-thia-4,7,10-triazacyclotridec...
参考文献标题:Synthesis and biological activities of cyclic lanthionine enkephalin analogues: delta-Opioid receptor selective ligands
文献作者:Rew,Y.; Malkmus,S.; Svensson,C.; Yaksh,T.L.; Chung,N.N.; Schiller,P.W.; Cassel,J.A.; DeHaven,R.; Goodman,M.
参考来源:J Med Chem 2002,45(17),3746

GPI-1511

Chemical Name: 1-(3,3-Dimethyl-2-oxopentanoyl)piperidine-2(S)-carbothioic acid S-(3,3-diphenylpropyl) ester
CAS No. 252770-39-1, 205388-57-4 (undefined stereoch.)
项目整合开发状态: Preclinical
项目研究机构...
参考文献标题:Synthesis of N-glyoxyl prolyl and pipecolyl amides and thioesters and evaluation of their in vitro and in vivo nerve regenerative effects
文献作者:Hamilton,G.S.; Wu,Y.-Q.; Limburg,D.C.; Wilkinson,D.E.; Vaal ,M.J.; Li,J.-H.; Thomas,C.; Huang,W.; Sauer,H.; Ross,D.T.; Soni,R.; Chen,Y.; Guo,H.; Howorth,P.; Valentine,H.; Liang,S.; Spicer,D.; Fuller,M.; Steiner,J.P
参考来源:J Med Chem 2002,45(16),3549

TT-24

Chemical Name: Mixture of 2-bromo-3-methoxy-6-(methylamino)-1,4,5,8,9,10-hexahydro-9,10[1',2']-benzenoanthracene-1,4,5,8-tetraone and 2-bromo-3-methoxy-7-(methylamino)-1,4,5,8,9,10-hexahydro-9,10[1',2...
参考文献标题:Triptycene analogs
文献作者:Hua,D.H.; Perchellet,J.-P.(Kansas State University)
参考来源:WO 0228808