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

新产品编号:367533

Chemical Name: 4-Nitro-N-[1,2,3-tris(acetyloxy)-5,6,7,9-tetrahydro-10-(methylsulfanyl)-9-oxobenzo[a]heptalen-7(S)-yl]benzamide
CAS No. 205805-09-0
项目整合开发状态: Biological Testing
项目研究机构: Nationa...
参考文献标题:Antitumor agents.185.Synthesis and biological evaluation of tridemethylthiocolchicine analogues as novel topoisomerase II inhibitors
文献作者:Guan,J.; Zhu,X.K.; Tachibana,Y.; Bastow,K.F.; Brossi,A.; Hamel,E.; Lee,K.H.
参考来源:J Med Chem 1998,41(11),1956

JTP-20993

Chemical Name: 2-[4-[2-(5-Methyl-2-phenyl-4-oxazolyl)ethoxy]benzyl]malonic acid dimethyl diester
CAS No. 170861-71-9
项目整合开发状态: Preclinical
项目研究机构: Japan Tobacco (Originator)
合成路线:Acetylati...
参考文献标题:Isoxazolidine-3,5-dione and noncyclic 1,3-dicarbonyl compounds as hypoglycemic agents
文献作者:Shinkai,H.; Onogi,S.; Tanaka,M.; Shibata,T.; Iwao,M.; Wakitani,K.; Uchida,I.
参考来源:J Med Chem 1998,41(11),1927

新产品编号:244137

Chemical Name: 2(R)-[N-Benzyl-N-(4-methoxyphenylsulfonyl)amino]-3(S)-methylpentanohydroxamic acid
CAS No. 192570-27-7
项目整合开发状态: Preclinical
项目研究机构: Novartis (Originator)
合成路线:Condensation ...
参考文献标题:Discovery of CGS 27023A,a non-peptidic,potent,and orally active stromelysin inhibitor that blocks cartilage degradation in rabbits
文献作者:MacPherson,L.J.; Bayburt,E.K.; Capparelli,M.P.; Carroll,B.J.; Goldstein,R.; Justice,M.R.; Zhu,L.; Hu,S.; Melton,R.A.; Fryer,L.; Goldberg,R.L.; Doughty,J.R.; Spirito,S.; Blancuzzi,V.; Wilson,D.M.; O'Byrne,E.M.; Ganu,V.; Parker,D.T.
参考来源:J Med Chem 1997,40(16),2525

新产品编号:388099

Chemical Name: 2(R)-[N-(4-Methoxyphenylsulfonyl)-N-(2-pyridylmethyl)amino]-3-methylbutyrohydroxamic acid
CAS No. 208663-30-3, 161313-61-7 (mono HCl salt)
项目整合开发状态: Preclinical
项目研究机构: Novarti...
参考文献标题:Arylsulfonamido-substd.hydroxamic acids
文献作者:MacPherson,L.J.; Parker,D.T.; Jeng,A.Y.(Novartis Corp.)
参考来源:US 5506242; US 5552419

新产品编号:109667

Chemical Name: [4R-(4alpha,5alpha,6beta,7beta)]--4,7-Dibenzyl-5,6-dihydroxy-1,3-bis[3-[3(5)-pyrazolyl]benzyl]perhydro-1,3-diazepin-2-one
CAS No. 167825-00-5, 167937-41-9 (diHCl)
项目整合开发状态: Precli...
参考文献标题:Cyclic ureas and analogues useful as retroviral protease inhibitors
文献作者:Lam,P.Y.; Eyermann,C.J.; Hodge,C.N.; Jadhav,P.K.; DeLucca,G.V.(DuPont Pharmaceuticals Co.)
参考来源:EP 0607334; EP 0686151; EP 0765873; JP 1995500324; JP 1996509700; US 5610294; WO 9307128; WO 9419329

新产品编号:111249

Chemical Name: [4R-(4alpha,5alpha,6beta,7beta)]-1-(3-Aminobenzyl)-4,7-dibenzyl-5,6-dihydroxy-3-[3-[3(5)-pyrazolyl]benzyl]perhydro-1,3-diazepin-2-one
CAS No. 167825-68-5
项目整合开发状态: Preclinical
...
参考文献标题:Cyclic ureas and analogues useful as retroviral protease inhibitors
文献作者:Lam,P.Y.; Eyermann,C.J.; Hodge,C.N.; Jadhav,P.K.; DeLucca,G.V.(DuPont Pharmaceuticals Co.)
参考来源:EP 0607334; EP 0686151; EP 0765873; JP 1995500324; JP 1996509700; US 5610294; WO 9307128; WO 9419329

F-14679, F-13714

Chemical Name: 1-(3-Chloro-4-fluorobenzoyl)-4-fluoro-4-[5-methyl-6-(methylamino)pyridin-2-ylmethylaminomethyl]piperidine fumarate
CAS No. 208109-39-1, 208109-38-0 (free base)
项目整合开发状态: Preclinic...
参考文献标题:Pyridin-2-yl-methylamine derivs.,method of preparing and application as medicine
文献作者:Vacher,B.; Bonnaud,B.; Koek,W.(Pierre Fabre M閐icament)
参考来源:EP 0946546; JP 2001504129; US 6020345; WO 9822459

Ro-32-6167

Chemical Name: 1-[N-(4-Hydroxysuccinyl)-L-aspartyl-L-glutamyl-L-(2-methyl)phenylalanyl-L-(3-methyl)valyl-L-leucylamino]-3-butenylboronic acid ; N-(3-Carboxypropionyl)-L-aspartyl-L-glutamyl-2-methyl-L-...
参考文献标题:Antiviral peptide derivs.
文献作者:Attwood,M.R.; Hurst,D.N.; Jones,P.S.; Kay,P.B.; Raynham,T.M.; Wilson,F.X.(F.Hoffmann-La Roche AG)
参考来源:JP 2000508344; WO 9822496

S-DABO, HI-280

Chemical Name: 6-Benzyl-5-isopropyl-2-(methylsulfanylmethylsulfanyl)pyrimidin-4(3H)-one
CAS No. 210645-95-7
项目整合开发状态: Preclinical
项目研究机构: Parker Hughes Institute (Originator)
合成路线:The reac...
参考文献标题:Structure-based design of novel dihydroalkoxybenzyloxopyrimidine derivatives as potent nonnucleoside inhibitors of the human immunodeficiency virus reverse transcriptase
文献作者:Sudbeck,E.A.; Mao,C.; Vig,R.; Venkatachalam,T.K.; Tuel-Ahlgren,L.; Uckun,F.M.
参考来源:Antimicrob Agents Chemother 1998,42(12),3225

DW-2143

Chemical Name: 1-[1-(4-Aminobenzoyl)indolin-5-ylsulfonyl]-4-phenylimidazolidin-2-one
CAS No. 210691-35-3
项目整合开发状态: Preclinical
项目研究机构: Dong-Wha (Originator)
合成路线:The bromination of styrene...
参考文献标题:Arylsulfonylimidazolone derivs.as an antitumor agent
文献作者:Yoon,S.J.; Chung,Y.H.; Lee,M.S.; Choi,D.R.; Lee,J.A.; Lee,H.S.; Yun,H.R.; Lee,D.K.; Moon,E.Y.; Hwang,H.S.; Choi,C.H.; Jung,S.H.(Dong-Wha Pharmaceuticals Industry Co.Ltd)
参考来源:EP 1021437; JP 2000505096; US 5929103; WO 9807719