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

Zatosetron maleate, LY-277359 maleate

扎托司琼 Chemical Name: endo-5-Chloro-2,2-dimethyl-N-(8-methyl-8-azabicyclo[3.2.1]oct-3-yl)-2,3-dihydrobenzofuran-7-carboxamide maleate
CAS No. 123482-23-5, 123482-22-4 (free base)
项目整合开发状态: Phase ...
参考文献标题:Improvements in or relating to specific 5-HT3 antagonists
文献作者:Cohen,M.L.; Lacefield,W.B.(Eli Lilly and Company)
参考来源:AU 8821916; EP 0307172; JP 1989110684

Zalospirone hydrochloride, Wy-47846

扎螺酮 Chemical Name: 3a,4,4a,6a,7,7a-Hexahydro-2-[4-[4-(2-pyrimidinyl)-1-piperazinyl]butyl]-4,7-etheno-1H-cyclobut[f]isoindole-1,3(2H)-dione hydrochloride; endo-(3aalpha,4alpha,4abeta,6abeta,7alpha,7aa...
参考文献标题:Polycyclic aryl- and heteroarylpiperazyl imides as 5-HT1A receptor ligands and potential anxiolytic agents: synthesis and structure-activity relationship studies
文献作者:Abou-Gharbia,M.; et al.
参考来源:J Med Chem 1988,31(7),1382

Toborinone, OPC-18790, Tobonone

托波力农Chemical Name: (?-6-[3-(3,4-Dimethoxybenzylamino)-2-hydroxypropoxy]carbostyril; (?-6-[3-(3,4-Dimethoxybenzylamino)-2-hydroxypropoxy]-1,2-dihydroquinolin-2-one
CAS No. 143343-83-3, 128668-62-2 ...
参考文献标题:Novel positive inotropic agents; synthesis and biological activities of 6-(3-amino-2-hydroxypropoxy)-2(1H)-quinolinone derivatives
文献作者:Fujioka,T.; Teramoto,S.; Mori,T.; Hosokawa,T.; Sumida,T.; Tominaga,M.; Yabuuchi,Y.
参考来源:J Med Chem 1992,35(20),3607-12

Tocofibrate

托考贝特Chemical Name: 2-(4-chlorophenoxy)-2-methylpropionic acid 2,5,7,8-tetramethyl-2-(4,8,12-trimethyltridecyl)-3,4-dihydro-2H-1-benzopyran-6-yl ester
CAS No. 50465-39-9
项目整合开发状态: Not Determined...
参考文献标题:
文献作者:Shindo,H.; et al.
参考来源:CH 576970; DE 2304941; FR 2181702; JP 7618954; US 3869477

Tonazocine mesylate, Win-421562

托那佐辛 Chemical Name: (?-(2alpha,6alpha,11S*)-1-(1,2,3,4,5,6-Hexahydro-8-hydroxy-3,6,11-trimethyl-2,6-methano-3-benzazocin-11-yl)-3-octanone methanesulfonate (salt); (?-1-[(2R*,6S*,11S*)]-1,2,3,4,5,6-H...
参考文献标题:Tonazocine mesylate
文献作者:Castar,J.; Serradell,M.N.
参考来源:Drugs Fut 1984,9(11),844

Tonabersat, SB-220453

托那博沙Chemical Name: (-)-(3S,4S)-cis-N-(6-Acetyl-3-hydroxy-2,2-dimethyl-3,4-dihydro-2H-1-benzopyran-4-yl)-3-chloro-4-fluorobenzamide; (-)-cis-6-acetyl-4(S)-(3-chloro-4-fluorobenzamido)-3,4-dihydro-2,2-...
参考文献标题:Bicyclic cpds.with pharmaceutical activity
文献作者:Thompson,M.; Evans,J.M.; Upton,N.; Chan,W.N.; Vong,K.K.; Willette,R.N.(SmithKline Beecham plc)
参考来源:EP 0673373; JP 1996505132; US 5908860; WO 9413656

Zetidoline, DL-308

折替多林Chemical Name: 1-(3-Chlorophenyl)-3-[2-(3,3-dimethyl-1-azetidinyl)ethyl]-2-imidazolidinone
CAS No. 51940-78-4
项目整合开发状态: Biological Testing
项目研究机构: Aventis Pharma (Originator), Lepetit (O...
参考文献标题:2-Imidazolidione derivatives
文献作者:Fontanella,L.; Maffii,G.(Lepetit SpA)
参考来源:US 4011238

Lanicemine hydrochloride, AR-R15896AR, FPL-15895AR((-)-enantiomer), FPL-15035AR(racemate), ARL-15896, FPL-15896AR(former code)

拉尼西明 Chemical Name: (+)-(S)-1-Phenyl-2-(2-pyridyl)ethylamine dihydrochloride
CAS No. 153322-06-6, 153322-05-5 (free base)
项目整合开发状态: Phase II
项目研究机构: AstraZeneca (Originator)
合成路线:Addition...
参考文献标题:Enantiomeric 1-phenyl-2-(2-pyridinyl)ethylamine for the treatment of neurodegenerative disorders
文献作者:Griffith,R.C.; Murray,R.J.; Balestra,M.(Celltech Group plc)
参考来源:EP 0633879; JP 2000319259; WO 9320052

TAK-475

拉帕司他Chemical Name: 2-[1-[2-[1-(3-Acetoxy-2,2-dimethylpropyl)-7-chloro-5(S)-(2,3-dimethoxyphenyl)-2-oxo-1,2,3,5-tetrahydro-4,1-benzoxazepin-3(R)-yl]acetyl]piperidin-4-yl]acetic acid
CAS No. 189060-...
参考文献标题:Benzoxazepine cpds.,their production and use as lipid lowering agents
文献作者:Yukimasa,H.; Sugiyama,Y.; Tozawa,R.(Takeda Chemical Industries,Ltd.)
参考来源:EP 0862562; EP 1097928; JP 1997136880; JP 2001097963; US 6110909; US 6613761; WO 9710224

Pravastatin sodium, Eptastatin sodium, SQ-31000, CS-514, Pravaselect, Liplat, Pravachol, Lipostat, Vasten, Selectin, Elisor, Mevalotin

普伐他汀钠普伐他汀 Chemical Name: [1S-[1alpha(betaS*,deltaS*),2alpha,6alpha,8beta(R*),8aalpha]]-1,2,6,7,8,8a-Hexahydro-beta,delta,6-trihydroxy-2-methyl-8-(2-methyl-1-oxobutoxy)-1-naphthaleneheptanoic acid m...
参考文献标题:The synthesis of carbon-14 labeled pravastatin
文献作者:Wallace,M.A.; Dean,D.C.; White,R.F.; Ellsworth,R.L.; Melillo,D.G.; Marks,T.
参考来源:J Label Compd Radiopharm 1993,33(8),697