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

Levofolinate calcium, Levoleucovorin calcium, Isovorin

左亚叶酸钙Chemical Name: N-[4-[2-Amino-5-formyl-4-oxo-1,4,5,6,7,8-hexahydropteridin-6(S)-ylmethylamino]benzoyl]-L-glutamic acid calcium salt (1:1)
CAS No. 80433-71-2
项目整合开发状态: Launched-1999
项目研究机构...
参考文献标题:Process for separation of folinic acids
文献作者:Mueller,H.R.; Ulmann,M.; Conti,J.; Muerdel,G.
参考来源:WO 8808844

(-)-Bupivacaine hydrochloride, Levobupivacaine hydrochloride, Chirocaine

左布比卡因Chemical Name: (-)-(S)-1-Butyl-N-(2,6-dimethylphenyl)piperidine-2-carboxamide hydrochloride; (-)-(S)-1-Butyl-2',6'-pipecoloxylidide hydrochloride
CAS No. 27262-47-1 (free base)
项目整合开发状态: La...
参考文献标题:The manufacture of levo-bupivacaine and analogues thereof from L-lysine
文献作者:Hutton,G.E.(Celltech Chiroscience plc)
参考来源:WO 9611181

Levobetaxolol hydrochloride, AL-1577A, Betaxon

左旋倍他洛尔Chemical Name: (S)-1-[4-[2-(Cyclopropylmethoxy)ethyl]phenoxy]-3-[(1-methylethyl)amino]-2-propanol hydrochloride; (-)-(S)-1-[p-[2-(Cyclopropylmethoxy)ethyl]phenoxy]-3-(isopropylamino)-2-propanol ...
参考文献标题:Stereoselective process and chiral intermediates for aryloxydropanolamines
文献作者:Kitteringham,J.; Mitchell,M.B.(GlaxoSmithKline plc)
参考来源:WO 8606368

Levocabastine hydrochloride, R-50547, Livostin, Livocab, Levophta, Levocon, Livostin Nasal Spray

左旋多巴左卡巴司丁 Chemical Name: (-)-[1(cis),3alpha,4beta]-1-[4-Cyano-4-(4-fluorophenyl)cyclohexyl]-3-methyl-4-phenyl-4-piperidinecarboxylic acid monohydrochloride; (-)-trans-1-[cis-4-Cyano-4-(4-fluorophenyl...
参考文献标题:Process for obtaining a 4-amino-5-chloro-2-methoxybenzoic acid deriv.
文献作者:Izquierdo Sanjos? M.; Mart韓 Escudero,U.
参考来源:ES 2002640

R-1270, ICN-17261, Levovirin

左旋韦林Chemical Name: 1-(beta-L-Ribofuranosyl)-1H-1,2,4-triazole-3-carboxamide
CAS No. 206269-27-4
项目整合开发状态: Discontinued
项目研究机构: Ribapharm (Originator), Roche (Licensee)
合成路线:Treatment of L-...
参考文献标题:Monocyclic L-nucleosides,analogs and uses thereof
文献作者:Ramasamy,K.; Averett,D.; Tam,R.(ICN Pharmaceuticals,Inc.)
参考来源:EP 1027359; WO 9816186

Levofloxacin, HR-355, RWJ-25213, DR-3355, Iquix, Oftaquix, Quixin, Tavanic, Levaquin, Floxacin, Cravit

左氧氟沙星左氧氟沙星半水合物 Chemical Name: (S)-(-)-9-Fluoro-3-methyl-10-(4-methyl-1-piperazinyl)-7-oxo-2,3-dihydro-7H-pyrido[1,2,3-de]-1,4-benzoxazine-6-carboxylic acid
CAS No. 100986-85-4, 138199-71-0 (hemihy...
参考文献标题:Pure enantiomeric 1,8-bridged-4-quinolo-3-carboxylic acids,process for their preparation and medicaments containing them,and their use in the preparation of medicaments
文献作者:Bhagen,H.; Stoltefuss,J.; Berschauer,F.; De Jong,A.; Scheer,M.(Bayer AG)
参考来源:DE 3543513; EP 0225552; JP 1987145088

Levodropropizine, Levdropropizine, DF-526, Salvituss, Danka, Rapitux, Levotuss

左羟丙哌嗪左羟丙哌嗪 Chemical Name: (-)-(S)-3-(4-Phenyl-1-piperazinyl)propane-1,2-diol
CAS No. 99291-25-5, 99291-24-4 ((R)-isomer)
项目整合开发状态: Launched-1989
项目研究机构: Domp?(Originator), Almirall Prodesfar...
参考文献标题:Optically active compounds with antitussive and central sedative activity,a process for the preparation thereof and compositions containing the same
文献作者:Borsa,M.; Tonon,G.; Malandrino,S.(Domp?Farm.SpA)
参考来源:EP 0147847; US 4699911; US 4764515

Levosimendan, (-)-OR-1259, Simdax

左西孟旦左西孟旦 Chemical Name: (R)-(-)-2-[4-(4-Methyl-6-oxo-1,4,5,6-tetrahydropyridazin-3-yl)phenylhydrazono]propanedinitrile; (R)-(-)-2-[4-(4-Methyl-6-oxo-1,4,5,6-tetrahydropyridazin-3-yl)phenylhydrazono]m...
参考文献标题:Heterocyclic cpds.
文献作者:Haikala,H.O.; Nore,P.T.; Honkanen,E.J.; Pystynen,J.J.; L鰊nberg,K.K.; Luiro,A.M.; Pippuri,A.K.(Orion Corporation)
参考来源:EP 0383449; JP 1990288868; US 5019575; US 5122524; US 5185332

Batabulin sodium, T-67(free acid), Tl-138067(free acid), TL-138067(free acid), T-138067(free acid)

巴他布林酸钠Chemical Name: 2,3,4,5,6-Pentafluoro-N-(3-fluoro-4-methoxyphenyl)benzenesulfonamide sodium salt
CAS No. 195533-98-3, 195533-53-0 (free acid), 195533-97-2 (K salt), 202998-72-9 (tritium labele...
参考文献标题:Pentafluorobenzenesulfonamides and analogs
文献作者:Rosen,T.; Medina,J.C.; Flygare,J.; Shan,B.; Clark,D.(Tularik Inc.)
参考来源:EP 0896533; JP 2000505459; US 5880151; WO 9730677

Bazinaprine, SR-95191

巴嗪普令Chemical Name: 3-[(2-Morpholinoethyl)amino]-6-phenyl-4-pyridazinecarbonitrile
CAS No. 94011-82-2
项目整合开发状态: Phase I
项目研究机构: Sanofi-Aventis (Originator)
合成路线:The reaction of 3-chloro-4-c...
参考文献标题:SR-95191
文献作者:Eastland,G.Jr.
参考来源:Drugs Fut 1987,12(2),137