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

Bisnafide mesylate, Bisnafide mesilate, NSC-D640430, DMP-840

双奈法德双奈法德 Chemical Name: (R,R)-2,2'-(Ethane-1,2-diyl)bis[imino(1-methylethane-2,1-diyl)]bis(5-nitro-2,3-dihydro-1H-benzo[de]isoquinoline-1,3-dione) dimethanesulfonate; (R,R)-2,2'-(Ethylenediimino)bis(...
参考文献标题:Bis-naphthalimides containing amino-acid derived linkers as anticancer agents
文献作者:Sun,J.-H.(DuPont Pharmaceuticals Co.)
参考来源:EP 0506008; EP 0577753; JP 1994506229; US 5206249; WO 9217453

LY-418426

双环[3.1.0]己烷-2,6-二羧酸,2-氨基-4-氧基-,(1R,2R,5S,6S)-rel-Chemical Name: (1S*,2S*,5R*,6R*)-2-Amino-4-oxobicyclo[3.1.0]hexane-2,6-dicarboxylic acid
CAS No. 215867-19-9
项目整合开发状态: Biological Testing
项目研究...
参考文献标题:Excitatory amino acid receptor modulators
文献作者:Massey,S.M.; Monn,J.A.; Valli,M.J.(Eli Lilly and Company)
参考来源:EP 0878463; US 5958960

Diacetylrhein, Diacerhein, Diacerein, KW-4800, SF-277, Art 50, Fisiodar, Artrodar

双醋瑞因; 二乙酰大黄酸; 二乙酰二氢蒽羧酸Chemical Name: 9,10-Dihydro-4,5-diacetoxy-9,10-dioxo-2-anthracenecarboxylic acid
CAS No. 13739-02-1
项目整合开发状态: Launched-1985
项目研究机构: Gentili (Originator), Proter (Origina...
参考文献标题:SF-277
文献作者:Neuman,M.
参考来源:Drugs Fut 1979,4(6),445

AZP

反式-2,4-二(1-氮丙啶基)-2,2,4,4,6,6-六氢-2,4,6,6-四(甲基氨基)-1,3,5,2,4,6-三氮杂三磷杂苯Chemical Name: trans-2,4-Bis(1-aziridinyl)-2,2,4,4,6,6-hexahydro-2,4,6,6-tetrakis(methylamino)-1,3,5,2,4,6-triazatriphosphorine
CA...
参考文献标题:AZP
文献作者:Eastland,G.
参考来源:Drugs Fut 1988,13(9),815

M-32

反式-9,10-反式-5H,5-(3,4,5-三甲氧基苯甲酰胺基)-2-甲基十氢异喹啉Chemical Name: (4aalpha,5alpha,8abeta)-N-(Decahydro-2-methyl-5-isoquinolinyl)-3,4,5-trimethoxybenzamide; trans-5-(3,4,5-Trimethoxybenzamido)-2-methyldecahydr...
参考文献标题:Benzamido 2 lower alkyl decahydroisoquinolines
文献作者:Mathison,I.W.(Aventis Pharmaceuticals,Inc.)
参考来源:DE 1900948; FR 2004748; GB 1246051; JP 7114060; US 3674791

Eszopiclone, (+)-Zopiclone, (S)-Zopiclone, Estorra

右佐匹克隆 (R)-佐匹克隆 Chemical Name: (+)-6-(5-Chloro-2-pyridyl)-7(S)-(4-methylpiperazin-1-ylcarbonyloxy)-6,7-dihydro-5H-pyrrolo[3,4-b]pyrazin-5-one; (+)-4-Methylpiperazine-1-carboxylic acid 6-(5-chloro-2-pyr...
参考文献标题:Optically active deriv.of 5H-pyrrolo[3,4-b]pyrazine,its preparation and pharmaceutical compsns.containing it
文献作者:Cotrel,C.; Roussel,G.(Aventis Pharma SA)
参考来源:EP 0495717; EP 0609210; FR 2671800; JP 1994504548; WO 9212980

Dexindoprofen

右吲哚洛芬Chemical Name: (+)-4-(1,3-Dihydro-1-oxo-2H-isoindol-2-yl)-alpha-methylbenzeneacetic acid
CAS No. 53086-13-8
项目整合开发状态: Biological Testing
项目研究机构: Pfizer (Originator)
合成路线:It can be obt...
参考文献标题:Indoprofen
文献作者:Castar,J.; Arrigoni,Martelli,E.
参考来源:Drugs Fut 1976,1(5),242

Pemedolac, AY-30715

右培美酸Chemical Name: (?-cis-4-Benzyl-1-ethyl-1,3,4,9-tetrahydropyrano[3,4-b]indole-1-acetic acid
CAS No. 114716-16-4, 114030-45-4 ((-)-cis-isomer), 114030-44-3 ((+)-cis-isomer), 113975-74-9 ((?-trans...
参考文献标题:Substd.1,3,4,9-tetrahydropyrano[3,4-b]indole-1-ac
文献作者:Katz,A.H.; Demerson,C.A.; Humber,L.G.(American Home Products Corp.)
参考来源:EP 0238226; JP 1987221688; US 4670462; US 4775690

Dexloxiglumide, CR-2017

右氯谷胺Chemical Name: (R)-4-(3,4-Dichlorobenzamido)-5-[N-(3-methoxypropyl)-N-pentylamino]-5-oxopentanoic acid; N2-(3,4-Dichlorobenzoyl)-N1-(3-methoxypropyl)-N1-pentyl-D-aspartic acid 1-amide
CAS No. 1...
参考文献标题:Derivs.of (R)-5-pentylamino-5-oxopentanoic acid with anticholecystokinin activity
文献作者:Makovec,F.; Chiste,R.; Peris,W.; Rovati,L.(Rotta Research Laboratorium SpA)
参考来源:EP 0344184; JP 1988201156; US 5130474; US 5391574; WO 8805774

(S)-Sotalol, Dexsotalol, (+)-Sotalol, BMY-05763-1-D(monoHCl), BMY-5763

右索他洛尔甲烷磺酰胺,N-[4-[(1S)-1-羟基-2-[(1-甲基)氨基]乙基]苯,盐酸盐(1:1) Chemical Name: (+)-(S)-N-[4-[1-Hydroxy-2-(isopropylamino)ethyl]phenyl]methanesulfonamide; (+)-(S)-4'-[1-Hydroxy-2-(isopropylamino)ethyl]methanesul...
参考文献标题:Asymmetric synthesis of the antiarrhythmia agent d-sotalol
文献作者:Brodfuehrer,P.R.; et al.
参考来源:Org Process Res Dev 1997,1(2),176