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

FCE-20700

甲基(5Z,15S,16S)-15-羟基-16-甲基-9-氧代前列腺-5-烯-13-炔-1-酸酯Chemical Name: (Z)-7-[(1R,2S)-[(3S,4S)-3-Hydroxy-4-methyloct-1-y-nyl]-5-oxocyclopentyl]-5-heptenoic acid methyl es-ter
CAS No. 89648-76-0
项目整合开发状态...
参考文献标题:13,14-Dehydro-11-deoxy-prostaglandins and process for their preparation
文献作者:Gandolfi,C.; Pellegata,R.Fumagalli,A.(Pharmacia & Upjohn SpA)
参考来源:US 4293705

NNC-63-0532

甲基[8-(2-萘基甲基)-4-氧代-1-苯基-1,3,8-三氮杂螺[4.5]癸-3-基]乙酸酯Chemical Name: 2-[8-(1-Naphthylmethyl)-4-oxo-1-phenyl-1,3,8-triazaspiro[4.5]dec-3-yl]acetic acid methyl ester
CAS No. 250685-44-0
项目整合开发状态: Precli...
参考文献标题:Novel 1,3,8-triazaspiro[4.5]decanones with high affinity for opioid receptor subtypes
文献作者:Watson,B.; Thomsen,C.; Hohlweg,R.(Novo Nordisk A/S)
参考来源:EP 1080091; WO 9959997

Laniquidar, R-101933

甲基11-[1-[2-[4-(喹啉-2-甲氧基)苯基]乙基,哌啶-4-酰胺]-5,6-二氢亚咪唑[2,1-b][3]苯甲西泮-3-羧酸盐Chemical Name: 11-[1-[2-[4-(2-Quinolylmethoxy)phenyl]ethyl]piperidin-4-ylidene]-6,11-dihydro-5H-imidazo[2,1-b][3]benzazepine-3-carbo...
参考文献标题:Fused imidazole derivs.as multidrug resistance modulators
文献作者:Janssens,F.E.; Leenaerts,J.E.; Sommen,F.M.; Surleraux,D.L.N.G.(Janssen Pharmaceutica NV)
参考来源:EP 0888352; JP 2000505477; US 6218381; WO 9734897

ONO-4819.CD, ONO-4819

甲基4-({2-[(1R,2R,3S)-3-羟基-2-{(1E)-3-羟基-4-[3-(甲氧基甲基)苯基]-1-丁烯-1-基}-5-氧代环戊基]乙基}硫基)丁酸酯Chemical Name: 11alpha,15alpha-Dihydroxy-16-(3-methoxymethylphenyl)-9-oxo-17,18,19,20-tetranor-5-thia-13(E)-prostenoic ...
参考文献标题:5-Thia-omega-substd.phenyl-prostaglandin E derivs.,process for producing the same and drugs containing the same as the active ingredient
文献作者:Ohuchida,S.; Maruyama,T.(Ono Pharmaceutical Co.,Ltd.)
参考来源:EP 1097922; JP 2001089444; US 6462081; WO 0003980

CV-159

甲基6-[(5-苯基-1H-吡唑-3-基)氧基]己基2,6-二甲基-4-(3-硝基苯基)-1,4-二氢-3,5-吡啶二羧酸酯Chemical Name: 1,4-Dihydro-2,6-dimethyl-4-(3-nitrophenyl)-3,5-pyridinedicarboxylic acid methyl 6-(5-phenyl-3-pyrazolyloxy)hexyl ester; 1,4...
参考文献标题:Novel 1,4-dihydropyridine derivatives
文献作者:Masato,K.; Shinji,T.; Kozo,H.; Susumu,T.(Tokyo Tanabe Co.,Ltd.)
参考来源:DE 3230400; FR 2511370; FR 8214008; GB 2108108; JP 88023193; US 4418197

CDRI-87/144

甲基N-[6-(4-甲基哌啶-1-羰基)-1H-苯并咪唑-2-基]氨基甲酸酯Chemical Name: 5(6)-(4-Methylpiperidin-1-ylcarbonyl)benzimidazole-2-carbamic acid methyl ester
CAS No. 128579-70-4
项目整合开发状态: Preclinical
项目研究机构: Central ...
参考文献标题:5(6)-Benzene ring substd.benzimidazole-2-carbamate derivs.having anthelmintic activity
文献作者:Beard,C.C.(Syntex (USA),Inc.)
参考来源:US 4086235

CDDO-Me, TP-155C

甲基巴多索隆Chemical Name: 2-Cyano-3,12-dioxoolean-1,9(11)-dien-28-oic acid methyl ester; (6aR,6bS,8aR,12aS,14aR,14bS)-11-Cyano-2,2,6a,6b,9,9,12a-heptamethyl-10,14-dioxo-1,3,4,5,6,6a,6b,7,8,8a,9,10,12a,14,1...
参考文献标题:Therapeutic compsns.and methods of use
文献作者:Suh,N.; Gribble,G.W.; Honda,T.; Sporn,M.B.(Dartmouth College)
参考来源:WO 9965478

Methylprednisolone aceponate, SH-440, ZK-91588, Adventan, Advantan

甲基泼尼松龙乙丙酸酯Chemical Name: (6alpha,11beta)-21-Acetoxy-11-hydroxy-6-methyl-17-(propionyloxy)pregna-1,4-diene-3,20-dione
CAS No. 86401-95-8
项目整合开发状态: Launched-1992
项目研究机构: Leiras (Originator), Sc...
参考文献标题:New 6alpha-methylprednisolone derivs.their preparation and use
文献作者:Annen,K.; Petzoldt,K.; Laurent,H.; Wiechert,R.; Hofmeister,H.; Wendt,H.(Schering AG)
参考来源:EP 0072547

Metitepine, Methiothepin, Ro-8-6837(maleate), VUFB-6276(mesylate)

甲替平Chemical Name: (?-10-(4-Methylpiperazin-1-yl)-8-(methylsulfanyl)-10,11-dihydrodibenzo[b,f]thiepin; (?-1-[10,11-Dihydro-8-(methylsulfanyl)dibenzo[b,f]thiepin-10-yl]-4-methylpiperazine
CAS No. 202...
参考文献标题:Metitepine
文献作者:Protiva,M.
参考来源:Drugs Fut 1977,2(4),250

Moxipraquine, 349-C-59

甲氧丙喹Chemical Name: 4-[4-[6-(6-Methoxyquinolin-8-ylamino)hexyl]piperazin-1-yl]butan-2-ol
CAS No. 23790-08-1, 23790-07-0 (triHCl)
项目整合开发状态: Biological Testing
项目研究机构:
合成路线:The reaction of 8...
参考文献标题:Moxipraquine
文献作者:Blancafort,P.; Serradell,M.N.; Castar,J.; Hillier,K.
参考来源:Drugs Fut 1981,6(6),356