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

Licofelone, ML-3000

利克飞龙Chemical Name: 2-[6-(4-Chlorophenyl)-2,2-dimethyl-7-phenyl-2,3-dihydro-1H-pyrrolizin-5-yl]acetic acid
CAS No. 156897-06-2
项目整合开发状态: Phase III
项目研究机构: EuroAlliance (Originator), Merckle (...
参考文献标题:Method for producing 6-(4-chlorophenyl)-2,2-dimethyl-7-phenyl-2,3-dihydro-1H-pyrrolizine-5-yl acetic acid
文献作者:Laufer,S.; Striegel,H.-G.; Kammermeier,T.; Merckle,P.(Merckle GmbH)
参考来源:US 6417371; WO 0155149

Riodipine, PP-1466, Foridone, Phoridone

利奥地平Chemical Name: 4-[2-(Difluoromethoxy)phenyl]-1,4-dihydro-2,6-dimethyl-3,5-pyridinecarboxylic acid dimethyl ester; Dimethyl 4-[o-(difluoromethoxy)phenyl]-1,4-dihydro-2,6-dimethy-3,5-pyridinedicarb...
参考文献标题:2,6-Dimethyl-3,5-dimethoxycarbonyl-4-(o-difluoromethoxyphenyl)1,4-dihydropyridine
文献作者:Dubur,G.Y.
参考来源:DE 2900537; FR 2414501; GB 2013186; JP 79122280; US 4219653

Linogliride, McN-3935

利诺格列 N-(1-甲基-2-吡咯烷基亚基)-N'-苯基-4-吗啉甲脒富马酸盐 Chemical Name: N-(1-Methyl-2-pyrrolidinylidene)-N'-phenyl-4-morpholinecarboxamidine; N-(1-Methyl-2-pyrrolidinylidene)-N'-phenyl-4-morpholinecarboximidamide
...
参考文献标题:Nitrogen heterocyclic carboximidamide compounds
文献作者:Rasmussen,C.R.(Ortho-McNeil Pharmaceutical,Inc.)
参考来源:US 4211867

Galocitabine, Ro-09-1390

加洛他滨Chemical Name: 5'-Deoxy-5-fluoro-N4-(3,4,5-trimethoxybenzoyl)cytidine; N-[1-(5-Deoxy-beta-D-ribofuranosyl)-5-fluoro-2-oxo-1,2-dihydro-4-pyrimidinyl]-3,4,5-trimethoxybenzamide
CAS No. 124012-42...
参考文献标题:Fluorocytidine derivs.,their preparation and medical preparations containing them
文献作者:Fujiu,M.; Ishitsuka,H.; Miwa,M.; Umeda,I.; Yokose,K.(F.Hoffmann-La Roche AG)
参考来源:AU 8825168; EP 0316704; JP 1989153696; US 4966891

Galamustine hydrochloride, G-6-M, C6-GalM, C6-GLM, C6-Galactose mustard

加莫司汀 Chemical Name: 6-[Bis(2-chloroethyl)amino]-6-deoxy-D-galactopyranose hydrochloride
CAS No. 107811-63-2, 105618-02-8 (free base)
项目整合开发状态: Phase I
项目研究机构: Georgetown University (Originat...
参考文献标题:6-bis-(2-Chloroethyl)amino-6-deoxy-D-galactopyranose hydrochloride: Synthesis,chemical characterization,murine P388 antitumor activity,and bone marrow toxicity
文献作者:Schein,P.S.; Green,D.; Hammer,C.F.; McPherson,E.; Talebian,A.
参考来源:J Pharm Sci 1989,78(11),918-21

Piquindone((-)-enantiomer), Ro-221319

匹喹酮 Chemical Name: (-)-2,6-Dimethyl-3-ethyl-4,4a,5,6,7,8,8a,9-octahydro-4a,8a-trans-1H-pyrrolo[2,3-g]isoquinolin-4-one; trans-(-)-3-Ethyl-1,4a,5,6,7,8,8a,9-octahydro-2,6-dimethyl-4H-pyrrolo[2,3-g]iso...
参考文献标题:Isoquinoline derivs.,process for their preparation,intermediates and pharmaceutical compsns.containing them
文献作者:Berger,L.; Olson,G.L.(F.Hoffmann-La Roche AG)
参考来源:EP 0010661

Pixantrone maleate, BBR-2778

匹杉琼Chemical Name: 6,9-Bis(2-aminoethylamino)-5,10-dihydrobenz[g]isoquinoline-5,10-dione dimaleate
CAS No. 144510-96-3 (free base)
项目整合开发状态: Phase III
项目研究机构: Cell Therapeutics (Originator) 参考文献标题:6,9-Bis(substd.-amino)benzo-[g]isoquinoline-5,10-diones
文献作者:Krapcho,P.A.(University of Vermont)
参考来源:EP 0503537; EP 0575526; JP 1994511230; WO 9215300

Carocainide hydrochloride, MD-770207

卡罗卡尼 Chemical Name: N-[4,7-Dimethoxy-6-[2-(1-pyrrolidinyl)ethoxy]-5-benzofuranyl]-N'-methylurea hydrochloride; 4,7-Dimethoxy-5-N-methylcarbamoylamino-6-[2-(N-pyrrolidino)ethoxy]benzofuran hydrochlori...
参考文献标题:Carocainide Hydrochloride
文献作者:Ancher,J.F.
参考来源:Drugs Fut 1984,9(6),410

Divalproex sodium, Valproate semisodium, Abbott-50711, Cereb, Epival, Depakote, D閜akine Chrono

双丙戊酸钠Chemical Name: 2-Propylpentanoic acid sodium salt (2:1)
CAS No. 76584-70-8
项目整合开发状态: Launched-1983
项目研究机构: Abbott (Originator), Andrx (Not Determined), National Institute of Child Healt...
参考文献标题:Process for preparing an acetonitrile deriv.
文献作者:Chignac,M.; Grain,C.; Pigerol,C.(Labaz)
参考来源:GB 1522450

Stiripentol, BCX-2600

司替戊醇Chemical Name: 4,4-Dimethyl-1-[(3,4-methylenedioxy)phenyl]-1-penten-3-ol; 1-(1,3-Benzodioxol-5-yl)-4,4-dimethyl-1-penten-3-ol
CAS No. 49763-96-4
项目整合开发状态: Phase II
项目研究机构: Biocodex (Orph...
参考文献标题:Stiripentol
文献作者:Castar,J.; Hillier,K.
参考来源:Drugs Fut 1980,5(8),413