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

Deramciclane fumarate, EGIS-3886, EGYT-3886

N,N-二甲基-2-[[(1R,2R,4R)-1,7,7-三甲基-2-苯基二环[2.2.1]庚-2-基]氧基]乙胺富马酸盐德伦环烷Chemical Name: (1R,2S,4R)-(-)-N,N-Dimethyl-2-[(1,7,7-trimethyl-2-phenylbicyclo[2.2.1]hept-2-yl)oxy]ethanamine 2(E)-butenedioate (1:1);...
参考文献标题:Basic ethers and pharmaceutical compsns.containing the same
文献作者:Budai,Z.; Magdanyi,L.; Lay,A.; Mezei,T.; Grasser,K.; Pet鯿z,L.; Kosoczky,I.(Egis Pharmaceuticals Ltd.)
参考来源:US 4342762

E-6039, E-6006 citrate

N,N-二甲基-N-[2-[1-(1-甲基-1H-吡氮醇-5-基)-1-(2-哧基)甲氧基]乙基]胺柠檬酸盐Chemical Name: N,N-Dimethyl-N-[2-[1-(1-methyl-1H-pyrazol-5-yl)-1-(2-thienyl)methoxy]ethyl]amine citrate
CAS No. 247046-64-6, 247046-62-4 (free ...
参考文献标题:Thienylazolylalcoxyethanamines,their preparation and their application as medicaments
文献作者:Frigola-Constansa,J.; Andaluz-Mataro,B.; Merce-Vidal,R.(Laboratorios del Dr.Esteve,SA)
参考来源:WO 9952525

Dimethynur

N,N'-二甲基亚硝基脲Chemical Name: 1,3-Dimethyl-1-nitrosourea
CAS No. 13256-32-1
项目整合开发状态: Phase I
项目研究机构: Inst. Khim. Fiz. Akad. Nauk (Originator)
合成路线:By nitrosation of symmetrical dimethylurea ...
参考文献标题:DIMETHYNUR
文献作者:Ostrovskaya,L.A.
参考来源:Drugs Fut 1989,14(11),1038

DIBA-4, NSC-672594, CI-1013, PD-159206

N,N'-二硫代二(2,1-亚苯基)二(羰基)二(L-异亮氨酸)Chemical Name: N,N'-Dithiobis(2,1-phenylene)bis(carbonyl)bis(L-isoleucine)
CAS No. 171744-42-6
项目整合开发状态: Phase I
项目研究机构: Pfizer (Originator)
合成路线:The protec...
参考文献标题:Development and pilot-scale demonstration of a process for inhibitors of the HIV nucleocapsid protein,NCp7
文献作者:Fiore,P.J.; et al.
参考来源:Org Process Res Dev 1998,2(3),151

Hexamethylenebisacetamide, HMBA, NSC-95580, Hexabid

N,N'-六亚甲基双乙酰胺Chemical Name: N,N'-Hexamethylenebisacetamide
CAS No. 3073-59-4
项目整合开发状态: Phase II
项目研究机构: National Cancer Institute (Originator), Memorial Sloan-Kettering Cancer Center (License...
参考文献标题:Preparation of polyacetylalkylenediamines
文献作者:Grimmelikhuysen,J.; Schroeder,A.(Unilever NV)
参考来源:BE 769655; DE 2133458; FR 2100320; GB 1335204

EUK-189

N,N'-双(3-乙氧基亚水杨基)-1,2-乙二胺-锰(II)Chemical Name: (SP-5-13)-(Acetato-kappaO)[[2,2'-[1,2-ethanediylbis[(nitrilo-kappaN)methylidyne]]bis[6-ethoxyphenolato-kappaO1]](2-)]manganese
CAS No. 186350-27-6
项...
参考文献标题:Synthetic catalytic free radical scavengers useful as antioxidants for prevention and therapy of disease
文献作者:Malfroy-Camine,B.; Doctrow,S.R.(Eukarion,Inc.)
参考来源:JP 1999507646; US 5696109; WO 9640148; WO 9640149

SL-11047

N,N'-双[3-(乙氨基)丙基]-2(Z)-丁烯-1,4-二胺四盐酸盐Chemical Name: N,N'-Bis[3-(ethylamino)propyl]-2(Z)-butene-1,4-diamine tetrahydrochloride
CAS No. 206991-64-2, 308145-19-9 (free base)
项目整合开发状态: Phase I/II
...
参考文献标题:Conformationally restricted polyamines
文献作者:Witiak,D.T.; Frydman,B.J.; Marton,L.J.; Reddy,V.K.; Valasinas,A.L.(Wisconsin Alumni Research Foundation)
参考来源:US 5889061

D-threo-PDPP

N-[(1R,2R)-2-羟基-2-苯基-1-(1-吡咯烷甲基)乙基]-癸酰胺Chemical Name: (R,R)-N-[2-Hydroxy-2-phenyl-1-(1-pyrrolidinylmethyl)ethyl]decanamide
CAS No. 193545-89-0
项目整合开发状态: Biological Testing
项目研究机构: Seikagaku (...
参考文献标题:Amino alcohol deriv.and method for preparing the
文献作者:Oyamada,H.; Inokuchi,J.; Jinbo,M.(Seikagaku Corp.)
参考来源:EP 0782992

BW-540C

N-[(1-甲基-5-苯基-2,3-二氢-1H-1,4-苯并二氮卓-2-基)甲基]苯酰胺二盐酸Chemical Name: 4,5-Dihydro-N-methyl-1-[3-(trifluoromethyl)phenyl]-1H-pyrazol-3-amine; 3-Methylamino-1-[3-(trifluoromethyl)phenyl]-2-pyrazoline; 3-Methyla...
参考文献标题:Pyrazoline derivates,processes for their preparation and pharmaceutical formulations containing them
文献作者:Copp,F.C.; Caldwell,A.G.; Collard,D.(Glaxo Wellcome plc)
参考来源:DE 3149710; EP 0055418; FR 2496100; GB 2093832

Gludapcin, FK-156

N-[(2R)-2-羟基-1-氧代丙基]-L-丙氨酰-D-gamma-谷氨酰-(6R)-6-羧基-L-赖氨酰-甘氨酸Chemical Name: D-Lactyl-L-alanyl-gamma-D-glutamyl-(L)-meso-diaminopimelyl-(L)-glycine; (R)-N-(2-Hydroxy-1-oxopropyl)-L-alanyl-D-gamma-glutamyl...
参考文献标题:New lactyl tetrapeptide,processes for preparation thereof and pharmaceutical compsns.containing it
文献作者:Kitaura,Y.; Nakaguchi,O.; Hemmi,K.(Fujisawa Pharmaceutical Co.,Ltd.)
参考来源:EP 0011283