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

RS-86

2-乙基-8-甲基-2,8-二氮杂螺[4.5]-1,3-癸二酮Chemical Name: 2-Ethyl-8-methyl-2,8-diazaspiro[4.5]decane-1,3-dione hydrobromide; Spiro(1-methyl-4-piperidyl)-(N-ethylsuccinimide) hydrobromide
CAS No. 3576-73-6 (fr...
参考文献标题:Improvements in or relating to Spiropiperidyl-Succinimide Derivatives
文献作者:Br黶chweiler,C.; Schereier,E.; S黣s,R.; Winkler,H.
参考来源:CH 411895; CH 449628; GB 1041015

NSC-678516, FM-ara-U, FMAU

2'-氟-5-甲基阿拉伯糖基尿嘧啶Chemical Name: 1-(2-Deoxy-2-fluoro-beta-D-arabinofuranosyl)thymine; 2'-Deoxy-2'-fluoro-5-methylarauridine; 2'-Deoxy-2'-fluoro-5-methyl-1-beta-D-arabinosyluracil; 1-(2-Deoxy-2-fluoro-...
参考文献标题:FMAU
文献作者:Lopez,C.
参考来源:Drugs Fut 1985,10(4),288

SK&F-105685

2-氮杂螺[4.5]十烷-2-丙氨酸,N,N-二甲基-8,8-二丙基- Chemical Name: N,N-Dimethyl-8,8-dipropyl-2-azaspiro[4.5]decane-2-propanamine dihydrochloride; 2-[3-(Dimethylamino)propyl]-8,8-dipropyl-2-azaspiro[4.5]decane dihydr...
参考文献标题:SK&F-105685
文献作者:Schwartz,D.A.; Badger,A.M.
参考来源:Drugs Fut 1991,16(9),815

DL-262

3-(1,2-二苯基乙基)-1,2,5,6-四氢-1,2,4-三嗪 Chemical Name: 3-(1,2-Diphenylethyl)-1,4,5,6-tetrahydro-1,2,4-triazine hydrochloride
CAS No. 24638-35-5, 21038-20-0 (free base)
项目整合开发状态: Biological Testing 参考文献标题:DL - 262
文献作者:Castar,J.; Hillier,K.
参考来源:Drugs Fut 1979,4(3),196

Enzastaurin hydrochloride, LY-317615.2HCl, 317615.2HCl

3-(1-甲基-1H-吲哚-3-基)-4-[1-[1-(2-吡啶甲基)-4-哌啶基]-1H-吲哚-3-基]-1H-吡咯-2,5-二酮二盐酸盐恩扎妥林Chemical Name: 3-(1-Methyl-1H-indol-3-yl)-4-[1-[1-(pyridin-2-ylmethyl)piperidin-4-yl]-1H-indol-3-yl]-1H-pyrrole-2,5-dione di...
参考文献标题:Protein kinase C inhibitors
文献作者:Heath,W.F.H.Jr.; McDonald,J.H.III; Paal,M.; Rher,G.; Schotten,T.; Stenzel,W.(Eli Lilly and Company)
参考来源:EP 0817627; JP 1997507066; US 5545636; WO 9517182

EMD-23448

3-(4-(4-苯基-1,2,3,6-四氢-1-吡啶基)丁基)吲哚盐酸盐 Chemical Name: 3-[4-(4-Phenyl-1,2,3,6-tetrahydro-1-pyridyl)butyl]indole; 3-[4-(4-Phenyl-3,4-dehydro-1-piperidyl)butyl]indole; 3-[4-(3,6-Dihydro-4-phenyl-1(2H)-pyr...
参考文献标题:EMD-23,448
文献作者:Blancafort,P.; Hillier,K.; Serradell,M.N.; Castar,J.
参考来源:Drugs Fut 1983,8(5),400

WP-631

3,3'-(1,4-亚苯基二(亚甲基亚氨基))二((1S,3S)-3-乙酰基-1,2,3,4,6,11-六氢-3,5,12-三羟基-10-甲氧基-6,11-二氧代-1-并四苯基2,3,6-三脱氧-alpha-L-来苏-吡喃己糖苷 Chemical Name: N,N'-Phenylenebis(methylene)bis(daunomycin) dihydrochloride
CAS No...
参考文献标题:Bis-anthracyclines with high activity against doxorubicin resistant tumors
文献作者:Priebe,W.; Chaires,J.B.; Przewloka,T.; Fokt,I.; Perez-Soler,R.
参考来源:EP 0971716; JP 2000506899; WO 9734612

Delucemine hydrochloride, NPS-1506

3,3-二(3-氟苯基)-N-甲基-丙-1-胺 Chemical Name: N-[3,3-Bis(3-fluorophenyl)propyl]-N-methylamine hydrochloride
CAS No. 186495-99-8, 186495-49-8 (free base)
项目整合开发状态: Phase I
项目研究机构: NPS Pharmaceutical...
参考文献标题:Cpds.active at a novel site on receptor-operated calcium channels useful for treatment of neurological disorders and diseases
文献作者:Moe,S.T.; Mueller,A.L.; Vanwagenen,B.C.; Barmore,R.M.; Delmar,E.G.; Artman,L.D.; Balandrin,M.F.; Smith,D.L.(NPS Pharmaceuticals,Inc.)
参考来源:WO 9746511

Glutapyrone

3,5-吡啶二羧酸,4-[[[(1S)-1,3-二羧丙基]氨基]-1,4-二氢-2,6-二甲基-,3,5-二乙基酯,二钠盐 Chemical Name: 4-[N-[1(S),3-Dicarboxypropyl]carbamoyl]-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylic acid diethyl ester disodium salt...
参考文献标题:2-(2,6-Dimethyl-3,5-diethoxycarbonyl-1,4-dihydropyridine-4-carboxamide) glutaric acid its disodium salt and method of their preparation
文献作者:Biseniex,E.A.; Uldrikis,Y.R.; Dubur,G.Y.; Veveris,M.M.; Kimenis,A.A.; Ivanov,E.V.(Latvian Institute of Organic Synthesis)
参考来源:US 4485239

AZD-0947, ZD-0947

3-[(4S)-5-氧代-2-(三氟甲基)-1,4,5,6,7,8-六氢喹啉-4-基]苯甲腈Chemical Name: (-)-3-[5-Oxo-2-(trifluoromethyl)-1,4,5,6,7,8-hexahydroquinolin-4(S)-yl]benzonitrile
CAS No. 172649-40-0, 159208-31-8 (undefined stereoc...
参考文献标题:Quinolone and acridinone derivs.for the treatment of urinary incontinence
文献作者:Ohnmacht,C.J.; Trainor,D.A.; Forst,J.M.; Stein,M.M.; Harris,R.J.(AstraZeneca plc)
参考来源:EP 0665834; JP 1996502282; US 5622964; WO 9408966