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

NSC-724771, JS-K

4-[(Z)-(2,4-二硝基苯氧基)-氧偶氮基]-1-哌嗪羧酸乙酯Chemical Name: 4-(2,4-Dinitrophenoxy)-NNO-azoxy]piperazine-1-carboxylic acid ethyl ester
CAS No. 205432-12-8
项目整合开发状态: Preclinical
项目研究机构: National Cancer In...
参考文献标题:O2-Arylated or O2-glycosylated 1-substd.diazen-1-ium-1,2-diolates and O2-substd.1-[(2-carboxylato)pyrrolidin-1-yl]diazen-1-ium-1,2-diolates
文献作者:Keefer,L.K.; Saavedra,J.E.; Srinivasan,A.; Rice,W.G.; Bogdan,C.; Ji,X.(US Department of Health & Human Services)
参考来源:JP 2002506421; WO 9813358

L-755507

4-[(己基氨基甲酰)氨基]-N-[4-(2-{[(2S)-2-羟基-3-(4-羟基苯氧基)丙基]氨基}乙基)苯基]苯磺酰胺Chemical Name: 4-(3-Hexylureido)-N-[4-[2-[2(S)-hydroxy-3-(4-hydroxyphenoxy)propylamino]ethyl]phenyl]benzenesulfonamide
CAS No. 159182-4...
参考文献标题:Substd.phenyl sulfonamides as selective beta3 agonists for the treatment of diabetes and obesity
文献作者:Fisher,M.H.; Mathvink,R.J.; Ok,H.O.; Parmee,E.R.; Weber,A.E.(Merck & Co.,Inc.)
参考来源:CA 2114712; EP 0611003; JP 1995010827; US 5451677; WO 9418161

RO-1130830, RS-130830

4-[[[4-(4-氯苯氧基)苯基]磺酰基]甲基]四氢-n-羟基-2H-吡喃-4-羧酰胺Chemical Name: 4-[4-(4-Chlorophenoxy)phenylsulfonylmethyl]tetrahydropyran-4-carbohydroxamic acid; 4-[4-(4-Chlorophenoxy)phenylsulfonylmethyl]-N-hydroxytetra...
参考文献标题:Metalloproteinase inhibitors,pharmaceutical compsns.containing them and their pharmaceutical uses,and methods and intermediates useful for their preparation
文献作者:Zook,S.E.; Dagnino,R.Jr.; Deason,M.E.; Bender,S.L.; Melnick,M.J.(Agouron Pharmaceuticals,Inc.)
参考来源:EP 0874830; JP 2000502330; WO 9720824

CB-300919

4-[[[7-氯-3,4-二氢-3-甲基-2-[(4-甲基-1-哌嗪基)甲基]-4-氧代-6-喹唑啉基]甲基]-2-丙炔-1-基氨基]-N-(3-吡啶基甲基)苯甲酰胺Chemical Name: 4-[N-[7-Chloro-3-methyl-2-(4-methylpiperazin-1-ylmethyl)-4-oxo-3,4-dihydroquinazolin-6-ylmethyl]-N-(2-...
参考文献标题:Anti-cancer dihydroquinazoline derivs.
文献作者:Bavetsias,V.; Jackman,A.; Skelton,L.(Cancer Research Campaign Technology Ltd.)
参考来源:WO 0050417

Reglitazar, PNU-182716, JTT-501

4-[[4-[2-(5-甲基-2-苯基-1,3-恶唑-4-基)乙氧基]苯基]甲基]-1,2-恶唑烷-3,5-二酮Chemical Name: 4-[4-[2-(5-Methyl-2-phenyl-4-oxazolyl)ethoxy]benzyl]isoxazolidine-3,5-dione
CAS No. 170861-63-9
项目整合开发状态: Discontinued
项...
参考文献标题:Isoxazolidinedione deriv.and use thereof
文献作者:Shinkai,H.(Japan Tobacco Inc.)
参考来源:EP 0684242; JP 1996517913; US 5728720; US 6057343; WO 9518125

AG-12286

4-[[4-氨基-5-(2,6-二氟苯甲酰基)-1,3-噻唑-2-基]氨基]苯磺酰胺Chemical Name: 4-[4-Amino-5-(2,6-difluorobenzoyl)thiazol-2-ylamino]benzenesulfonamide
CAS No. 223784-75-6
项目整合开发状态: Biological Testing
项目研究机构: Agouro...
参考文献标题:4-Aminothiazole derivs.,their preparation and their use as inhibitors of cyclin-dependent kinases
文献作者:Yang,Y.; Xiao,W.; Chu,S.S.; Li,L.; Chong,W.K.M.; Duvadie,R.R.(Agouron Pharmaceuticals,Inc.)
参考来源:WO 9921845

YM-17551

4-[[5-[(4-乙酰基-3-羟基-2-丙基苯基)甲基硫烷基]-1,3,4-噻二唑-2-基]硫烷基甲基]苯甲酸Chemical Name: 4-[5-(4-Acetyl-3-hydroxy-2-propylbenzylthio)-1,3,4-thiadiazol-2-ylthiomethyl]benzoic acid
CAS No. 107859-85-8
项目整合开发状态: Pre...
参考文献标题:(Substd.benzyl)thio heterocyclic cpds.having leukotriene-antagonist activity
文献作者:Mase,T.; Murase,K.; Tsuzuki,R.; Tomioka,K.; Hara,H.(Yamanouchi Pharmaceutical Co.,Ltd.)
参考来源:EP 0214732; US 4803211; US 4933348; US 5180730

SM-18163

4-[1-(1,3-苯并二噁唑-5-基羰基)哌啶-4-基]-6-(4-甲氧苄基)嘧啶-2-胺Chemical Name: 4-[1-(1,3-Benzodioxol-5-ylcarbonyl)piperidin-4-yl]-6-(4-methoxybenzyl)pyrimidin-2-amine; 1-[4-[2-Amino-6-(4-methoxybenzyl)pyrimidin-4-yl]pi...
参考文献标题:Piperidinylpyramidine derivs.
文献作者:Fujiwara,N.; Ueda,Y.; Murata,S.; Hirota,F.; Kawakami,H.; Fujita,H.(Sumitomo Pharmaceuticals Co.,Ltd.)
参考来源:EP 0892795; JP 2001511764; US 5948786; WO 9738992

SM-8849

4-[1-(3-氟-4-苯基苯基)乙基]-N-甲基-1,3-噻唑-2-胺Chemical Name: 4-[1-(2-Fluorobiphenyl-4-yl)ethyl]-N-methylthiazole-2-amine; 4-[1-(2-Fluorobiphenyl-4-yl)ethyl]-2-(methylamino)thiazole
CAS No. 113759-19-6
项目整...
参考文献标题:Aminazole derivatives and their production and use
文献作者:Ozato,Y.; Tamura,N.; Masumori,H.; Yamamoto,M.; Kojima,A.; Nishikakau,F.; Kimura,Y.(Sumitomo Pharmaceuticals Co.,Ltd.)
参考来源:EP 0248399; JP 1988152368; JP 1993247014; US 4914112; US 5066666; US 5180731

新产品编号:206169

4-[2-(4-氟苯基)-5-(1-甲基-4-哌啶基)-1H-吡咯-3-基]吡啶Chemical Name: 4-[2-(4-Fluorophenyl)-5-(1-methylpiperidin-4-yl)-1H-pyrrol-3-yl]pyridine
CAS No. 188343-77-3
项目整合开发状态: Preclinical
项目研究机构: Merck & Co. (...
参考文献标题:2-Substd.aryl pyrroles,compsns.containing such cpds.and methods of use
文献作者:De Laszlo,S.E.; Mantlo,N.B.; Ponticello,G.S.; Selnick,H.G.; Liverton,N.J.(Merck & Co.,Inc.)
参考来源:EP 0863757; JP 1999510510; US 5792778; WO 9705877