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

Cipamfylline, HEP-688, BRL-61063

西潘茶碱Chemical Name: 8-Amino-1,3-bis(cyclopropylmethyl)xanthine
CAS No. 132210-43-6
项目整合开发状态: Phase II
项目研究机构: GlaxoSmithKline (Originator), Leo (Licensee)
合成路线:N,N'-Bis(cyclopropylmethyl)ur...
参考文献标题:Xanthine derivs.,process for their preparation and their pharmaceutical use
文献作者:Maschler,H.; Spicer,B.A.; Smith,H.(GlaxoSmithKline plc)
参考来源:AU 9052083; EP 0389282; EP 1120417; JP 1990273676; US 5734051; US 5981535; US 6180791; US 6531600

Sinitrodil, ITF-296

西硝地尔Chemical Name: 3-[2-(Nitrooxy)ethyl]-2H-1,3-benzoxazin-4(3H)-one
CAS No. 143248-63-9
项目整合开发状态: Phase II
项目研究机构: Italfarmaco (Originator)
合成路线:Sinitrodil (ITF-296) is obtained in four m...
参考文献标题:Synthesis and cardiovascular activity of 3-nitrooxyalkyl-2,3-dihydro-4H-1,3-benzoxazin-4-ones,a novel class of nitrate esters
文献作者:Levi,S.; Benedini,F.; Bertolini,G.; et al.
参考来源:12th Int Symp Med Chem (Sept 13-17,Basel) 1992,Abst P152C

Rivastatin, Cerivastatin sodium, Bay-w-6228, Certa, Baycol, Lipobay(free acid)

西立伐他汀钠西立伐他汀 Chemical Name: (+)-(3R,5S,6E)-7-[4-(4-Fluorophenyl)-2,6-diisopropyl-5-(methoxymethyl)pyridin-3-yl]-3,5-dihydroxy-6-heptenoic acid monosodium salt
CAS No. 143201-11-0, 145599-86-6 (fre...
参考文献标题:Substituted pyridines
文献作者:Angerbauer,R.; Fey,P.; H黚sch,W.; Philipps,T.; Bischoff,H.; Petzinna,D.; Schmidt,D.; Thomas,G.(Bayer AG)
参考来源:AU 8928617; EP 0325130; JP 1989216974; US 5006530; US 5169857

Ceronapril, Ceranapril, SQ-29852, Novopril

西罗普利Chemical Name: N-[(S)-6-Amino-2-[hydroxy(4-phenylbutyl)phosphinyloxy]-1-oxohexyl]-L-proline; 1-[(2S)-6-Amino-2-hydroxyhexanoyl]-L-proline hydrogen (4-phenylbutyl)phosphonate ester; N-[(S)-6-Amino-...
参考文献标题:Orally active phosphonyl hydroxyacyl prolines and processes for preparing phosphonyl hydroxyacyl prolines
文献作者:Karanewsky,D.S.; Petrillo,E.W.Jr.(E.R.Squibb & Sons,Inc.)
参考来源:AU 8666133; EP 0229520; JP 1987164691; US 4745196

Temsirolimus, NSC-683864, CCI-779

西罗莫司脂化物Chemical Name: [1R,9S,12S[1'R(1''R,3''R,4''R)],15R,18R,19R,21R,23S,30S,32S,35R]-1,18-Dihydroxy-12-[2-[4-[3-hydroxy-2-(hydroxymethyl)-2-methylpropionyloxy]-3-methoxycyclohexyl]-1-methylethyl]-19...
参考文献标题:Rapamycin hydroxyesters
文献作者:Skotnicki,J.S.; Leone,C.L.; Schiehser,G.A.(American Home Products Corp.)
参考来源:EP 0763039; JP 1997512018; US 5362718; WO 9528406

Cinoxacin, Cinobac

西诺沙星Chemical Name: 1-Ethyl-4-oxo-1,4-dihydro[1,3]dioxolo[4,5-g]cinnoline-3-carboxylic acid
CAS No. 28657-80-9
项目整合开发状态: Launched
项目研究机构: Lilly (Originator)
合成路线:The reduction of 2-nitro-4,...
参考文献标题:Un m閠odo para la preparaci髇 de 醕idos 6,7-metilendioxi-4(1H)-oxocinnolin-3-carbox韑icos
文献作者:
参考来源:ES 376173; ES 402312

Cinolazepam, OX-373, Gerodorm

西诺西泮Chemical Name: 7-Chloro-1-(2-cyanoethyl)-5-(2'-fluorophenyl)-3-hydroxy-1,3-dihydro-2H-1,4-benzodiazepin-2-one; 3-[7-Chloro-5-(2-fluorophenyl)-3-hydroxy-2,3-dihydro-2-oxo-1H-1,4-benzodiazepin-1-yl]...
参考文献标题:Novel 3-hydroxy-1,4-benzodiazepine-2-ones and process for the preparation thereof
文献作者:Schlager,L.H.(Gerot Pharmazeutika GmbH)
参考来源:AT 361492B; DE 2950235; ES 8103738; FR 2444672; US 4388313

Nolatrexed dihydrochloride, AG-337, Thymitaq

诺拉曲特Chemical Name: 2-Amino-6-methyl-5-(4-pyridylsulfanyl)quinazolin-4(3H)-one dihydrochloride
CAS No. 147149-76-6 (free base)
项目整合开发状态: Phase III
项目研究机构: Eximias Pharmaceutical (Orphan Drug),...
参考文献标题:Antiproliferative quinazolines
文献作者:Webber,S.E.; Bleckman,T.M.; Attard,J.; Jones,T.R.; Varney,M.D.(Agouron Pharmaceuticals,Inc.)
参考来源:EP 0637300; US 5430148; WO 9320055

Nocloprost, ZK 94 726, ZK-84726

诺氯前列素Chemical Name: (Z)-7-[(1R,2R,3R,5R)-5-Chloro-3-hydroxy-2-[(E)-(3R)-3-hydroxy-4,4-dimethyl-1-octenyl]cyclopentyl]-5-heptenoic acid; (9R,11R,15R)-9-Chloro-11,15-dihydroxy-16,16-dimethylprosta-5Z,13...
参考文献标题:Pharmaceutically active 9-chloroprostaglandins
文献作者:Elger,W.; Loge,O.; Skuballa,W.; Vorbr黦gen,H.; Radb點hel,B.; Schillinger,E.(Schering AG)
参考来源:DE 2950027; US 4444788; US 5079259

Nomifensine maleate, Hoe-984, Merital

诺米芬新马来酸盐诺米芬辛 Chemical Name: 8-Amino-2-methyl-4-phenyl-1,2,3,4-tetrahydroisoquinoline maleate
CAS No. 32795-47-4, 24526-64-5 (free base)
项目整合开发状态: Launched
项目研究机构: Aventis Pharma (Originator)...
参考文献标题:4-Phenyl-8-amino tetrahydroisoquinolines
文献作者:Hoffmann,I.; Gustav,E.; Heinrich,O.; Schmitt,K.(Aventis Pharma AG)
参考来源:DE 1670694; DE 1670848; FR 1524487; FR 6496M; FR 6646M; GB 1164192; US 3577424