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

Furopenem, Faropenem sodium, Fropenem sodium, BLA-857, RU-67655, Wy-49605, YM-044, SY-5555, ALP-201, SUN-5555, Farom

法罗培南钠法罗培南钠 Chemical Name: (5R,6S)-6-[1(R)-Hydroxyethyl]-2-[2(R)-tetrahydrofuryl]penem-3-carboxylic acid monosodium salt; [5R-[3(R*),5alpha,6alpha(R*)]]-6-(1-Hydroxyethyl)-7-oxo-3-(tetrahydro-2-furan...
参考文献标题:Penem cpds
文献作者:Ishiguro,M.; Iwata,H.; Nakatsuka,T.(Suntory Ltd.)
参考来源:AU 8654460; EP 0199446; JP 1994128267; US 4997829

Fasidotril, Alatriopril, Aladotril, BP1.137

法西多曲Chemical Name: (-)-(S)-N-[2-(Acetylthiomethyl)-3-(3,4-methylenedioxyphenyl)propanoyl]-(S)-alanine benzyl ester
CAS No. 135038-57-2
项目整合开发状态: Phase II
项目研究机构: Bioprojet (Originator), Lilly...
参考文献标题:Amino acid derivs.,method for their preparation and their therapeutic application
文献作者:Plaquevent,J.-C.; Danvy,D.; Monteil,T.; Greciet,H.; Duhamel,L.; Duhamel,P.; Gros,C.; Schwartz,J.-C.; Lecomte,J.-M.(Societe Civile Bioprojet)
参考来源:EP 0419327; FR 2652087; WO 9104246

Fanapanel, ZK-200775, MPQX

法那帕奈Chemical Name: 7-Morpholino-2,3-dioxo-6-(trifluoromethyl)-1,2,3,4-tetrahydroquinoxalin-1-ylmethylphosphonic acid
CAS No. 161605-73-8
项目整合开发状态: Phase I
项目研究机构: Novo Nordisk (Originator), S...
参考文献标题:Quinoxalindione derivs.,their preparation and their use in drugs
文献作者:Huth,A.; Turski,L.(Schering AG)
参考来源:DE 4314591; DE 4344486; EP 0696288; EP 1002796; JP 1996508037; US 5750525; WO 9425469

Fantofarone, SR-33557

泛托法隆Chemical Name: 2-Isopropyl-1-[4-[3-[N-methyl-N-[2-(3,4-dimethoxyphenyl)ethyl]amino]propoxy]phenylsulfonyl]indolizine
CAS No. 114432-13-2
项目整合开发状态: Phase III
项目研究机构: Labaz (Originator), Sa...
参考文献标题:Novel heterocyclic analogues of the new potent class of calcium entry blockers: 1-[[4-(Aminoalkoxy)phenyl]sulfonyl]indolizines
文献作者:Gubin,J.; de Vogelaer,H.; Inion,H.; Houben,C.; Lucchetti,J.; Mahaux,J.; Rosseels,G.; Peiren,M.; Clinet,M.; Polster,P.; et al.
参考来源:J Med Chem 1993,36(10),1425

Famciclovir, BRL-42810, Famvir

泛昔洛韦Chemical Name: 9-[4-Acetoxy-3-(acetoxymethyl)butyl]-2-aminopurine
CAS No. 104227-87-4
项目整合开发状态: Launched-1994
项目研究机构: Novartis (Proprietary), GlaxoSmithKline (Originator), Solvay (License...
参考文献标题:Prodrugs of the selective antiherpesvirus agent 9-[4-hydroxy-3-(hydroxy methyl)but-1-yl]guanine (BRL 39123) with improved gastrointestinal absorption properties
文献作者:Harnden,M.R.; Boyd,M.R.; Vere Hodge,R.A.; Jarvest,R.L.; Sutton,D.
参考来源:J Med Chem 1989,321738-43

Bopindolol, LT-31200, Wandonorm, Sandonorm

波吲洛尔Chemical Name: (?-1-(tert-Butylamino)-3-[(2-methylindol-4-yl)oxy]-2-propanol benzoate (ester)
CAS No. 62658-63-3
项目整合开发状态: Launched-1985
项目研究机构: Novartis (Originator)
合成路线:By esterific...
参考文献标题:Use of 4-(2-benzoyloxy-3-tert-butylaminopropoxy)-2-methyl-indole for inducing beta-adrenoceptor blocade
文献作者:Troxler,F.; Seemann,F.(Novartis AG)
参考来源:BE 0845197; DE 2635209; FR 2320743; GB 1575509; JP 56049318; US 4434176

Bofumustine, RFCNU, ICI-G1105

波呋莫司汀Chemical Name: N-(2-Chloroethyl)-N'-[2,3-O-(1-methylethylidene)-5-O-(4-nitrobenzoyl)-1-ribofuranosyl]-N-nitrosourea; 1-(2-Chloroethyl-3-(2,3-O-isopropylidene-D-ribofuranosyl)-1-nitrosourea 5'-(p-...
参考文献标题:Bofumustine
文献作者:Eastland,G.
参考来源:Drugs Fut 1984,9(9),641

Botiacrine, DMA

波普吖啶Chemical Name: 9,9-Dimethylacridine-10(9H)-carbothioic acid S-[2-(dimethylamino)ethyl] ester
CAS No. 4774-53-2
项目整合开发状态: Biological Testing
项目研究机构:
合成路线:The esterification of N-phenyl...
参考文献标题:Botiacrine
文献作者:Castar,J.; Hopkins,S.J.
参考来源:Drugs Fut 1978,3(1),16

Ponalrestat, MK-538, ICI-128436, Prodiax, Statil

波来瑞斯Chemical Name: 3-(4-Bromo-2-fluorobenzyl)-4-oxo-3,4-dihydro-1-phthalazineacetic acid
CAS No. 72702-95-5, 72703-73-2 (Na salt)
项目整合开发状态: Phase III
项目研究机构: AstraZeneca (Originator), Banyu (...
参考文献标题:Increasing vigilance or treating cerebral insuffi
文献作者:Pf鋐fli,P.(Novartis AG)
参考来源:GB 1492579; US 4146643

Bosentan, Ro-47-0203/039, Ro-47-0203/029(monohydrate), Ro-47-0203, Tracleer

波生坦 N-[6-(2-羟基)-5-(2-甲氧基苯氧基)-2-嘧啶-2-酰嘧啶-4-酰]-4-叔丁基-苯磺酰胺波生坦Chemical Name: 4-tert-Butyl-N-[6-(2-hydroxyethoxy)-5-(2-methoxyphenoxy)-2-(2-pyrimidinyl)pyrimidin-4-yl]benzenesulfonamide
CAS No. 147536-...
参考文献标题:Sulfonamide,preparation and use thereof as medicine and intermediate
文献作者:Burri,K.; Clozel,M.; Fischli,W.; Hirth,G.; L鰂fler,B.-M.; Ramuz,H.; Neidhart,W.(F.Hoffmann-La Roche AG)
参考来源:EP 0526708; JP 1993222003; US 4292740