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

Pentopril, CGS-13945

喷托普利Chemical Name: 1-(4-Ethoxycarbonyl-2,4(R,R)-dimethylbutanoyl)indoline-2(S)-carboxylic acid; [2S-[1-(alphaS*,gammaS*),2R*]]-2-Carboxy-2,3-dihydro-alpha,gamma-dimethyl-delta-oxo-1H-indole-1-pentanoi...
参考文献标题:1-Carboxyalkanoylindolin-2-carboxylic acids and derivs.thereof,processes for their preparation,and pharmaceutical compsns.containing these cpds.as well as their use
文献作者:Gruenfeld,N.(Novartis AG)
参考来源:EP 0050850

Penciclovir, BRL-39123, Denavir, Vectavir

喷昔洛韦钠4-(2-氨基-6-氧-6,9-二氢-1H-嘌呤-9-基)-2-(羟甲基)丁烷-1-奥莱特 Chemical Name: 9-[4-Hydroxy-3-(hydroxymethyl)butyl]guanine
CAS No. 39809-25-1, 97845-62-0 (Na salt)
项目整合开发状态: Launched-1996
项目研究机构: Novarti...
参考文献标题:Guanine derivs.
文献作者:Harnden,M.R.; Jarvest,R.L.(SmithKline Beecham plc)
参考来源:EP 0141927; ES 8602791; ES 8603887; ES 8603888; JP 1994293764; US 5075445

Pentisomide, Penticainide, ME-3202, CM-7857

喷替索胺Chemical Name: 2-[2-(Diisopropylamino)ethyl]-4-methyl-2-(2-pyridyl)pentanamide; alpha-[2-[Bis(1-methylethyl)amino]ethyl]-alpha-(2-methylpropyl)-2-pyridineacetamide
CAS No. 78833-03-1, 96513-83-...
参考文献标题:CM-7857
文献作者:Blancafort,P.; Castar,J.; Serradell,M.N.
参考来源:Drugs Fut 1983,8(12),1016

LY-141865

喹吡罗Chemical Name: (4abeta,7beta,8aalpha)-(?-4-4a,5,6,7,8,8a,9-Octahydro-7-(methylthiomethyl)-5-propyl-2H-pyrazolo[43,4-g]quinoline
CAS No. 80373-22-4
项目整合开发状态: Phase II
项目研究机构: Lilly (Origina...
参考文献标题:Prolactin inhibiting octahydropyrazolo[3,4-g]quinolines
文献作者:Bach,N.; Kornfeld,E.C.(Eli Lilly and Company)
参考来源:DD 148517; EP 0013787; ES 482087; FR 2446820; FR 2446821; FR 2446822; GB 2040915; GB 2092579; US 4198415

Cethromycin, A-195773.0, ABT-773

喹红霉素Chemical Name: (1S,2R,5R,7R,8R,9R,11R,13R,14R)-2-Ethyl-1,5,7,9,11,13-hexamethyl-9-[3-(3-quinolyl)-2(E)-propenyloxy]-8-[3,4,6-trideoxy-3-(dimethylamino)-beta-D-glucopyranosyloxy]-3,17-dioxa-15-azab...
参考文献标题:6-O-Substd.ketolides having antibacterial activity
文献作者:Or,Y.S.; Ma,Z.; Clark,R.F.; Chu,D.T.; Plattner,J.J.(Abbott Laboratories Inc.)
参考来源:EP 0929563; US 5866549; WO 9809978

Quinacainol, PK-10139

喹那卡诺Chemical Name: (?-2-(1,1-Dimethylethyl)-alpha-[2-(4-piperidinyl)ethyl]-4-quinolinemethanol; (?-2-tert-Butyl-alpha-[2-(4-piperidyl)ethyl]-4-quinolinemethanol; (?-1-[4-(2-tert-Butylquinolyl)]-3-(4-p...
参考文献标题:Quinacainol
文献作者:Castar,J.; Serradell,M.N.; Koch,H.
参考来源:Drugs Fut 1984,9(4),273

Zindotrine, MDL-257

嗪多群Chemical Name: 8-Methyl-6-(1-piperidinyl)-1,2,4-triazolo[4,3-b]pyridazine; 8-Methyl-6-piperidino-s-triazolo[4,3-b]pyridazine
CAS No. 56383-05-2
项目整合开发状态: Phase II
项目研究机构: Aventis Pharma (O...
参考文献标题:Triazolopyridazines used to alleviate bronchial spasms
文献作者:Lewis,J.; Shea,P.J.(Aventis Pharmaceuticals,Inc.)
参考来源:US 4136182

CDD-0102

嘧啶,5-(3-乙基-1,2,4-氧二唑-5-基)-1,4,5,6-四氢-Chemical Name: 5-(3-Ethyl-1,2,4-oxadiazol-5-yl)-1,4,5,6-tetrahydropyrimidine
CAS No. 146422-58-4
项目整合开发状态: Preclinical
项目研究机构: Cognitive Pharmaceuticals (...
参考文献标题:Design,synthesis,and neurochemical evaluation of 5-(3-alkyl-1,2,4-oxadiazol-5-yl)-1,4,5,6-tetrahydropyrimidines as M1 muscarinic receptor agonists
文献作者:Dunbar,P.G.; Durant,G.J.; Fang,Z.; Abuh,Y.F.; El-Assadi,A.A.; Ngur,D.O.; Periyasamy,S.; Hoss,W.P.; Messer,W.S.Jr.
参考来源:J Med Chem 1993,36(7),842

Tiazofurin, Tiazofurine, Cpd-5825, ICN-4221, CI-909, TCAR, NSC-286193, Tiazole

噻唑呋林Chemical Name: 2-(beta-D-Ribofuranosyl)thiazole-4-carboxamide
CAS No. 60084-10-8
项目整合开发状态: Phase III
项目研究机构: Valeant (Orphan Drug), Valeant (Originator)
合成路线:A new synthesis of thiazof...
参考文献标题:Tiazofurine
文献作者:Eastland,G.
参考来源:Drugs Fut 1985,10(4),304

Tianeptine sodium, S-1574, Stablon

噻奈普汀钠盐噻奈普汀 (+)-噻奈普汀单钠盐Chemical Name: 7-(3-Chloro-6-methyl-6,11-dihydrodibenzo[c,f][1,2]thiazepin-11-ylamino)heptanoic acid S,S-dioxide sodium salt
CAS No. 30123-17-2, 66981-73-5 (free acid), 54317...
参考文献标题:S-1574
文献作者:Castar,J.; Neuman,M.; Blancafort,P.; Serradell,M.N.
参考来源:Drugs Fut 1979,4(7),522