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

Oxmetidine Hydrochloride, SK&F-92994-J2(mesylate), SK&F-92994(free base), SK&F-92994-A2

5-(1,3-苯并二氧-5-甲基)-2-[[2-[[(5-甲基-1h-咪唑-4-基)甲基]硫代]乙基]氨基]-1h-嘧啶-4-酮二盐酸盐奥美替丁 Chemical Name: 5-(1,3-Benzodioxol-5-ylmethyl)-2-[[2-[[(5-methyl-1H-imidazol-4-yl)methyl]thio]ethyl]amino]-4-(1H)-pyrimidinone ...
参考文献标题:Process for preparing 2-aminopyrimidones,intermediate 2-nitroaminopyrimidones and a process for their preparation
文献作者:Brown,T.H.(SmithKline Beecham plc)
参考来源:EP 0004793

Apaziquone, NOR-701, E-85/050, E09, E-85/053, NSC-382456, EO9, EOquin, Neoquin

5-(1-氮丙啶基)-3-(羟基甲基)-2-[(1E)-3-羟基-1-丙烯-1-基]-1-甲基-1H-吲哚-4,7-二酮Chemical Name: (E)-5-(1-Azirinyl)-3-(hydroxymethyl)-2-(3-hydroxy-1-propenyl)-1-methyl-1H-indole-4,7-dione
CAS No. 114560-48-4
项目整合开发状态...
参考文献标题:Indoloquinone cpds
文献作者:Speckamp,W.N.; Oostveen,E.A.(University of Amsterdam)
参考来源:JP 1989502906; US 5079257; WO 8706227

VX-745

5-(2,6-二氯苯基)-2-((2,4-二氟苯基)硫基)-6H-嘧啶并[1,6-b]哒嗪-6-酮Chemical Name: 5-(2,6-Dichlorophenyl)-2-(2,4-difluorophenylsulfanyl)-6H-pyrimido[3,4-b]pyridazin-6-one
CAS No. 209410-46-8
项目整合开发状态: Phase II
...
参考文献标题:Substd.nitrogen containing heterocycles as inhibitors of p38 protein kinase
文献作者:Salituro,F.G.; Duffy,J.P.; Murcko,M.A.; Bemis,G.W.; Su,M.; Wilson,K.P.; Cochran,J.E.; Harrington,E.M.; Galullo,V.P.(Vertex Pharmaceuticals Inc.)
参考来源:EP 0951467; JP 2001506266; WO 9827098

FPL-52694

5-(2-羟基丙氧)-4-氧-8-丙基-4H-1-苯并吡喃-2-羧酸单钠盐Chemical Name: 5-(2-Hydroxypropoxy)-4-oxo-8-propyl-4H-1-benzopyran-2-carboxylic acid monosodium salt
CAS No. 58974-94-0, 58974-93-9 (free acid)
项目整合开发状态: Ph...
参考文献标题:FPL-52,694
文献作者:Sneddon,J.M.; Serradell,M.N.; Castar,J.; Blancafort,P.
参考来源:Drugs Fut 1982,7(6),388

Velaresol, 12C79, BW-12C

5-(2-醛基-3-羟基苯氧基)戊酸Chemical Name: 5-(2-Formyl-3-hydroxyphenoxy)pentanoic acid
CAS No. 77858-21-0
项目整合开发状态: Phase II
项目研究机构: GlaxoSmithKline (Originator)
合成路线:The reaction of 2-hydroxy-6-met...
参考文献标题:Substd.phenol ethers,their preparation,intermediates therefor,pharmaceutical compsns.containing them and the preparation thereof
文献作者:Kneen,G.(Glaxo Wellcome plc)
参考来源:EP 0022229

KT-362

5-(3-((2-(3,4-二甲氧基苯基)乙基)氨基)-1-氧代丙基)-2,3,4,5-四氢-1,5-苯并硫氮杂卓(E)-2-丁烯二酸盐(1:1)Chemical Name: 5-[N-[2-(3,4-Dimethoxyphenyl)ethyl]-beta-alanyl]-2,3,4,5-tetrahydrobenzo-1,5-thiazepine bifumarate
CAS No. 10...
参考文献标题:Antihypertensive 1,5-benzothiazepine derivs.and compsns.thereof
文献作者:Tomiyama,T.(Kotobuki Pharmaceutical Co.,Ltd.)
参考来源:US 4584292

Risarestat, CT-112

5-(3-乙氧基-4-戊氧基苯基)-1,3-噻唑烷-2,4-二酮Chemical Name: 5-[3-Ethoxy-4-(pentyloxy)phenyl]-2,4-thiazolidinedione
CAS No. 79714-31-1
项目整合开发状态: Phase II
项目研究机构: Senju (Originator), Takeda (Originator)
...
参考文献标题:Thiazolidine derivs.and their production and use
文献作者:Kawamatsu,Y.; Yamamoto,Y.(Senju Pharmaceuticals Co.,Ltd.; Takeda Chemical Industries,Ltd.)
参考来源:EP 0033617

ABT-702

5-(3-溴苯基)-7-[6-(4-吗啉基)-3-吡啶基]-吡啶并[2,3-d]嘧啶-4-胺Chemical Name: 5-(3-Bromophenyl)-7-[6-(4-morpholinyl)pyridin-3-yl]pyrido[2,3-d]pyrimidin-4-amine; 5-(3-Bromophenyl)-7-[6-(4-morpholinyl)pyridin-3-yl]pyrid...
参考文献标题:5,7-Disubstd.-4-aminopyrido[2,3-d]pyrimidine cpds.and their use as adenosine kinase inhibitors
文献作者:Cowart,M.D.; Lee,C.-H.; Grillot,A.L.; Bhagwat,S.S.; McKie,J.(Abbott Laboratories Inc.)
参考来源:EP 0989986; WO 9846605

SLV-319

5-(4-氯苯基)-N-(4-氯苯基)磺酰基-N'-甲基-4-苯基-3,4-二氢吡唑-2-甲脒Chemical Name: 4-Chloro-N-[1-[3-(4-chlorophenyl)-4(S)-phenyl-4,5-dihydro-1H-pyrazol-1-yl]-1-(methylamino)methylidene]benzenesulfonamide; 3-(4-Chloropheny...
参考文献标题:4,5-Dihydro-1H-pyrazole derivs.having CB 1-antagonistic activity
文献作者:Kruse,C.G.; Tulp,M.T.M.; Lange,J.H.M.; Tipker,J.; Van Vliet,B.J.(Solvay Pharmaceuticals BV)
参考来源:EP 1268435; US 2001053788; US 6476060; WO 0170700

Trifluoropentoxypicolinic acid, ND-186 H-5

5-(5,5,5-三氟戊氧基)吡啶-2-羧酸Chemical Name: 5-[(5,5,5-Trifluoropentyl)oxy]-2-pyridinecarboxylic acid; 5-(5,5,5-Trifluoropentoxy)picolinic acid
CAS No. 72133-44-9, 72133-65-4 (Ca salt)
项目整合开发状态: Biologi...
参考文献标题:5-Alkoxypicolinic acid ester,its preparation,and hypotensive agent containing the same
文献作者:Hachisu,M.; Inouye,S.; Sezaki,M.; Shimomura,K.; Koeda,T.; Tsuruoka,T.; Niida,T.; Shibata,U.; Miyamoto,M.; Mizutani,K.; Sekizawa,Y.(Meiji Seika Kaisha,Ltd.)
参考来源:BE 875070; JP 1979125680