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

AR-C89855AA

Chemical Name: 3-[2-(4-Hydroxy-2-oxo-2,3-dihydrobenzothiazol-7-yl)ethylamino]-N-[2-[2-(4-methylphenyl)ethoxy]ethyl]propanesulfonamide
CAS No. 189012-09-7, 189011-90-3 (monohydrochloride)
项目整合开发状...
参考文献标题:Benzothiazolone derivs.
文献作者:Bonnert,R.V.; Brown,R.C.; Cage,P.A.; Ince,F.; Pairaudeau,G.(AstraZeneca plc)
参考来源:JP 1999512422; US 5846989; WO 9710227

KF-24705

Chemical Name: 1-[2-(Hydroxymethyl)-6,11-dihydrodibenzo[b,e]oxepin-11-yl]-4-phenylpiperidin-4-ol
CAS No. 188607-29-6
项目整合开发状态: Preclinical
项目研究机构: Kyowa Hakko (Originator)
合成路线:Hydroxy dib...
参考文献标题:Phenylpiperidine derivs.
文献作者:Kumazawa,T.; Koshimura,H.; Aono,S.; Ichikawa,S.; Kitamura,S.(Kyowa Hakko Kogyo Co.,Ltd.)
参考来源:EP 0974583; WO 9710213

RPR-115135

Chemical Name: (3aR*,4S*,9S*,9aR*)-2-[2-(2-Methoxyphenyl)-2-propenoyl]-9-phenyl-2,3,3a,4,9,9a-hexahydro-1H-4,9-ethanobenzo[f]isoindole-3a-carboxylic acid
CAS No. 191989-28-3
项目整合开发状态: Preclinica...
参考文献标题:4,9-Ethano-benzo(f)isoindole derivs.as farnesyl transferase inhibitors
文献作者:Truchon,A.; Sounigo,F.; Peyronel,J.-F.; Zucco,M.; Mailliet,P.; Commer鏾n,A.; Lebrun,A.(Aventis Pharma SA)
参考来源:WO 9703050

Cryptophycin 55

Chemical Name: [3S-(3alpha,10beta,13E,16beta)]-16-[3(S)-Chloro-2(R)-hydroxy-1(R)-methyl-3-phenylpropyl]-10-(3-chloro-4-methoxybenzyl)-3-isobutyl-6,6-dimethyl-1,4-dioxa-8,11-diazacyclohexadec-13-ene-2,...
参考文献标题:Stereoselective process for producing antineoplastic agents
文献作者:Zmijewski,M.J.J.; Zhang,T.Y.; Aikins,J.A.; Briggs,B.S.(Eli Lilly and Company; University of Hawaii; Wayne State University)
参考来源:WO 0023429

Paclitaxel ceribate, Protaxel, BP-179

Chemical Name: 3(S)-Benzamido-2(R)-hydroxybenzenepropionic acid (2aR,4S,4aS,6R,9S,11S,12S,12aR,12bS)-6,12b-diacetoxy-12-(benzoyloxy)-4-[(2,3-dihydroxypropoxy)carbonyloxy]-11-hydroxy-4a,8,13,13-tetrame...
参考文献标题:Novel taxoids
文献作者:Sovak,M.; Douglass,J.G.; Bressi,J.C.; Seligson,A.(Biophysica Foundation)
参考来源:JP 1998509461; US 5801191; WO 9638138

RS-100975, Ro-70-0004

Chemical Name: 3-[3-[4-[4-Fluoro-2-(2,2,2-trifluoroethoxy)phenyl]piperazin-1-yl]propyl]-5-methylpyrimidine-2,4(1H,3H)-dione
CAS No. 186386-21-0
项目整合开发状态: Discontinued
项目研究机构: Roche Bioscience...
参考文献标题:Pyrimidinedione,pyrimidinetrione,triazinedione,tetrahydroquinazolinedione derivs.as alpha1-adrenergic receptor antagonists
文献作者:Bantle,G.W.; Elworthy,T.R.; Guzman,A.; Jaime-Figueroa,S.; Lopez-Tapia,F.J.; Morgans,D.J.Jr.; Perez-Medrano,A.; Pfister,J.R.; Sjogren,E.B.; Talamas,F.X.(F.Hoffmann-La Roche AG)
参考来源:EP 0748800; JP 1997100269

MPB-07

Chemical Name: 10-Chloro-6-hydroxybenzo[c]quinolizinium chloride
CAS No. 191091-55-1
项目整合开发状态: Biological Testing
项目研究机构: INSERM (Originator)
合成路线:The condensation of 2-methylpyridine (I) ...
参考文献标题:CFTR channel activator cpds.and pharmaceutical compsns.containing same
文献作者:Becq,F.; Mettey,Y.; Vierfond,J.-M.; Verrier,B.; Gola,M.(CNRS (Centre National de la Recherche Scientifique))
参考来源:EP 0937044; WO 9805642

新产品编号:239391

Chemical Name: 5-(Aziridin-1-yl)-3-(hydroxymethyl)-1,2-dimethyl-4,7-dihydro-1H-indole-4,7-dione
CAS No. 191846-71-6
项目整合开发状态: Biological Testing
项目研究机构: BTG (Originator)
合成路线:Ethyl 5-hydro...
参考文献标题:Indolequinone antitumor agents: Correlation between quinone structure,rate of metabolism by recombinant human NAD(P)H:quinone oxidoreductase,and in vitro cytotoxicity
文献作者:Beall,H.D.; Winski,S.; Swann,E.; Hudnott,A.R.; Cotterill,A.S.; O'Sullivan,N.; Green,S.J.; Bien,R.; Siegel,D.; Ross,D.; Moody,C.J.
参考来源:J Med Chem 1998,41(24),4755

SIB-1553A

Chemical Name: (?-2-[2-(4-Hydroxyphenylsulfanyl)ethyl]-1-methylpyrrolidine hydrochloride
CAS No. 191611-76-4 (free base)
项目整合开发状态: Phase II
项目研究机构: Merck & Co. (Originator)
合成路线:The conden...
参考文献标题:Novel substd.aryl cpds.useful as modulators of acetylcholine receptors
文献作者:Vernier,J.M.; McDonald,I.A.(SIBIA Neurosciences,Inc.)
参考来源:EP 0874818; JP 2000501080; WO 9719059

OPB-9195

Chemical Name: (?-2-(Isopropylidenehydrazono)-5-[N-(phenyl)carbamoylmethyl]thiazolidin-4-one
CAS No. 163107-50-4
项目整合开发状态: Preclinical
项目研究机构: Otsuka (Originator)
合成路线:The title amide was ...
参考文献标题:Thiazole or imidazole derivs.as Maillard reaction inhibitors
文献作者:Yasumura,K.; Miyajima,K.; Nagahama,T.; Ishikawa,S.; Tohyama,Y.; Sugiyama,K.(Otsuka Pharmaceutical Co.,Ltd.)
参考来源:EP 0638075; JP 1995133264; JP 1998167965; WO 9419335