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

YNS-15P

Chemical Name: (2R,11bS)-N-(9-Methoxy-2,3,4,6,7,11b-hexahydro-1H-benzo[a]quinolizin-2-yl)-N-methylmethanesulfonamide hydrochloride
CAS No. 198954-06-2, 198953-89-8 (trans-isomer, monoHCl)
项目整合开发...
参考文献标题:Benzoquinolizine derivs.and medicinal compsns.
文献作者:Yamamoto,O.; Shirouchi,Y.(Nippon Shinyaku Co.,Ltd.)
参考来源:EP 0897923; WO 9740046

TAP-doxorubicin, Super-Leu-Dox, CPI-0004, CPI-004Na, CPI-0004Na

Chemical Name: N-[N-(3-Carboxypropionyl)-beta-alanyl-L-leucyl-L-alanyl-L-leucyl]daunorubicin sodium salt; (8S,10S)-10-[3-[N-(3-Carboxy-1-oxopropyl)-beta-alanyl-L-leucyl-L-alanyl-L-leucylamido]-2,3,6-t...
参考文献标题:Prodrug cpds.and process for preparation thereof
文献作者:Lobl,T.J.; Trouet,A.; Fernandez,A.-M.; Nieder,M.H.; Yarranton,G.T.; Gangwar,S.; Viski,P.; Lewis,E.; Dubois,V.(Beckman Coulter,Inc.)
参考来源:WO 0033888

FR-202893(racemate), FR-208418(S), FR-208419

Chemical Name: N-[1-(2-Cyclohexyl-2-oxoethyl)-5-ethyl-9-methyl-2-oxo-2,3-dihydro-1H-1,4-benzodiazepin-3(R)-yl]-N'-(3-methylphenyl)urea
CAS No. 206001-43-6
项目整合开发状态: Preclinical
项目研究机构: Fujisa...
参考文献标题:Design of dual CCK-A and CCK-B receptor antagonists
文献作者:Satoh,Y.; Tabuchi,S.; Mitsui,H.
参考来源:Drugs Fut 1997,22(10),1117

FR-184280

Chemical Name: N-[N-[2,4-Dichloro-3-(2-methylquinolin-8-yloxymethyl)phenyl]-N-methylcarbamoylmethyl]-3-[6-[2(E)-(4-pyridyl)vinyl]pyridin-3-yl]-2(E)-propenamide
CAS No. 179623-05-3
项目整合开发状态: Prec...
参考文献标题:A novel class of orally active non-peptide bradykinin B2 receptor antagonists.3.Discovering bioisosteres of the imidazo[1,2-a]pyridine moiety
文献作者:Abe,Y.; Kayakiri,H.; Satoh,S.; Inoue,T.; Sawada,Y.; Inamura,N.; Asano,M.; Aramori,I.; Hatori,C.; Sawai,H.; Oku,T.; Tanaka,H.
参考来源:J Med Chem 1998,41(21),4062

FR-193517

Chemical Name: 3-(6-Acetamidopyridin-3-yl)-N-[1-[2,4-dichloro-3-(2-methylquinolin-8-yloxymethyl)phenyl]pyrrol-2-ylmethyl]-2(E)-propenamide dihydrochloride
CAS No. 189266-51-1 (free base)
项目整合开发状...
参考文献标题:A novel class of orally active non-peptide bradykinin B2 receptor antagonists.4.Discovery of novel frameworks mimicking the active conformation
文献作者:Abe,Y.; Kayakiri,H.; Satoh,S.; Inoue,T.; Sawada,Y.; Inamura,N.; Asano,M.; Aramori,I.; Hatori,C.; Sawai,H.; Oku,T.; Tanaka,H.
参考来源:J Med Chem 1998,41(23),4587

Sch-51344

Chemical Name: 2-[2-(6-Methoxy-3-methyl-1H-pyrazolo[3,4-b]quinolin-4-ylamino)ethoxy]ethanol
CAS No. 171927-40-5
项目整合开发状态: Biological Testing
项目研究机构: Schering-Plough (Originator)
合成路线:The t...
参考文献标题:4-Substd.pyrazoloquinoline derivs.
文献作者:Afonso,A.; Kelly,J.M.; Chackalamannil,S.
参考来源:US 5608067

GW-275175X, GW-275175

Chemical Name: 2-Bromo-5,6-dichloro-1-beta-D-ribopyranosyl-1H-benzimidazole
CAS No. 217950-62-4
项目整合开发状态: Phase I
项目研究机构: GlaxoSmithKline (Originator)
合成路线:Condensation of 2-bromo-5,6-dich...
参考文献标题:Benzimidazole derivs.
文献作者:Daluge,S.M.; Townsend,L.B.; Freeman,G.A.; Deaton,D.N.; Andersen,M.W.; Drach,J.C.; Boyd,F.L.Jr.; Chamberlain,S.D.(Glaxo Group Ltd.; University of Michigan)
参考来源:WO 9856761

CGP-75176

Chemical Name: N-(Methoxycarbonyl)-L-tert-leucine N2-[2(S)-hydroxy-3(S)-[N-(methoxycarbonyl)-L-tert-leucylamino]-4-phenylbutyl]-N2-[4-(2-methyl-5-tetrazolyl)benzyl]hydrazide
CAS No. 198904-13-1
...
参考文献标题:Antivirally active heterocyclic azahexane derivs.
文献作者:F鋝sler,A.; Bold,G.; Capraro,H.-G.; Lang,M.; Khanna,S.C.(Novartis AG)
参考来源:EP 0900210; JP 1999511177; US 5849911; WO 9740029

新产品编号:307417

Chemical Name: 7-[4-[4-[N-(4-Cyclohexylbutyl)carbamoyl]oxazol-2-yl]phenyl]-7-(3-pyridyl)-6(E)-heptenoic acid
CAS No. 200399-71-9
项目整合开发状态: Preclinical
项目研究机构: Lilly (Originator)
合成路线:1,4-B...
参考文献标题:Development of dual-acting agents for thromboxane receptor antagonism and thromboxane synthase inhibition.2.Design,synthesis,and evaluation of a novel series of phenyl oxazole derivatives
文献作者:Takeuchi,K.; Kohn,T.J.; Mais,D.E.; True,T.A.; Wyss,V.L.; Jakubowski,J.A.
参考来源:Bioorg Med Chem Lett 1998,8(15),1943-1948

NGB-2849

Chemical Name: N-[4-[4-(2,3-Dichlorophenyl)piperazin-1-yl]butyl]biphenylene-2-carboxamide
CAS No. 198555-28-1
项目整合开发状态: Biological Testing
项目研究机构: Neurogen (Originator)
合成路线:Dichlorophenyl...
参考文献标题:NGB 2904 and NGB 2849: Two highly selective dopamine D3 receptor antagonists
文献作者:Yuan,J.; Chen,X.; Brodbeck,R.; Primus,R.; Braun,J.; Wasley,W.F.; Thurkauf,A.
参考来源:Bioorg Med Chem Lett 1998,8(19),2715