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

CNS-5161

鸟嘌呤,N'-[2-氯-5-(甲硫)苯]-N-甲基-配-[3-(甲基硫)苯]-Chemical Name: N1-[2-Chloro-5-(methylsulfanyl)phenyl]-N3-methyl-N3-[3-(methylsulfanyl)phenyl]guanidine
CAS No. 160754-76-7
项目整合开发状态: Phase II
项目研究机构: Ce...
参考文献标题:Therapeutic substd.guanidines
文献作者:Durant,G.J.; Magar,S.; Hu,L.-Y.(CeNeS Pharmaceuticals)
参考来源:EP 0705100; JP 1996510754; WO 9427591

Miglustat, N-Butyl-deoxynojirimycin, N-Bu-DNJ, OGT-918, SC-48334, Zavesca, Vevesca

麦格司他Chemical Name: N-Butyldeoxynojirimycin; 1,5-(Butylimino)-1,5-dideoxy-D-glucitol; (2R,3R,4R,5S)-1-Butyl-2-(hydroxymethyl)-3,4,5-piperidinetriol; N-Butylmoranoline
CAS No. 72599-27-0, 134282-77-2...
参考文献标题:New 3,4,5-Trihydroxypiperidine derivs.,process for their preparation and medicaments and fodder containing them
文献作者:Junge,B.; Puls,W.; Krause,H.P.; M黮ler,L.(Bayer AG)
参考来源:DE 2758025; EP 0000947

Nothapodytine B, Mappicine ketone

麦皮星酮Chemical Name: 8-Methyl-7-(propanoyl)indolizino[1,2-b]quinolin-9(11H)-one; 2-Methyl-3-propionylindolizino[1,2-b]quinolin-1(11H)-one
CAS No. 55854-89-2
项目整合开发状态: Biological Testing
项目研究机构:...
参考文献标题:A convergent total synthesis of mappicine ketone: A leading antiviral compound
文献作者:Yadav,J.S.; et al.
参考来源:Tetrahedron 1999,55(17),5449

Lergotrile

麦角腈Chemical Name: 2-[(6aR,9S,10aR)-5-Chloro-7-methyl-4,6,6a,7,8,9,10,10a-octahydroindolo[4,3-fg]quinolin-9-yl]acetonitrile
CAS No. 36945-03-6
项目整合开发状态: Not Determined
项目研究机构: Lilly
合成路线:It...
参考文献标题:D-6-methyl-2,8-disubstituted ergolines
文献作者:Clemens,J.A.; et al.(Eli Lilly and Company)
参考来源:DE 2335750; ES 446789; FR 2193606; GB 1423065; JP 57081487

Azidothymidine, Zidovudine, Cpd S, AZT, BW-A509U, AZTEC, Retrovir

齐多夫定Chemical Name: 3'-Azido-3'-deoxythymidine
CAS No. 30516-87-1
项目整合开发状态: Launched-1987
项目研究机构: GlaxoSmithKline (Originator)
合成路线:1) The mesylation of 5'-O-tritylthymidine with mesyl chlo...
参考文献标题:BW-A 509 U
文献作者:Castar,J.; Prous,J.
参考来源:Drugs Fut 1986,11(12),1017

Zidometacin

齐多美辛Chemical Name: 1-(p-Azidobenzoyl)-5-methoxy-2-methyl-1H-indole-3-acetic acid
CAS No. 62851-43-8
项目整合开发状态: Biological Testing
项目研究机构: Pierrel (Originator)
合成路线:The condensation of methy...
参考文献标题:
文献作者:Tricerri,S.; Bianchetti,A.
参考来源:DE 2722399

Zileuton, CTI-02, ABT-077, A-64077, Zyflo Filmtab , Zyflo, Leutrol

齐留通Chemical Name: (?-N-Hydroxy-N-[1-(benzothiophen-2-yl)ethyl]urea; (?-N-Hydroxy-N-[1-(benzo[b]thien-2-yl)ethyl]urea; (?-1-(1-Benzo[b]thien-2-ylethyl)-1-hydroxyurea
CAS No. 111406-87-2
项目整合开发状态:...
参考文献标题:Indole,benzofuran,benzothiophene containing lipoxygenease inhibiting compounds
文献作者:Summers,J.B.Jr.; Gunn,B.P.; Brooks,D.W.(Abbott Laboratories Inc.)
参考来源:EP 0279263; JP 1988264456; US 4873259

Zifrosilone, MDL-73745

齐罗硅酮Chemical Name: alpha,alpha,alpha-Trifluoro-3-(trimethylsilyl)acetophenone; 2,2,2-Trifluoro-1-[3-(trimethylsilyl)phenyl]ethanone
CAS No. 132236-18-1
项目整合开发状态: Phase II
项目研究机构: Aventis Phar...
参考文献标题:Novel acetylcholinesterase inhibitors
文献作者:Schirlin,D.; Collard,J.-N.; Hornsperger,J.-M.(Merrell Pharmaceuticals,Inc.)
参考来源:EP 0403713; EP 0409676; JP 1991038591; US 5693668

KW-5805

Chemical Name: 5-[2-(Diethylamino)ethylamino]-5,11-dihydro[1]benzoxepino[3,4-b]pyridine
CAS No. 95968-63-1, 95968-62-0 (hydrochloride)
项目整合开发状态: Phase II
项目研究机构: Kyowa Hakko (Originator)
合...
参考文献标题:Benzepino[3,4-b]pyridine derivs.
文献作者:Kumazawa,T.; Oiji,Y.; Shuto,K.; Tanaka,H.(Kyowa Hakko Kogyo Co.,Ltd.)
参考来源:EP 0129879; JP 1985006690; JP 1985078985; JP 1985089419; US 4547496

AH-23848B, AH-23848

Chemical Name: [1alpha(Z),2beta,5alpha]-(?-7-[5-[[(1,1'-Biphen-yl)-4-yl]methoxy]-2-(4-morpholinyl)-3-oxocyclopentyl]-4-heptenoic acid
CAS No. 81443-73-4
项目整合开发状态: Preclinical
项目研究机构: GlaxoSmi...
参考文献标题:AH-23848
文献作者:Lumley,P.
参考来源:Drugs Fut 1986,11(2),85