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

L-708906

Chemical Name: 4-[3,5-Bis(benzyloxy)phenyl]-2,4-dioxobutyric acid
CAS No. 251963-74-3
项目整合开发状态: Preclinical
项目研究机构: Amgen (Originator), Merck & Co. (Originator)
合成路线:Claisen condensation o...
参考文献标题:HIV integrase inhibitors
文献作者:Guare,J.P.Jr.; Jaen,J.; Tran,L.; Vacca,J.P.; Zhuang,L.; Egbertson,M.; Medina,J.C.; Melamed,J.; Clark,D.L.; Fisher,T.E.; Langford,M.; Wai,J.S.; Payne,L.S.; Embrey,M.W.; Young,S.D.(Merck & Co.,Inc.; Tularik Inc.)
参考来源:WO 9962520

新产品编号:615907

Chemical Name: 4-(3-Chlorophenyl)-2-hydroxy-4-oxobut-2(Z)-enoic acid methyl ester
CAS No. 235789-20-5
项目整合开发状态: Biological Testing
项目研究机构: GlaxoSmithKline (Originator)
合成路线:By condensation...
参考文献标题:Synthesis and SAR of 4-aryl-2-hydroxy-4-oxobut-2-enoic acids esters and 2-amino-4-aryl-4-oxobut-2-enoic acids and esters: Potent inhibitors of kynurenine-3-hydroxylase as potential neuroprotective agents
文献作者:Drysdale,M.J.; Hind,S.L.; Janssen,M.; Reinhard,J.F.Jr.
参考来源:J Med Chem 2000,43(1),123

新产品编号:256793

Chemical Name: 6alpha,9-Difluoro-11beta-hydroxy-16alpha,17-(isopropylidenedioxy)-21-(2-oxotetrahydrofuran-3-ylsulfanyl)pregna-1,4-diene-3,20-dione
CAS No. 193408-35-4 ((R)-isomer), 193408-36-5 ((S)...
参考文献标题:21-(2-Oxo-tetrahydrofuran)-thio pregnane derivs.,a process for their production and pharmaceutical compsns.containing them
文献作者:Farrell,R.M.; Biggadike,K.(Glaxo Wellcome Inc.)
参考来源:US 6013244; WO 9724367

新产品编号:190349

Chemical Name: 3-[5-[3-[N-(1H-Imidazol-2-yl)carbamoyl]propyl]-4,5-dihydroisoxazo-3-carboxamido]-2(S)-(2,4,6-trimethylphenylsulfonamido)propionic acid
CAS No. 185562-53-2
项目整合开发状态: Biological Tes...
参考文献标题:Isoxazoline and isoxazole derivs.as integrin receptor antagonists
文献作者:Voss,M.E.; Jadhav,P.K.; Smallheer,J.M.; Batt,D.G.; Pitts,W.J.; Wityak,J.(DuPont Pharmaceuticals Co.)
参考来源:EP 0828737; JP 1999506436; US 5710159; WO 9637492

新产品编号:698171

Chemical Name: 4-O-(2-Acetamido-4-amino-2,4,6-trideoxy-beta-D-galactopyranosyl)-2-acetamido-2-deoxy-1-O-methyl-alpha-L-altropyranosuronic acid
CAS No. 259534-62-8
项目整合开发状态: Biological Testing 参考文献标题:Synthesis of the repeating unit of the O-specific polysaccharide of Shigella sonnei and quantitation of its serologic activity
文献作者:T髏h,A.; Medgyes,A.; Bajza,I.; Liptak,A.; Batta,G.; Kontrohr,T.; Peterffy,K.; Pozsgay,V.
参考来源:Bioorg Med Chem Lett 2000,10(1),19

新产品编号:24239

Chemical Name: 4-[1-(3-Methyl-4-oxo-2-thioxothiazolidin-5-ylidenemethyl)naphthalen-2-yloxy]butyric acid
CAS No. 123021-26-1
项目整合开发状态: Preclinical
项目研究机构: Dainippon Pharmaceutical (Originator)...
参考文献标题:Synthesis and aldose reductase inhibitory activity of a new series of 5-[[2-(omega-carboxyalkoxy)aryl]methylene]-4-oxo-2-thioxothiazolidine derivatives
文献作者:Fujitani,B.; Mizuta,H.; Murata,M.
参考来源:Eur J Med Chem 1999,34(12),1061

新产品编号:282105

Chemical Name: 4-[3-(4-Fluorophenyl)-2-oxo-2,3-dihydrooxazol-4-yl]benzenesulfonamide
CAS No. 197240-09-8
项目整合开发状态: Preclinical
项目研究机构: Almirall Prodesfarma (Originator)
合成路线:The synthesis ...
参考文献标题:2-(3H)-Oxazolone derivs.and their use as COX-2 inhibitors
文献作者:Puig Duran,C.; Pujol Noguera,F.; Fernandez Forner,D.(Almirall Prodesfarma,SA)
参考来源:EP 0888316; ES 2125161; JP 2000506876; WO 9734882

TA-949

Chemical Name: (1R,5S,6S)-6-[1(R)-Hydroxyethyl]-1-methyl-2-[2-thioxopyrrolidin-4(R)-ylsulfanyl]-1-carba-2-penem-3-carboxylic acid isobutyryloxymethyl ester
CAS No. 141628-82-2, 141662-30-8 ((S)-iso...
参考文献标题:1-Methylcarbapenem derivs.and process for preparation thereof
文献作者:Iwasaki,T.; Kondo,K.; Horikawa,H.; Yamaguchi,T.; Matsushita,T.(Tanabe Seiyaku Co.,Ltd.)
参考来源:EP 0474243; JP 1992279588; US 5153187

新产品编号:286851

Chemical Name: O-[2-Deoxy-2-[3(R)-(tetradecanoyloxy)tetradecanoylamino]-beta-D-glucopyranosyl]-N-(tetradecanoyl)-L-seryl-beta-alanine
CAS No. 197663-09-5
项目整合开发状态: Biological Testing
项目研究机构: ...
参考文献标题:Synthesis of Tn,sialyl Tn and HIV-1-derived peptide antigen conjugates having a lipid A analog as an immunoadjuvant for synthetic vaccines
文献作者:Miyajima,K.; Nekado,T.; Ikeda,K.; Achiwa,K.
参考来源:Chem Pharm Bull 1998,46(11),1676

Arcyriacyanin A

Chemical Name: 5,9-Dihydro-1H-pyrrolo[3',4':6,7]cyclohepta[2,1-b:5,4,3-c'd']diindole-1,3(2H)-dione
CAS No. 188548-81-4
项目整合开发状态: Biological Testing
项目研究机构: Showa Coll. Pharm. Sciences (Origin...
参考文献标题:A new concise synthesis of arcyriacyanin A and its unique inhibitory activity against a panel of human cancer cell line
文献作者:Murase,M.; Watanabe,K.; Yoshida,T.; Tobinaga,S.
参考来源:Chem Pharm Bull 2000,48(1),81