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

Enofelast, BI-L-239 XX

Chemical Name: (E)-4-[2-(4-Fluorophenyl)vinyl]-2,6-dimethylphenol
CAS No. 127035-60-3
项目整合开发状态: Preclinical
项目研究机构: Boehringer Ingelheim (Originator)
合成路线:The reaction of 2,6-di-tert-butyl...
参考文献标题:2,6-Disubstituted-4-(2-arylethenyl)phenol 5-lipoxygenase inhibitors: Development and profile of BI-L-239
文献作者:Lazer,E.S.; Farina,P.R.; Gundel,R.H.; Wegner,C.D.
参考来源:Drugs Fut 1991,16(7),641

BRL-35135A

Chemical Name: (R*,R*)-(?-[4-[2-[2-(3-Chlorophenyl)-2-hydroxyethylamino]propyl]phenoxy]acetic acid methyl ester hydrobromide
CAS No. 86615-41-0, 91097-81-3 (free base, no stereoch.)
项目整合开发状态: Ph...
参考文献标题:Ethanamine derivs.,their preparation and use in pharmaceutical compsns
文献作者:Ainsworth,A.T.; Smith,D.G.(SmithKline Beecham plc)
参考来源:EP 0023385

Osutidine, T-593

Chemical Name: (?-1-[2-Hydroxy-2-(4-hydroxyphenyl)ethyl]-2-(methylsulfonyl)-3-[2-[5-(methylaminomethyl)furan-2-ylmethylthio]ethyl]guanidine
CAS No. 140695-21-2, 123280-14-8 ((R)-isomer), 123280-13-...
参考文献标题:Amine deriv.and its salts and antiulcer agent containing the same
文献作者:Hirai,S.; Hirano,H.; Arai,H.; Shibata,H.; Kusayanagi,Y.; Hashiba,K.(Toyama Chemical Co.,Ltd.)
参考来源:CH 675244; DE 3828869; US 4871765

A-71497

Chemical Name: (?-7-(3-Aminopyrrolidin-1-yl)-1-(2,4-difluorophenyl)-6-fluoro-4-oxo-1,4-dihydro-1,8-naphthyridine-3-carboxaldehyde hydrochloride
CAS No. 134762-03-1
项目整合开发状态: Preclinical
项目研究机...
参考文献标题:Synthesis and biological properties of A-71497: A prodrug of tosufloxacin
文献作者:Swanson,R.N.; Pernet,A.G.; Marsh,K.C.; Chu,D.T.W.; Lico,I.M.; Plattner,J.J.
参考来源:9th Int Symp Fut Trends Chemother 1990,21

Disodium cromproxate, 78012

Chemical Name: 7,7'-[(2-Hydroxytrimethylene)dioxy]bis(4-oxo-4H-1-benzopyran-2-carboxylic acid) disodium salt; 7,7'-[(2-Hydroxy-1,3-propanediyl)bis-(oxy)]bis[4-oxo-4H-1-benzopyran-2-carboxylic acid] di...
参考文献标题:A simplified synthesis of 1,3-bis-(2-carboxychromone-7-oxy)-2-hydroxypropane disodium salt (78012)
文献作者:Liang,X.; Qi,J.; Lu,Y.
参考来源:Acta Pharm Sin 1982,17(2),143-5

BN-50739

Chemical Name: 6-(2-Chlorophenyl)-9-[(3,4-dimethoxyphenylthiomethyl)thiocarbonyl]-1-methyl-7,8,9,10-tetrahydro-4H-pyrido[4',3'-4,5]thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepine
CAS No. 128672-0...
参考文献标题:Thieno-triazolo-diazepine derivs.and process for their preparation
文献作者:Braquet,P.; Esanu,A.; Laurent,J.-P.; Pommier,J.(SCRAS (Societ?de Conseils de Recherches et d'Applications Scientifiques))
参考来源:BE 1004122; CH 681009; DE 4015137; FR 2646774; FR 2646851; GB 2231330; JP 1991005484; US 5049559

RU-47067

Chemical Name: 5-(1-Methylethoxy)-1-[[3-(trifluoromethyl)phenyl]sulfonyl]-2-pyrrolidinone; 5-Isopropoxy-1-[[3-(trifluoromethyl)phenyl]sulfonyl]pyrrolidin-2-one
CAS No. 111711-92-3
项目整合开发状态: Prec...
参考文献标题:RU-47067
文献作者:Toja,E.; Galliani,G.
参考来源:Drugs Fut 1991,16(4),321

KW-3635

Chemical Name: (E)-11-[2-(5,6-Dimethyl-1-benzimidazolyl)ethylidene]-6,11-dihydrodibenz[b,e]oxepine-2-carboxylic acid sodium salt monohydrate
CAS No. 127166-41-0 (anhydrous), 127166-39-6 (anhydrous ...
参考文献标题:Tricyclic cpds
文献作者:Oshima,E.; Obase,H.; Karasawa,A.; Kubo,K.; Miki,I.; Ishii,A.(Kyowa Hakko Kogyo Co.,Ltd.)
参考来源:EP 0345747; JP 1990091040; US 4999363; US 5118701; US 5242931; US 5302596

U-50488 hydrochloride

Chemical Name: trans-2-(3,4-Dichlorophenyl)-N-methyl-N-(2-pyrrolidinocyclohexyl)acetamide hydrochloride
CAS No. 67197-96-0, 67198-13-4 (free base)
项目整合开发状态: Preclinical
项目研究机构: Pfizer (Origin...
参考文献标题:2-Aminocycloaliphatic amide compounds
文献作者:Szmuszkovicz,J.
参考来源:DE 2749950; ES 463876; FR 2370723; GB 1569225; JP 53063351; JP 61233654; US 4145435

FG-5803

Chemical Name: N-Cyclohexyl-4-[4-(4-fluorophenyl)-4-oxobutyl]-1-piperazinecarboxamide hydrochloride
CAS No. 97507-92-1
项目整合开发状态: Preclinical
项目研究机构: Pfizer (Originator)
合成路线:FG5803 is obta...
参考文献标题:Novel 1-piperazinecarboxamide derivs.
文献作者:Bjork,A.; Fex,T.; Olsson,K.; Abramo,A.; Gustafsson,B.; Christensson,E.(Ferrosan AB)
参考来源:EP 0136274; ES 8704917; ES 8705411; ES 8802039; JP 1985501956; US 4935419; WO 8500811