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

BOF-12013

Chemical Name: (6S,7S)-7-[2-(2-Aminothiazol-4-yl)-2(Z)-(1,5-dihydroxy-4-oxo-1,4-dihydropyridin-2-ylmethoxyimino)acetamido]-3-[5-(carboxymethyl)-4-methylthiazol-2-ylthiomethyl]-3-isocephem-4-carboxylic...
参考文献标题:Synthesis and structure-activity relationships of cephalosporins,2-isocephems,and 2-oxaisocephems with C-3' or C-7 catechol or related aromatics
文献作者:Tsuji,K.; Tsubouchi,H.; Yasumura,K.; Matsumoto,M.; Ishikawa,H.
参考来源:Bioorg Med Chem 1996,4(12),2135

MLS-337, SDZ-MLS-337, SRI-62834(racemate), SDZ-266337

Chemical Name: (R)-2-[Hydroxy[2-(octadecyloxymethyl)tetrahydrofuran-2-ylmethoxy]phosphinyloxy]-N,N,N-trimethylethylaminium hydroxide inner salt
CAS No. 140147-97-3
项目整合开发状态: Preclinical
项目研究机...
参考文献标题:Enantiomers of 2-tetrahydrofuran derivs.,intermediates therefor and their preparation
文献作者:Estermann,H.; Houlihan,W.J.; Kapa,P.K.; Underwood,R.L.(Novartis AG; Novartis Deutschland GmbH)
参考来源:EP 0462935; JP 1992270276

FOX-988, SDZ-FOX-988

Chemical Name: N-Methoxy-4-pivaloylbenzimidic acid 4-pivaloylbenzoyl anhydride; 4-Pivaloylbenzoic acid 1-(methoxyimino)-1-(4-pivaloylphenyl)methyl ester
CAS No. 139681-18-8
项目整合开发状态: Phase I
...
参考文献标题:N-Oxymidic acid derivs
文献作者:Kapa,P.K.; Lee,G.T.-S.; Nadelson,J.; Simpson,W.R.J.; Sunay,U.B.(Novartis AG; Novartis Deutschland GmbH)
参考来源:EP 0463989; JP 1992230255

Ro-44-2104

Chemical Name: 4'-(N-Allyl-N-methylaminomethyl)-4-biphenylyl-4-bromophenyl ketone
CAS No. 140620-63-9, 140621-14-3 (HCl)
项目整合开发状态: Preclinical
项目研究机构: Roche (Originator)
合成路线:Grignard reag...
参考文献标题:Use of phenylalkylamines for producing cholesterol lowering agents
文献作者:Aebi,J.; Guerry,P.; Jolidon,S.; Morand,O.(F.Hoffmann-La Roche AG)
参考来源:EP 0636367; JP 1995053479; US 5637771

SUN-9221

Chemical Name: 1-[4-[4-(4-Fluorobenzoyl)piperidin-1-yl]butyl]-4(E)-(hydroxyimino)-7-methyl-1,4,5,6,7,8-hexahydropyrrolo[2,3-c]azepin-8-one
CAS No. 136976-16-4
项目整合开发状态: Phase I
项目研究机构: Daiich...
参考文献标题:Synthesis and pharmacological evaluation of pyrroloazepine derivatives as potent antihypertensive agents with antiplatelet aggregation activity
文献作者:Mizuno,A.; Inomata,N.; Miya,M.; Kamei,T.; Shibata,M.; Tatsuoka,T.; Yoshida,M.; Takiguchi,C.; Miyazaki,T.
参考来源:Chem Pharm Bull 1999,47(2),246

MCDF

Chemical Name: 1,3,8-Trichloro-6-methyldibenzofuran
CAS No. 118174-38-2
项目整合开发状态: Preclinical
项目研究机构: University of Texas System (Originator)
合成路线:4-Chloro-2-methylphenol (I) is condensed ...
参考文献标题:MCDF
文献作者:Safe,S.H.
参考来源:Drugs Fut 1992,17(7),564

CB-1267

Chemical Name: 1(S),3(R)-Dihydroxy-20(R)-[5,5,5-trifluoro-4-hydroxy-4-(trifluoromethyl)-2-pentynyloxymethyl]-9,10-secopregna-5(Z),7(E),10(19)-triene; (5Z,7E)-17beta-[1(R)-Methyl-2-[5,5,5-trifluoro-4-h...
参考文献标题:Novel vitamin D analogues
文献作者:Calverley,M.J.; Grue-S鴕ensen,G.; Binderup,E.T.(Leo Pharmaceutical Products Ltd.A/S)
参考来源:EP 0522013; JP 1993505613; US 5374629; WO 9115475

新产品编号:30567

Chemical Name: cis-1,1-Dichloro-2,3-bis(4-methoxyphenyl)cyclopropane; cis-1,1'-(3,3-Dichloro-1,2-cyclopropanediyl)bis(4-methoxybenzene)
CAS No. 126987-63-1, 126987-64-2 (undefined isomer)
项目整合开发...
参考文献标题:Synthesis and biological evaluation of a series of gem-dichlorocyclopropanes as antitumor agents
文献作者:Griffin,M.T.; et al.
参考来源:Anti-Cancer Drug Des 1992,7(1),49

Fabesetron hydrochloride, FK-1052

Chemical Name: (+)-(R)-10-Methyl-7-(5-methyl-1H-imidazol-4-ylmethyl)-6,7,8,9-tetrahydropyrido[1,2-a]indol-6-one hydrochloride
CAS No. 129299-89-4 ((-)-enantiomer, free base), 129299-88-3 ((-)-enant...
参考文献标题:Pyridoindole and processes for preparation thereof
文献作者:Kato,M.; Ito,K.; Takasugi,H.(Fujisawa Pharmaceutical Co.,Ltd.)
参考来源:AU 8941406; EP 0361317; JP 1990117675; US 5141945; US 5173493; US 5290785

Sanfetrinem cilexetil, GV-118819

Chemical Name: (4S,8S,9R,10S)-10-[1(R)-Hydroxyethyl]-4-methoxy-11-oxo-1-azatricyclo[7.2.0.0(3,8)]undec-2-ene-2-carboxylic acid 1-(cyclohexyloxycarbonyloxy)ethyl ester; (1S,5S,8aS,8bR)-1-[1(R)-Hydroxye...
参考文献标题:10-(1-Hydroxyethyl)-11-oxo-1-azatricyclo[7.2.0.0.3,8]undec-2-ene-2-carboxylic acid derivs
文献作者:Tamburini,B.; Perboni,A.; Rossi,T.; Donati,D.; Andreotti,D.; Gaviraghi,G.; Carlesso,R.; Bismara,C.(Glaxo Wellcome plc)
参考来源:AU 9162265; EP 0416953; US 5407931