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

4-Iodopropofol

4-碘-2,6-双(1-甲基乙基)苯酚Chemical Name: 4-Iodo-2,6-diisopropylphenol
CAS No. 169255-48-5
项目整合开发状态: Preclinical
项目研究机构: Cornell University (Originator), Universit?degli Studi di Bari (Originator), U...
参考文献标题:Use derivatives of 2,4-bisubstituted phenols as 5-lipoxigenase inhibitors
文献作者:Bonal,J.; et al.(Bobel246 SL)
参考来源:WO 9521610

NIBA, AntiPARP-2, INO2BA

4-碘-3-硝基-苯甲酰胺Chemical Name: 4-Iodo-3-nitrobenzamide
CAS No. 160003-66-7
项目整合开发状态: IND Filed
项目研究机构: Octamer (Originator)
合成路线:The title benzamide derivative was prepared from 4-iodo-3-nitr...
参考文献标题:Novel aromatic and nitroso cpds.and their metabolites useful as anti-viral and anti-tumor agents
文献作者:Kun,E.; Mendeleyev,J.; Kirsten,E.(Octamer,Inc.)
参考来源:WO 9426730

(?-PPG

4-磷酰基苯甘氨酸Chemical Name: (?-2-Amino-2-(4-phosphonophenyl)acetic acid
CAS No. 120667-15-4, 120667-18-7 (hydrochloride)
项目整合开发状态: Preclinical
项目研究机构: Merck & Co. (Originator), Novartis (Originat...
参考文献标题:Exploration of phenyl-spaced 2-amino-(5-9)-phosphonoalkanoic acids as competitive N-methyl-D-aspartic acid antagonists
文献作者:Bigge,C.F.; et al.
参考来源:J Med Chem 1989,32(7),1580-90

TNP-470, AGM-1470

4-羟基-alpha-((乙基氨基)甲基)-苄醇盐酸盐Chemical Name: 6-O-(Chloroacetylcarbamoyl)fumagillol; [3R,4S(1R,2R),5S,6R]-6-(Chloroacetylcarbamoyloxy)-4-(1,2-epoxy-1,5-dimethyl-4-hexenyl)-5-methoxy-1-oxaspiro[2.5]octane;...
参考文献标题:Fumagillol derivs
文献作者:Kishimoto,S.; Fujita,T.(Takeda Chemical Industries,Ltd.)
参考来源:EP 0359036; EP 0682020; JP 1991007270; US 5164410; US 5166172; US 5180738; US 5698586

Oxfenicine, UK-25842

4-羟基-L-(+)-2-苯基甘氨酸Chemical Name: 2-(4-Hydroxyphenyl)-L-glycine
CAS No. 32462-30-9
项目整合开发状态: Biological Testing
项目研究机构:
合成路线:The condensation of p-anisaldehyde (I) with NaCN and NH4Cl in m...
参考文献标题:
文献作者:Clark,J.C.; Elks,J.
参考来源:BE 795874; CA 1010055; CH 595301; DE 2309180; FR 2173232; GB 1423822; JP 7397801; NL 7302544; US 3775946; US 3976680

TA-270

4-羟基-N-(4-羟基-1-甲基-3-辛氧基-2-氧基-1,2-二氢喹啉-7-基)-3,5-二甲氧基肉桂酸酰胺Chemical Name: 4-Hydroxy-N-(4-hydroxy-1-methyl-3-octyloxy-2-oxo-1,2-dihydroquinolin-7-yl)-3,5-dimethoxycinnamic acid amide; 4-Hydroxy-7-(4-hydro...
参考文献标题:Quinolinone derivs.and antiallergic agents containing the same as effective ingredient
文献作者:Takagaki,H.; Abe,M.; Sakai,M.; Aoki,Y.; Nakanishi,S.; Kimura,N.; Koda,A.(Dainippon Ink & Chemicals,Inc.)
参考来源:EP 0785190; JP 1997255659; US 5942521; US 6114352

BMS-188797

4-脱乙酰基紫杉醇4-甲基碳酸酯Chemical Name: 4-O-Deacetyl-4-O-(methoxycarbonyl)paclitaxel; 3(S)-Benzamido-2(R)-hydroxybenzenepropionic acid (2aR,4S,4aS,6R,9S,11S,12S,12aR,12bS)-6-acetoxy-12-(benzoyloxy)-4,11-dihydr...
参考文献标题:Synthesis and biological evaluation of novel paclitaxel (Taxol) D-ring modified analogs
文献作者:Gunatilaka,A.A.; Ramdayal,F.D.; Sarragiotto,M.H.; Kingston,D.G.I.; Sackett,D.L.; Hamel,E.
参考来源:J Org Chem 1999,64(8),2694

CI-1007, PD-143188

4-苯基-1-[[(1R)-3-苯基-1-环己-3-烯基]甲基]-3,6-二氢-2H-吡啶Chemical Name: (+)-(R)-4-Phenyl-1-(2,3,4,5-tetrahydrobiphenyl-3-ylmethyl)-1,2,3,6-tetrahydropyridine
CAS No. 150013-70-0
项目整合开发状态: Phase II
项目研究机构...
参考文献标题:1,3-Substd.cycloalkenes and cycloalkanes as central nervous system agents
文献作者:Caprathe,B.W.; Downing,D.M.; Jaen,J.C.; Johnson,S.J.; Smith,W.J.III; Wise,L.D.; Wright,J.; Wustrow,D.J.(Pfizer Inc.)
参考来源:EP 0545095; EP 0613465; JP 1995501075; US 5314896; WO 9310092

CI-1040, PD-184352

4-辛基酚乙氧基化物Chemical Name: 2-(2-Chloro-4-iodophenylamino)-N-(cyclopropylmethoxy)-3,4-difluorobenzamide
CAS No. 212631-79-3
项目整合开发状态: Discontinued
项目研究机构: Pfizer (Originator)
合成路线:The condens...
参考文献标题:4-Bromo or 4-iodo phenylamino benzhydroxamic acid derivs.and their use as MEK inhibitors
文献作者:Tecle,H.; Dudley,D.T.; Bridges,A.J.; Barrett,S.D.; Saltiel,A.R.; Doherty,A.M.(Pfizer Inc.)
参考来源:EP 0993439; WO 9901426

Formestane, 4-Hydroxyandrostenedione, CGP-32349, 4-OHA, Lentaron Depot, Lentaron

4-雄烯-4-醇-3,17-二酮Chemical Name: 4-Hydroxyandrost-4-ene-3,17-dione
CAS No. 566-48-3
项目整合开发状态: Launched-1992
项目研究机构: Novartis (Originator), Kyorin (Licensee)
合成路线:A novel synthetic strategy f...
参考文献标题:Novel approach to the synthesis of the aromatase inhibitor 4-hydroxyandrost-4-ene-3,17-dione (4-OHA)
文献作者:Melo,M.L.S.E.; Neves,A.S.C.; da Silva,E.J.T.
参考来源:J Chem Soc - Perkins Trans I 1996,14(14),1649