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

Sparfosic acid, USNUS-08, CI-882(disodium salt), PALA, NSC-224131

N-(2-膦酰乙酰基)-L-天冬氨酸二钠(3S)-4-羟基-3-[(1-氧化-2-膦乙基)氨基]-4-氧丁酸盐 Chemical Name: N-(Phosphonoacetyl)-L-aspartate
CAS No. 51321-79-0, 66569-27-5 (diNa salt)
项目整合开发状态: Phase III
项目研究机构: Pfizer (Originat...
参考文献标题:PALA
文献作者:Blancafort,P.; Castar,J.; Kuhn,J.; Serradell,M.N.; Magnuson,D.
参考来源:Drugs Fut 1981,6(3),152

GW-1929

N-(2-苯甲酰基苯基)-O-[2-(甲基-2-吡啶基氨基)乙基]-L-酪氨酸酪氨酸,N-(2-苯甲酰苯基)-O-[2-(甲基-2-吡啶基氨基)乙基]-Chemical Name: 2(S)-(2-Benzoylanilino)-3-[4-[2-[N-methyl-N-(2-pyridinyl)amino]ethoxy]phenyl]propionic acid; N-(2-Benzoypheny...
参考文献标题:Substd.4-hydroxy-phenylalkanoic acid derivs.with agonist activity to PPAR-gamma
文献作者:Willson,T.M.; Mook,R.A.Jr.; Kaldor,I.; Henke,B.R.; Deaton,D.N.; Collins,J.L.; Cobb,J.E.; Brackeen,M.; Sharp,M.J.; O'Callaghan,J.M.; Erickson,G.A.; Boswell,G.E.(Glaxo Wellcome plc)
参考来源:EP 0888317; JP 2000507216; WO 9731907

Farglitazar, GI-262570

N-(2-苯甲酰苯基)-O-2-(5-甲基-2-苯基-4-羟基唑)乙基-L-酪氨酸Chemical Name: 2(S)-(2-Benzoylphenylamino)-3-[4-[2-(5-methyl-2-phenyloxazol-4-yl)ethoxy]phenyl]propionic acid; N-(2-Benzoylphenyl)-O-[4-[2-(5-methyl-2-phenylox...
参考文献标题:Substd.4-hydroxy-phenylalkanoic acid derivs.with agonist activity to PPAR-gamma
文献作者:Willson,T.M.; Mook,R.A.Jr.; Kaldor,I.; Henke,B.R.; Deaton,D.N.; Collins,J.L.; Cobb,J.E.; Brackeen,M.; Sharp,M.J.; O'Callaghan,J.M.; Erickson,G.A.; Boswell,G.E.(Glaxo Wellcome plc)
参考来源:EP 0888317; JP 2000507216; WO 9731907

S-20928

N-(2-萘-1-基乙基)环丁烷甲酰胺Chemical Name: N-[2-(1-Naphthyl)ethyl]cyclobutanecarboxamide
CAS No. 152302-33-5
项目整合开发状态: Preclinical
项目研究机构: ADIR (Originator)
合成路线:Reduction of 1-naphthylacetonitrile...
参考文献标题:Synthesis and structure-activity relationships of novel naphthalenic and bioisosteric related amidic derivatives as melatonin receptor ligands
文献作者:Leclerc,V.; Fourmaintraux,E.; Depreux,P.; Lesieur,D.; Morgan,P.; Howell,H.E.; Renard,P.; Caignard,D.H.; Pfeiffer,B.; Delagrange,P.; Guardiola-Lemaitre,B.; Andrieux,J.
参考来源:Bioorg Med Chem 1998,6(10),1875

MR-827, YS-035

N-(3,4-二甲氧基苯乙基)-2-(3,4-二甲氧基苯基)-N-甲基乙-1-胺Chemical Name: N,N-Bis[2-(3,4-dimethoxyphenyl)ethyl]methylamine hydrochloride; 3,3',4,4'-Tetramethoxy-N-methyldiphenethylamine hydrochloride
CAS No. 33978-72...
参考文献标题:Compounds having calcium blocking activity
文献作者:Quadro,G.; Cahn,J.(SIR International SA; Yason Srl)
参考来源:BE 0897244; CA 431900; CH 3684839; DE 33247277; ES 524353; GB 2216213; IT 20838; IT 22339; JP 83125363; NL 832451; ZA 834975

SB-399885

N-(3,5-二氯-2-甲氧基苯基)-4-甲氧基-3-(1-哌嗪基)苯磺酰胺盐酸盐N-(3,5-二氯-2-甲氧基苯基)-4-甲氧基-3-(1-哌嗪基)苯磺酰胺盐酸盐Chemical Name: N-(3,5-Dichloro-2-methoxyphenyl)-4-methoxy-3-(1-piperazinyl)benzenesulfonamide
CAS No. 402713-80-8,...
参考文献标题:N-(3,5-Dichloro-2-methoxyphenyl)-4-methoxy-3-piperazin-1-yl-benzenesulfonamide
文献作者:Bromidge,S.M.; Moss,S.F.(GlaxoSmithKline plc)
参考来源:EP 1313720; WO 0218358

Indisulam, E-7070, ER-35744

N-(3-氯-1H-吲哚-7-基)-1,4-苯二磺酰胺Chemical Name: N-(3-Chloroindol-7-yl)benzene-1,4-disulfonamide
CAS No. 165668-41-7
项目整合开发状态: Phase II
项目研究机构: Eisai (Originator), Abbott (Licensee)
合成路线:The reac...
参考文献标题:Bicyclic heterocyclic sulfonamide and sulfonic ester derivs.
文献作者:Yoshino,H.; Yamato,T.; Okauchi,T.; Yoshimatsu,K.; Sugi,N.; Nagasu,T.; Ozawa,Y.; Koyanagi,N.; Kito,K.(Eisai Co.,Ltd.)
参考来源:EP 0673937; US 5721246; WO 9507276

ACC-789, ZK-202650, NVP-ACC-789

N-(3-溴-4-甲基苯基)-4-(4-吡啶甲基)-1-酞嗪胺Chemical Name: N-(3-Bromo-4-methylphenyl)-4-(pyridin-4-ylmethyl)phthalazin-1-amine
CAS No. 300842-64-2
项目整合开发状态: Preclinical
项目研究机构: Novartis (Originator), Sche...
参考文献标题:Phthalazines with angiogenesis inhibiting activity
文献作者:Altmann,K.-H.; Mett,H.; Wood,J.; Stover,D.R.; Frei,J.; Bold,G.; Traxler,P.(Novartis AG)
参考来源:EP 0970070; WO 9835958

SB-568849

N-(4-(2-(二乙胺基)乙氧基)-3-甲氧基苯基)-N-甲基-4'-(三氟甲基)-[1,1'-双苯]-4-羧酰胺Chemical Name: N-[4-[2-(Diethylamino)ethoxy]-3-methoxyphenyl]-N-methyl-4'-(trifluoromethyl)biphenyl-4-carboxamide
CAS No. 395679-53-5
项目...
参考文献标题:Carboxamide cpds.and their use as antagonists of a human 11CBy receptor
文献作者:Stemp,G.; Johnson,C.N.; Jones,M.; O'Toole,C.A.; Thewlis,K.M.; Witty,D.(GlaxoSmithKline plc)
参考来源:EP 1305304; WO 0210146

Palmitoyl cytarabine, Palmitoyl Ara-C

N(4)-棕榈酰阿糖胞苷Chemical Name: N4-Palmitoyl-1-beta-D-arabinofuranosylcytosine; N4-Hexadecanoyl-1-beta-D-arabinofuranosylcytosine; N-(1-beta-D-Arabinofuranosyl-1,2-dihydro-2-oxo-4-pyrimidinyl)hexadecanamid...
参考文献标题:N4-Acylarabinonucleosides and the preparation thereof
文献作者:Ishida,T.; et al.(Asahi Chemical Industry Co.,Ltd.)
参考来源:DE 2426304