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

新产品编号:403919

Chemical Name: 2(R)-[4-(5-Chloro-2-pyridinyl)-1-piperazinylsulfonamido]-N-hydroxy-3-methylbutyramide
CAS No. 210913-38-5
项目整合开发状态: Preclinical
项目研究机构: Agouron (Originator), Roche (Originator)...
参考文献标题:Sulfamide-metalloprotease inhibitors
文献作者:Castelhano,A.L.; Hendricks,R.T.; Melnick,M.J.; Campbell,J.A.; Walker,K.A.M.; Broka,C.A.; Chen,J.J.(Agouron Pharmaceuticals,Inc.; F.Hoffmann-La Roche AG)
参考来源:DE 19802350; EP 0958287; US 5998412; WO 9832748

新产品编号:483019

Chemical Name: (3S,9S,12S,15R,18S)-15-(Cyclohexylmethyl)-9-(3-guanidinopropyl)-12-(1H-indol-3-ylmethyl)-3-(L-phenylalanylamino)-1,7,10,13,16-pentaazabicyclo[16.3.0]henicosane-2,8,11,14,17-pentaone
...
参考文献标题:Effects of a new C5a receptor antagonist on C5a- and endotoxin-induced neutropenia in the rat
文献作者:Short,A.; Wong,A.K.; Finch,A.M.; Haaima,G.; Shiels,I.A.; Fairlie,D.P.; Taylor,S.M.
参考来源:Br J Pharmacol 1999,126(3),551

PF-9404C, PF-9404

Chemical Name: 1-[4-[2(S),3-Bis(nitrooxy)propoxymethyl]phenoxy]-3-(isopropylamino)propan-2(S)-ol
CAS No. 164340-32-3 (undefined isomer)
项目整合开发状态: Preclinical
项目研究机构: Almirall Prodesfarma (Ori...
参考文献标题:1-Aryloxy-3-alkylamino-2-propanol nitrate esters,the use thereof and corresponding pharmaceutical compsn.
文献作者:Prat Quinones,M.; Pi Sallent,J.; Vedrilla Veit,D.(Almirall Prodesfarma,SA)
参考来源:EP 0637583; JP 1995089910

新产品编号:490929

Chemical Name: 1-[5,6-Diethoxy-2-(methylsulfanyl)-1H-benzimidazol-1-yl]-1-(4-thiazolyl)methanone
CAS No. 219866-44-1
项目整合开发状态: Preclinical
项目研究机构: Kaunas Medical University (Originator), Viln...
参考文献标题:Synthesis and positive inotropic effects of 1-acyl-5,6-diethoxy-2-methylthiobenzimidazoles
文献作者:Brukstus,A.; Dauksas,V.; Garaliene,V.; Labanauskas,L.
参考来源:Arzneim-Forsch Drug Res 1998,48(12),1137

KP9

Chemical Name: 3-(2,2,2-Trifluoroethoxy)phenoxathiin-10,10-dioxide
CAS No. 205187-44-6
项目整合开发状态: Preclinical
项目研究机构: Krenitsky (Originator)
合成路线:The condensation of 2-hydroxythiophenol (I)...
参考文献标题:Pharmacologically active cpds.and use
文献作者:Boros,E.; Harfenist,M.; Heyer,D.(Krenitsky Pharmaceuticals,Inc.)
参考来源:WO 9812190

1346W95

Chemical Name: 3-[1-(Difluoromethyl)-2,2-difluoroethoxy]phenoxathiin-10,10-dioxide
CAS No. 205187-46-8
项目整合开发状态: Preclinical
项目研究机构: Krenitsky (Originator)
合成路线:The condensation of 2-hydro...
参考文献标题:Pharmacologically active cpds.and use
文献作者:Boros,E.; Harfenist,M.; Heyer,D.(Krenitsky Pharmaceuticals,Inc.)
参考来源:WO 9812190

新产品编号:87519

Chemical Name: 2-[3-[4-(3-Chlorophenyl)-2(S)-methylpiperazinyl]propyl]-1,2,4-triazolo[4,3-a]pyridin-3(2H)-one L-(+)-tartrate
CAS No. 161968-03-2, 161905-64-2 (free base), 161968-06-5 (maleate salt ...
参考文献标题:Pharmacologically active enantiomers
文献作者:Baiocchi,L.; Cioli,V.(Angelini Group)
参考来源:EP 0707587; JP 1996512036; WO 9501354

MEN-11575

Chemical Name: (2S,3aS,7aS)-1-[2-[11-(D-Arginyl-L-arginylamino)undecanoyl-L-seryl]-1,2,3,4-tetrahydroisoquinolin-3(R)-ylcarbonyl]perhydroindole-2-carboxylic acid
CAS No. 222165-43-7
项目整合开发状态: Bi...
参考文献标题:A new class of pseudopeptide antagonists of the kinin B1 receptor containing alkyl spacers
文献作者:Galoppini,C.; Meini,S.; Tancredi,M.; Di Fenza,A.; Triolo,A.; Quartara,L.; Maggi,C.A.; Formaggio,F.; Toniolo,C.; Mazzucco,S.; Papini,A.; Rovero,P.
参考来源:J Med Chem 1999,42(3),409

新产品编号:25821

Chemical Name: 5-Hydroxy-2-(3-hydroxy-4-methoxyphenyl)-7-[4-(2,3,4-trimethoxybenzyl)piperazin-1-ylcarbonylmethoxy]-4H-benzopyran-4-one
CAS No. 123580-63-2, 123580-64-3 (methanesulfonate)
项目整合开发状...
参考文献标题:Flavonoid-related modulators of multidrug resistance: Synthesis,pharmacological activity,and structure-activity relationships
文献作者:Fert? J.; K黨nel,J.-M.; Chapuis,G.; Rolland,Y.; Lewin,G.; Schwaller,M.A.
参考来源:J Med Chem 1999,42(3),478

新产品编号:71699

Chemical Name: 2-(5-tert-Butyl-1H-indol-3-yl)-1-ethanamine
CAS No. 156941-66-1 (hydrochloride)
项目整合开发状态: Biological Testing
项目研究机构: Lilly (Originator), Synaptic (Originator)
合成路线:Diazotiza...
参考文献标题:Method for treating 5HT2B receptor related conditions
文献作者:Audia,J.E.; Cohen,M.L.; Gidda,J.S.; Nelson,D.L.G.; Baker,S.R.; Ezquerra-Carrera,J.; Lamas-Peteira,C.; Pedregal-Tercero,C.(Eli Lilly and Company)
参考来源:EP 0749313; JP 1997510216; US 5663178; WO 9524200; WO 9624351