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

MG-2394

Chemical Name: 5,7-Dichloro-1-benzothien-2-ylsulfonamidomethylphosphonic acid 4-nitrophenyl monoester
CAS No. 318461-32-4
项目整合开发状态: Preclinical
项目研究机构: MethylGene (Originator)
合成路线:Alkylat...
参考文献标题:Sulfonamidomethyl phosphonate inhibitors of beta-lactamase
文献作者:Delorme,D.; Besterman,J.M.; Rahil,J.(MethylGene Inc.)
参考来源:EP 1194436; WO 0102411

AM-113

Chemical Name: (5R,6R)-2-tert-Butyl-6-[1(R)-hydroxyethyl]-1-oxa-2-penem-3-carboxylic acid potassium salt
CAS No. 155899-36-8, 150407-34-4 (diastereomer), 150407-32-2 (free acid), 157086-87-8 (Na sa...
参考文献标题:Synthesis and antibacterial activity of 1'R,5R,6R)-2-tert-butyl-6-(1'hydroxyethyl)oxapenem-3-carboxylic acid
文献作者:Pfaendler,H.R.; Weisner,F.
参考来源:Bioorg Med Chem Lett 1993,3(11),2211

XOB, AM-114

Chemical Name: (5R,6R)-2-tert-Butyl-6-[1(S)-hydroxyethyl]-1-oxa-2-penem-3-carboxylic acid potassium salt
CAS No. 150407-29-7, 150407-34-4 (diastereomer), 155899-36-8 (diastereomer)
项目整合开发状态: Bio...
参考文献标题:(1'S)-Hydroxyalkyloxapenem-3-carboxylic acids and their use as beta-lactamase inhibitors
文献作者:Pfaendler,H.R.(Eli Lilly and Company)
参考来源:DE 4142423; EP 0548790

PNU-253998

Chemical Name: N-(4-Chlorobenzyl)-1-(4-morpholinyl)-6-(morpholin-4-ylmethyl)-4-oxo-1,4-dihydroquinoline-3-carboxamide
CAS No. 281651-76-1
项目整合开发状态: Preclinical
项目研究机构: Pfizer (Originator)
...
参考文献标题:Quinolinecarboxamides as antiviral agents
文献作者:Thaisrivongs,S.; Strohbach,J.W.; Turner,S.R.; Vaillancourt,V.A.; Tucker,J.A.; Schnute,M.E.(Pharmacia Corp.)
参考来源:EP 1140850; US 6248739; WO 0040561

PNU-276484

Chemical Name: N-(4-Chlorobenzyl)-1-(4-methylpiperazin-1-yl)-6-(morpholin-4-ylmethyl)-4-oxo-1,4-dihydroquinoline-3-carboxamide
CAS No. 281651-77-2
项目整合开发状态: Preclinical
项目研究机构: Pfizer (Origin...
参考文献标题:Quinolinecarboxamides as antiviral agents
文献作者:Thaisrivongs,S.; Strohbach,J.W.; Turner,S.R.; Vaillancourt,V.A.; Tucker,J.A.; Schnute,M.E.(Pharmacia Corp.)
参考来源:EP 1140850; US 6248739; WO 0040561

GSQ-1530

Chemical Name: N-[5-[N-[5-[N-[5-[N-(2-Amidinoethyl)carbamoyl]-1-methyl-1H-pyrrol-3-yl]carbamoyl]-1-methyl-1H-pyrrol-3-yl]carbamoyl]-1-methyl-1H-pyrrol-3-yl]-4,5-dichloroisothiazole-3-carboxamide aceta...
参考文献标题:HARP: A novel class of antibiotics
文献作者:Burli,R.; et al.
参考来源:41st Intersci Conf Antimicrob Agents Chemother (Dec 16 2001,Chicago) 2001,Abst F-1685

UR-8962

Chemical Name: 4-[4-(Methylsulfonyl)phenyl]-3-[6-(1-pyrrolidinyl)pyridin-3-yl]furan-2(5H)-one
CAS No. 372107-53-4
项目整合开发状态: Preclinical
项目研究机构: Uriach (Originator)
合成路线:6-Chloronicotinic a...
参考文献标题:Novel heterocyclic cpds.with anti-inflammatory activity
文献作者:Almansa Rosales,C.; Gonzalez Gonzalez,C.; Torres Barreda,M.C.(J.Uriach & C韆.,SA)
参考来源:EP 1281709; ES 2166710; WO 0183475

CDD-0273, CDD-0273-A

Chemical Name: 3,3'-Oxybis(ethyleneoxy)bis(ethyleneoxy)bis[4-(1-methyl-1,2,5,6-tetrahydropyridin-3-yl)-1,2,5-thiadiazole] dihydrochloride
CAS No. 331468-03-2, 331241-45-3 (free base)
项目整合开发状态: B...
参考文献标题:Muscarinic receptor agonists
文献作者:Cao,Y.; Rajeswaran,W.G.; Messer,W.S.(University of Toledo)
参考来源:US 6211204

GW-581506X, PL-1023

Chemical Name: 3-Des(hexopyranosyloxy)-6-O-methyl-3-oxo-8a-aza-8a-homoerythromycin A
CAS No. 244606-14-2
项目整合开发状态: Preclinical
项目研究机构: Pliva (Originator), GlaxoSmithKline (Codevelopment)
合...
参考文献标题:15-Membered lactams ketolides with antibacterial activity
文献作者:Kobrehel,G.; Lazarevski,G.; Kelneric,Z.(Pliva dd)
参考来源:EP 1070077; JP 2002510701; US 6110965; WO 9951616

GW-587726X, PL-1441

Chemical Name: 3-Des(hexopyranosyloxy)-6-O-methyl-3-[2-(4-nitrophenyl)acetoxy]-8a-aza-8a-homoerythromycin A
CAS No. 301151-61-1
项目整合开发状态: Preclinical
项目研究机构: Pliva (Originator), GlaxoSmithKli...
参考文献标题:15-Membered lactams ketolides with antibacterial activity
文献作者:Kobrehel,G.; Lazarevski,G.; Kelneric,Z.(Pliva dd)
参考来源:EP 1070077; JP 2002510701; US 6110965; WO 9951616