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

Isofloxythepin

4-[3-氟-10,11-二氢-8-异丙基二苯并[b,f]硫杂卓-10-基]哌嗪-1-乙醇Chemical Name: 4-[3-Fluoro-10,11-dihydro-8-(1-methylethyl)dibenzo[b,f]thiepin-10-yl]-1-piperazineethanol; 3-Fluoro-10-[4-(2-hydroxyethyl)piperazinyl]-8-iso...
参考文献标题:3-Fluoro-10-piperazino-8-substituted 10,11-dihydrodibenzo(bf) thiepins and method for the preparation thereof
文献作者:Dlabac,A.; Miksik,F.; Pomykacek,J.; Jilek,J.; Sindelar,K.; Rajsner,M.; Langsadl,L.; Metysova,J.; Bartl,V.; Protiva,M.(SPOFA - United Pharmaceutical Works)
参考来源:BE 0872496; DE 2855703; FR 2412312; GB 2010843; JP 7992979; US 4243805

SB-431542

4-[4-(1,3-苯并二唑-5-基)-5-(2-吡啶基)-1H-咪唑-2-基]-苯酰胺水合物Chemical Name: 4-[4-(1,3-Benzodioxol-5-yl)-5-(2-pyridyl)-1H-imidazol-2-yl]benzamide
CAS No. 301836-41-9
项目整合开发状态: Preclinical
项目研究机构: GlaxoSmith...
参考文献标题:Triarylimidazoles
文献作者:Callahan,J.F.; Burgess,J.L.(GlaxoSmithKline Inc.)
参考来源:EP 1169317; JP 2002541253; US 6465493; WO 0061576

Flobufen, VUFB-16066

4-[4-(2,4-二氟苯基)苯基]-2-甲基-4-氧代丁酸 2,4-二氟-α-甲基-γ-氧-(1,1-双苯)-4-丁酸 Chemical Name: 4-(2',4'-Difluorobiphenylyl)-4-oxo-2-methylbutanoic acid; 3-[4-(2,4-Difluorophenyl)benzoyl]-2-methylpropionic acid; gamma-Ox...
参考文献标题:omega-(2',4'-Dihalobiphenylyl)oxoalkanoic acid derivs.
文献作者:Kuchar,M.; Brunova,B.; Grimova,J.; Maturova,E.(SPOFA - United Pharmaceutical Works)
参考来源:CS 243570; EP 0180290; JP 1986065842; US 4683331

L-770644

4-[4-(3-环戊基丙基)-5-羰基-4,5-二氢-1H-四唑-1-基]-N-[4-[2-[2(R)-羟基-2-(3-吡啶基)乙胺基]乙基]苯基]苯磺酰胺Chemical Name: 4-[4-(3-Cyclopentylpropyl)-5-oxo-4,5-dihydro-1H-tetrazol-1-yl]-N-[4-[2-[2(R)-hydroxy-2-(3-pyridyl)ethylamin...
参考文献标题:Substd.sulfonamides as selective beta3 agonists for the treatment of diabetes and obesity
文献作者:Fisher,M.H.; Naylor,E.M.; Ok,D.; Weber,A.E.; Shih,T.; Ok,H.(Merck & Co.,Inc.)
参考来源:EP 0757674; JP 1997512275; US 5541197; US 5561142; WO 9529159

Syn-2869

4-[4-[(1R,2R)-2-(2,4-二氟苯基)-2-羟基-1-甲基-3-(1H-1,2,4-三唑-1-基)丙基]-1-哌拉嗪基]-2-[4-(三氟甲氧基)苯基]-2-[4-(三氟甲氧基)苯]-2,4-二氢-3H-1,2,4-三唑-3-一Chemical Name: 4-[4-[4-[(1R,2R)-2-(2,4-Difluorophenyl)-2-hydroxy-1-methyl-3-(1H...
参考文献标题:New triazoles as therapeutic agents for fungal infections
文献作者:Ha,C.; Unemi,N.; Nguyen,D.; Furukawa,T.; Sidhu,I.; Daneshtalab,M.; Bathini,Y.; Micetich,R.; Khan,J.; Abel,M.; Salama,S.(Synphar Laboratories Inc.; Taisho Pharmaceutical Co.,Ltd.)
参考来源:EP 0889881; JP 2000507275; WO 9831675

BMS-229724

4-[4-[2-[2-[双(4-氯苯基)甲氧基]乙基磺酰]乙氧基]苯基]-1,1,1-三氟丁烷-2-1Chemical Name: 4-[4-[2-[2-[Bis(4-chlorophenyl)methoxy]ethylsulfonyl]ethoxy]phenyl]-1,1,1-trifluorobutan-2-one
CAS No. 221914-85-8
项目整合开发状态: Pre...
参考文献标题:Selective cPLA2 inhibitors
文献作者:Banville,J.; Burke,J.R.; Gai,Y.; Johnson,G.; Zusi,F.C.(Bristol-Myers Squibb Co.)
参考来源:EP 1140791; WO 9915129

Cimicoxib, UR-8880

4-[4-氯-5-(3-氟-4-甲氧基苯基)-1H-咪唑-1-基]苯磺酰胺Chemical Name: 4-[4-Chloro-5-(3-fluoro-4-methoxyphenyl)-1H-imidazol-1-yl]benzenesulfonamide
CAS No. 265114-23-6
项目整合开发状态: Phase II
项目研究机构: Uriach (Origina...
参考文献标题:Novel imidazoles with anti-inflammatory activity
文献作者:Almansa,C.; Torres,M.C.; Gonzalez,C.(J.Uriach & C韆.,SA)
参考来源:EP 1122243; JP 2002527508; WO 0023426

SC-58236, SC-236

4-[5-(4-氯苯基)-3-(三氟甲基)吡唑-1-基]苯磺酰胺Chemical Name: 4-[5-(4-Chlorophenyl)-3-(trifluoromethyl)pyrazol-1-yl]benzenesulfonamide
CAS No. 170569-86-5, 251972-30-2
项目整合开发状态: Preclinical
项目研究机构: Pfizer (...
参考文献标题:Synthesis and biological evaluation of the 1,5-diarylpyrazole class of cyclooxygenase-2 inhibitors: Identification of 4-[5-(4-methylphenyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl]benzenesulfonamide (SC-58635,celecoxib)
文献作者:Penning,T.D.; Bertenshaw,S.R.; Talley,J.J.; Carter,J.S.; Collins,P.W.; Docter,S.; Graneto,M.J.; Lee,L.F.; Malecha,J.W.; Miyashiro,J.M.; Rogers,R.S.; Rogier,D.J.; Yu,S.S.; Anderson,G.D.; Burton,E.G.; Cogburn,J.N.; Gregory,S.A.; et al.
参考来源:J Med Chem 1997,40(9),1347

FK-838

4-[6-氧代-3-(2-苯基吡唑并[1,5-a]吡啶-3-基)哒嗪-1-基]丁酸Chemical Name: 3-[2-(3-Carboxypropyl)-3-oxo-2,3-dihydropyridazin-6-yl]-2-phenylpyrazolo[1,5-a]pyridine; 4-[6-Oxo-3-(2-phenylpyrazolo[1,5-a]pyridin-3-yl)-1,6-di...
参考文献标题:Efficient large-scale synthesis of 4-phenyl-3-butyn-2-one,a key intermediate for a novel potent adenosine antagonist
文献作者:Zanka,A.
参考来源:Org Process Res Dev 1998,2(1),60

新产品编号:377025

4-[8-(3-硝基苯基)-1,7-萘啶-6-基]苯甲酸Chemical Name: 4-[8-(3-Nitrophenyl)-1,7-naphthyridin-6-yl]benzoic acid
CAS No. 207279-23-0
项目整合开发状态: Preclinical
项目研究机构: Novartis (Originator)
合成路线:Reaction of ...
参考文献标题:Naphtyridine derivs.
文献作者:Hersperger,R.(Novartis AG)
参考来源:EP 0934320; US 6136821; WO 9818796