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:532061

Chemical Name: N-[2-(1-Benzyl-4-piperidinyl)ethyl]-6-phenylpyridazin-3-amine dihydrochloride hydrate
CAS No. 221196-21-0 (anhydrous), 221196-76-5 (free base)
项目整合开发状态: Biological Testing
项目研究...
参考文献标题:Aminopyridazines as acetylcholinesterase inhibitors
文献作者:Contreras,J.M.; Rival,Y.M.; Chayer,S.; Bourguignon,J.J.; Wermuth,C.G.
参考来源:J Med Chem 1999,42(4),730

LG-100324

Chemical Name: (Z)-4-[(Hydroxyimino)(3,5,5,8,8-pentamethyl-5,6,7,8-tetrahydronaphthalen-2-yl)methyl]benzoic acid
CAS No. 221343-42-6
项目整合开发状态: Preclinical
项目研究机构: Ligand (Originator)
合成路线:...
参考文献标题:Synthesis and structure-activity relationships of novel retinoid X receptor-selective retinoids
文献作者:Boehm,M.F.; Zhang,L.; Badea,B.A.; White,S.K.; Mais,D.E.; Berger,E.; Suto,C.M.; Goldman,M.E..; Heyman,R.A.
参考来源:J Med Chem 1994,37(18),2930

新产品编号:293179

Chemical Name: 1-[4-[3-(3,5-Difluorophenyl)-2-propynyloxy]-1,2,5-thiadiazol-3-yl]-4-azatricyclo[2.2.1.0(2,6)]heptane oxalate
CAS No. 198143-43-0, 198143-42-9 (free base), 198143-54-3 (HCl)
项目整合开...
参考文献标题:Heterocyclic cpds.and their preparation and use
文献作者:Jeppesen,L.; Olesen,P.H.; Sauerberg,P.(Novo Nordisk A/S)
参考来源:EP 0891363; JP 1999509864; US 5914338; WO 9736906

SCH-206272

Chemical Name: N-[3(R)-(3,4-Dichlorophenyl)-5-[4-[3(R)-(N-methylcarbamoylmethyl)-2-oxopiperidin-1-yl]piperidin-1-yl]-2(Z)-(methoxyimino)pentyl]-N-methyl-3,5-dichlorobenzamide
CAS No. 226915-43-1, 2...
参考文献标题:Substd.oximes as neurokinin antagonists
文献作者:Carruthers,N.I.; Alaimo,C.A.; Shih,N.-Y.; Lavey,B.J.; Ting,P.C.; Reichard,G.A.(Schering Corp.)
参考来源:EP 1032561; WO 9926924

Reveromycin B

Chemical Name: (-)-(5R)-10-[2(R)-Butyl-2-[5-carboxy-1(S)-(4-hydroxysuccinyloxy)-4-methyl-2(E),4(E)-pentadienyl]-8(S)-methyl-1,6-dioxaspiro[4.5]dec-7(R)-yl]-5(R)-hydroxy-4(S),8-dimethyl-2(E),6(E),8(E)-...
参考文献标题:Total synthesis of (-)-reveromycin B
文献作者:Cuzzupe,A.N.; Hutton,C.A.; Lilly,M.J.; Mann,R.K.; Rizzacasa,M.A.; Zammit,S.C.
参考来源:Org Lett 2000,2(2),191

A-198401

Chemical Name: 11-Amino-3'-N-(cyclopropylmethyl)-3'-N-demethyl-11-deoxy-3-O-deshexopyranosyl-11-[2-(3,4-dichlorophenyl)ethyl]-6-O-methyl-3-O-[4(S)-methyl-2-oxooxazolidin-3-ylcarbonyl]erythromycin A 11...
参考文献标题:Macrolide LHRH antagonists
文献作者:Waid,P.; Dalton,C.R.; Randolph,J.T.; Greer,J.; Nichols,C.J.; Haviv,F.; Mort,N.A.; Sauer,D.R.(Abbott Laboratories Inc.)
参考来源:WO 0012522

DC-41-33, PRL-2903

Chemical Name: (4-Fluoro)-L-phenylalanyl-D-cysteinyl-(3-pyridyl)-L-alanyl-D-tryptophyl-L-lysyl-(3-methyl)-L-valyl-L-cysteinyl-(2-naphthyl)-L-alaninamide cyclic (2-7)-disulfide
CAS No. 209006-13-3 参考文献标题:Somatostatin antagonists
文献作者:Murphy,W.; Coy,D.H.; Morgan,B.(Biomeasure Inc.; Tulane Educational Fund)
参考来源:WO 9824807

WAY-133537

Chemical Name: 4-[3,4-Dioxo-2-[1(R),2,2-trimethylpropylamino]-1-cyclobuten-1-ylamino]-3-ethylbenzonitrile
CAS No. 177476-74-3
项目整合开发状态: Preclinical
项目研究机构: Wyeth Pharmaceuticals (Originator)<...
参考文献标题:Design and SAR of novel potassium channel openers targeted for urge urinary incontinence.I.N-Cyanoguanidine bioisosteres possessing in vivo bladder selectivity
文献作者:Butera,J.A.; Antane,M.M.; Antane,S.A.; Argentieri,T.M.; Freeden,C.; Graceffa,R.F.; Hirth,B.H.; Jenkins,D.; Lennox,J.R.; Matelan,E.; Norton,N.W.; Quagliato,D.; Sheldon,J.H.; Spinelli,W.; Warga,D.; Wojdan,A.; Woods,M.
参考来源:J Med Chem 2000,43(6),1187-1202

新产品编号:565283

Chemical Name: (-)-(3S,4S,6R,11S,11Sa)-4-Azido-11-bromo-11-methyl-3,6-epoxyperhydropyrimido[6,1-b][1,3]oxacine-8,10-dione; 3'-Azido-5(S)-bromo-3'-deoxy-6(S)-hydroxy-5',6-anhydrothymidine
CAS No. 22...
参考文献标题:Synthesis,lipophilicity and anti-HIV activity of a new brominated analog of zidovudine
文献作者:Motura,M.; Salomon,H.; Moroni,G.; Wainberg,M.; Brinon,M.C.
参考来源:Nucleosides Nucleotides 1999,18(3),337

新产品编号:73281

Chemical Name: (-)-3-[4-[2-[N-(2-Benzoxazolyl)-N-methylamino]ethoxy]phenyl]-2(S)-methoxypropionic acid
CAS No. 158062-26-1
项目整合开发状态: Preclinical
项目研究机构: GlaxoSmithKline (Originator)
合成路线:R...
参考文献标题:Heterocyclic cpds.as pharmaceutical
文献作者:Haigh,D.; Sime,J.(SmithKline Beecham plc)
参考来源:EP 1000938; US 5869495; US 6048883; WO 9401420