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

SL-59.1227

Chemical Name: 3-(Cyclopropylcarboxamido)-N-[2-(dimethylamino)ethyl]-4-[4-(5-methyl-1H-imidazol-4-yl)piperidin-1-yl]benzamide
CAS No. 326488-60-2
项目整合开发状态: Preclinical
项目研究机构: Sanofi-Aventis ...
参考文献标题:4-[(1H-Imidazol-4-yl)piperidin-1-yl]anilide derivs.,their preparation and application in therapy
文献作者:Hoornaert,C.; Rouannet,V.; Dellac,G.; Daumas,M.; Adler,M.-A.; Cremer,G.(Sanofi-Synthabo)
参考来源:EP 0991639; WO 9900379

新产品编号:32149

Chemical Name: N-Acetyl-8,9-didehydro-N-demethyl-9-deoxo-6-deoxy-6,9-epoxyerythromycin A
CAS No. 127955-37-7
项目整合开发状态: Biological Testing
项目研究机构: Kitasato Institute (Originator)
合成路线:By tr...
参考文献标题:Motilides,macrolides with gastrointestinal motor stimulating activity.I.O-Substituted and tertiary N-substituted derivatives of 8,9-anhydroerythromycin A 6,9-hemiacetal
文献作者:Tsuzuki,K.; Toyoda,H.; Inatomi,N.; Sunazuka,T.; Omura,S.; Marui,S.; Itoh,Z.
参考来源:Chem Pharm Bull 1989,37(10),2687

CT-5219

Chemical Name: N-Acetyl-4-thia-D-prolyl-[4-O-(2,6-dichlorobenzyl)]-L-tyrosine; N-[3-Acetyl-4(S)-thiazolidinylcarbonyl]-L-[4-O-(2,6-dichlorobenzyl)]-tyrosine
CAS No. 217478-98-3
项目整合开发状态: Preclin...
参考文献标题:Anti-inflammatory tyrosine derivs.
文献作者:Head,J.C.; Warrellow,G.J.; Archibald,S.C.(Celltech Chiroscience plc)
参考来源:EP 0984981; US 6093696; WO 9854207

新产品编号:555791

Chemical Name: 1-(Cyclohexylmethoxy)-3-(1H-imidazol-4-yl)propane-2(S)-amine dihydrochloride
CAS No. 223117-94-0
项目整合开发状态: Biological Testing
项目研究机构: University of Kuopio (Originator)
合成路线:...
参考文献标题:Synthesis and in vitro pharmacology of a series of new chiral histamine H3-receptor ligands: 2-(R and S)-amino-3-(1H-imidazol-4(5)-yl)propyl ether derivatives
文献作者:Kovalainen,J.T.; Christiaans,J.A.; Kotisaari,S.; Laitinen,J.T.; Mannisto,P.T.; Tuomisto,L.; Gynther,J.
参考来源:J Med Chem 1999,42(7),1193

新产品编号:327983

Chemical Name: (4-Benzylbenzyl)[2(S)-[N-[2,2-dimethyl-1(S)-(N-methylcarbamoyl)propyl]carbamoyl]-4-phenylbutyl]phosphinic acid
CAS No. 202976-34-9
项目整合开发状态: Preclinical
项目研究机构: Pfizer (Origina...
参考文献标题:Phosphinate based inhibitors of matrix metalloproteases
文献作者:Reiter,L.A.(Pfizer Inc.)
参考来源:EP 0923585; JP 1999514673; WO 9803516

新产品编号:418157

Chemical Name: N1-(Benzyl)-Nalpha-[trans-4-ethoxy-1-(sulfanylmethyl)-1-cyclohexylcarbonyl]-L-phenylalanylamide
CAS No. 213914-60-4
项目整合开发状态: Preclinical
项目研究机构: Novartis (Originator)
合成路线:...
参考文献标题:Certain cyclic thio substd.acylaminoacid amide derivs.
文献作者:Fink,C.A.(Novartis AG)
参考来源:EP 0966439; US 6034136; WO 9842662

新产品编号:419739

Chemical Name: Nalpha-[trans-4-Ethoxy-1-(sulfanylmethyl)-1-cyclohexylcarbonyl]-N1-(3-pyridyl)-L-phenylalaninamide
CAS No. 213915-01-6
项目整合开发状态: Preclinical
项目研究机构: Novartis (Originator)
合成...
参考文献标题:Certain cyclic thio substd.acylaminoacid amide derivs.
文献作者:Fink,C.A.(Novartis AG)
参考来源:EP 0966439; US 6034136; WO 9842662

新产品编号:525733

Chemical Name: [1R,9S,12S(1'R,3'R,4'R),13R,14S,17R,21S,23S,24R,25S,27R]-17-Ethyl-1,14-dihydroxy-23,25-dimethoxy-12-[2(E)-[3-methoxy-4-(3-phenylcarbazoyloxy)cyclohexyl]-1-methylvinyl]-13,19,21,27-tetra...
参考文献标题:Preparation and immunosuppressive activity of 32-(O)-acylated and 32-(O)-thioacylated analogues of ascomycin
文献作者:Hersperger,R.; Schuler,W.; Zenke,G.
参考来源:Bioorg Med Chem Lett 1999,9(2),227

新产品编号:372279

Chemical Name: 1(S)-[2,3-dioxo-7-(trifluoromethyl)-1,2,3,4-tetrahydroquinoxalin-5-ylmethylamino]ethylphosphonic acid hydrochloride
CAS No. 206649-01-6 (free base)
项目整合开发状态: Preclinical
项目研究机构...
参考文献标题:Substd.aminoalkane phosphonic acids
文献作者:Acklin,P.; Allgeier,H.; Auberson,Y.; Ofner,S.; Veenstra,S.J.(Novartis AG)
参考来源:EP 0934326; US 6117873; WO 9817672

新产品编号:506749

Chemical Name: N-(2-Hydroxy-1,2-dioxoethyl)-4-(phosphonomethyl)-L-phenylalanyl-(1-aminocyclohexylcarbonyl)-L-asparagine 3-(1-naphthyl)propyl amide
CAS No. 220193-87-3
项目整合开发状态: Biological Testin...
参考文献标题:Potent inhibition of Grb2 SH2 domain binding by non-phosphate-containing ligands
文献作者:Yao,Z.-J.; King,C.R.; Cao,T.; Kelley,J.; Milne,G.W.; Voigt,J.H.; Burke,T.R.Jr.
参考来源:J Med Chem 1999,42(1),25