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

MRE-3008, MRE-3008-F20

Chemical Name: N-[2-(2-Furyl)-8-propyl-8H-pyrazolo[4,3-e][1,2,4]triazolo[1,5-c]pyrimidin-5-yl]-N'-(4-methoxyphenyl)urea
CAS No. 252979-43-4
项目整合开发状态: Biological Testing
项目研究机构: Medco (Origina...
参考文献标题:Pyrazolo[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidine derivatives as highly potent and selective human A3 adenosine receptor antagonists
文献作者:Baraldi,P.G.; Cacciari,B.; Ropmagnoli,R.; Spalluto,G.; Klotz,K.N.; Leung,E.; Varani,K.; Gessi,S.; Merighi,S.; Borea,P.A.
参考来源:J Med Chem 1999,42(22),4473

CF-1368

Chemical Name: 3-(2'-Deoxy-beta-D-ribofuranosyl)-6-octyl-2,3-dihydrofuro[2,3-d]pyrimidin-2-one
CAS No. 215668-64-7
项目整合开发状态: Biological Testing
项目研究机构: Cardiff University (Originator), Rega I...
参考文献标题:Anti-viral pyrimidine nucleoside analogues
文献作者:Jones,G.; Balzarini,J.; McGuigan,C.; Yarnold,C.; De Clercq,E.(University College,Cardiff)
参考来源:EP 0980377; WO 9849177

新产品编号:177693

Chemical Name: N-[4-Guanidino-1(S)-[4-(2-hydroxyethyl)piperidin-1-ylcarbonyl]butyl]-3,3-dimethyl-1,2,3,4-tetrahydroquinoline-8-sulfonamide
CAS No. 184037-69-2, 184037-70-5 (acetate)
项目整合开发状态: Pr...
参考文献标题:Trypsin and thrombin inhibitors
文献作者:Hoyle,W.; Howarth,G.A.; Brundish,D.E.; Kane,P.D.; Walker,C.V.; Hayler,J.; Fullerton,J.D.; Smith,G.P.; Wathey,W.B.; Le Grand,D.M.; Allen,M.C.; Herold,P.(Novartis AG)
参考来源:EP 0815103; JP 1999502219; WO 9629327

新产品编号:495675

Chemical Name: 2-Deoxy-6-O-[2-deoxy-4-O-phosphono-3-O-[3(R)-(tetradecanoyloxy)tetradecanoyl]-2-[3(R)-(tetradecanoyloxy)tetradecanamido-beta-D-glucopyranosyl]-2-[3(R)-(tetradecanoyloxy)tetradecanamido]...
参考文献标题:3-O-Desacyl monophosphoryl lipid A derivatives: Synthesis and immunostimulant activities
文献作者:Johnson,D.A.; Keegan,D.S.; Sowell,C.G.; Livesay,M.T.; Johnson,C.L.; Taubner,L.M.; Harris,A.; Myers,K.R.; Thompson,J.D.; Gustafson,G.L.; Rhodes,M.J.; Ulrich,J.T.; Ward,J.R.; Yorgensen,Y.M.; Cantrell,J.L.; Brookshire,V.G.
参考来源:J Med Chem 1999,42(22),4640

IQM-97423

Chemical Name: N-[(4aS,5R)-2-Benzyl-1,3-dioxoperhydropyrido[1,2-c]pyrimidin-5-yl]-2(S)-(3-tert-butylureido)-3-(1H-indol-3-yl)propionamide; N1-[(4aS,5R)-2-Benzyl-1,3-dioxoperhydropyrido[1,2-c]pyrimidin...
参考文献标题:Synthesis and stereochemical structure-activity relationships of 1,3-dioxoperhydropyrido[1,2-c]pyrimidine derivatives: Potent and selective cholecystokinin-A receptor antagonists
文献作者:Mart韓-Mart韓ez,M.; Bartolome-Nebreda,J.M.; Gomez-Monterrey,I.; Gonzalez-Muniz,R.; Garcia-Lopez,M.T.; Ballaz,S.; Barber,A.; Fortuno,A.; del Rio,J.; Herranz,R.
参考来源:J Med Chem 1997,40(21),3402

新产品编号:661785

Chemical Name: 3,9-Dibenzyl-1,5,7,11-tetrahydroxymethyl-6,12-diphenyl-3,9-diazapentacyclo[6.4.0.0(2,7).0(4,11).0(5,10)]dodecane
CAS No. 252671-48-0
项目整合开发状态: Biological Testing
项目研究机构: Novart...
参考文献标题:Synthesis and biological evaluation of the first N-alkyl cage dimeric 4-aryl-1,4-dihydropyridines as novel nonpeptidic HIV-1 protease inhibitors
文献作者:Hilgeroth,A.; Wiese,M.; Billich,A.
参考来源:J Med Chem 1999,42(22),4729

FR-226807

Chemical Name: N-(3,4-Dimethoxybenzyl)-2-[2-hydroxy-1(R)-methylethylamino]-5-nitrobenzamide
CAS No. 247568-68-9, 247567-47-1 ((S)-isomer)
项目整合开发状态: Preclinical
项目研究机构: Fujisawa (Originator) 参考文献标题:Anthranilic acid derivs.as inhibitors of the cGMP-phosphodiesterase
文献作者:Oku,T.; Sawada,K.; Kuroda,A.; Kayakiri,N.; Sawada,Y.; Inoue,T.; Mizutani,T.(Fujisawa Pharmaceutical Co.,Ltd.)
参考来源:EP 1080069; JP 2001508811; US 6384080; WO 9954284

bis(tBuSATE)AZT-MP, UA-428

Chemical Name: 3'-Azido-5'-O-[bis[2-(S-pivaloylsulfanyl)ethoxy]phosphoryl]-3'-deoxythymidine
CAS No. 168777-50-2
项目整合开发状态: Preclinical
项目研究机构: Katholieke Universiteit Leuven (Originator), Uni...
参考文献标题:Synthesis of the tBuSATE pronucleotide of AZT by two different synthetic approaches
文献作者:Lannuzel,M.; Egron,D.; Imbach,J.L.; Gosselin,G.; Perigaud,C.
参考来源:Nucleosides Nucleotides 1999,18(4-5),1001

新产品编号:581103

Chemical Name: N-[2-(1H-Indol-3-yl)ethyl]-7,8-dihydroisoquinoline-6-carboxamide hydrochloride
CAS No. 227199-46-4 (free base)
项目整合开发状态: Preclinical
项目研究机构: Shire BioChem (Originator)
合成路线:...
参考文献标题:Antiviral cpds.
文献作者:Bedard,J.; Rando,R.; Falardeau,G.; Lavallee,J.-F.(BioChem Pharma Inc.)
参考来源:WO 9929318

DPP-AZT

Chemical Name: 3'-Azido-3'-deoxy-5'-O-[2,3-bis(hexadecanoyloxy)propoxy(hydroxy)phosphoryl]thymidine; 3'-Azido-3'-deoxythymidilic acid mono[2,3-bis(hexadecanoyloxy)propyl] ester
CAS No. 161106-33-8,...
参考文献标题:Lymphatic targeting of anti-HIV nucleosides: Distribution of 3'-azido-3'-deoxythymidine (AZT) and 3'-azido-2',3'-dideoxyuridine (AZdU) after administration of dipalmitoylphosphatidyl prodrugs to mice
文献作者:Manouilov,K.K.; Fedorov,I.I.; Boudinot,F.D.; White,C.A.; Kotra,L.P.; Schinazi,R.F.; Hong,C.I.; Chu,C.K.
参考来源:Antivir Chem Chemother 1995,6(4),230