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

CT-4694

Chemical Name: 4-[6-[3(S)-Ethylpiperazinyl]-3-pyridinyl]-N-(3,4,5-trimethoxyphenyl)pyrimidine-2-amine
CAS No. 207284-01-3
项目整合开发状态: Biological Testing
项目研究机构: Celltech (Originator)
合成路线:Re...
参考文献标题:4-Pyridin-5-yl-2-(3,4,5-trimethoxyphenylamino)pyrimidines: Potent and selective inhibitors of ZAP 70
文献作者:Moffat,D.; Davis,P.; Hutchings,M.; Davis,J.; Berg,D.; Batchelor,M.; Johnson,J.; O'Connell,J.; Martin,R.; Crabbe,T.; Delgado,J.; Perry,M.
参考来源:Bioorg Med Chem Lett 1999,9(23),3351

新产品编号:101757

Chemical Name: 4-[4-(4-Fluorophenyl)-1-[3-(4-morpholinyl)propyl]-1H-imidazol-5-yl]pyrimidin-2-amine
CAS No. 165806-48-4
项目整合开发状态: Preclinical
项目研究机构: GlaxoSmithKline (Originator)
合成路线:Cond...
参考文献标题:Tri-substd.imidazoles having multiple therapeutic properties
文献作者:Adams,J.L.; Sheldrake,P.W.; Gallagher,T.F.; Garigipati,R.S.; Bender,P.E.; Boehm,J.C.(SmithKline Beecham plc)
参考来源:EP 0708768; WO 9502591

CW-252053

Chemical Name: 2(S)-[4-(2-Amino-6-methyl-4-oxo-3,4-dihydroquinazolin-5-ylsulfanyl)benzamido]-2-(3-carboxyphenyl)acetic acid disodium salt
CAS No. 220096-00-4 (free acid)
项目整合开发状态: Preclinical 参考文献标题:Design of thymidylate synthase inhibitors using protein crystal structures: The synthesis and biological evaluation of a novel class of 5-substituted quinazolinones
文献作者:Webber,S.E.; Bleckman,T.M.; Attard,J.; Deal,J.G.; Kathardekar,V.; Welsh,K.M.; Webber,S.; Janson,C.A.; Matthews,D.A.; Smith,W.W.; et al.
参考来源:J Med Chem 1993,36(6),733

新产品编号:433977

Chemical Name: 4-(Benzyloxy)-2-(4-fluorophenyl)-3-(4-pyridinyl)-1H-pyrrolo[2,3-b]pyridin-6-amine
CAS No. 215307-20-3
项目整合开发状态: Biological Testing
项目研究机构: R.W. Johnson (Originator)
合成路线:Syl...
参考文献标题:Substd.pyrrolopyridines useful in the treatment of inflammatory diseases
文献作者:Dodd,J.H.; Henry,J.R.; Rupert,K.(Ortho-McNeil Pharmaceutical,Inc.)
参考来源:WO 9847899

新产品编号:160291

Chemical Name: 5-Butyl-9-fluoro-2,2,4-trimethyl-2,5-dihydro-1H-[1]benzopyran[3,4-f]quinoline
CAS No. 179895-44-4
项目整合开发状态: Preclinical
项目研究机构: Ligand (Originator)
合成路线:The Skraup reaction ...
参考文献标题:Steroid receptor modulator cpds.and methods
文献作者:Jones,T.K.; Goldman,M.E.; Pooley,C.L.F.; Winn,D.T.; Edwards,J.E.; West,S.J.; Tegley,C.M.; Zhi,L.; Hamann,L.G.; Farmer,L.J.; Davis,R.J.(Ligand Pharmaceuticals,Inc.)
参考来源:EP 0800519; JP 1998510840; US 5688808; US 5688810; US 5693646; US 5693647; US 5696127; US 5696130; US 5696133; WO 9619458

新产品编号:503585

Chemical Name: (Z)-1-Methyl-4-[2-(3,4,5-trimethoxyphenyl)vinyl]pyridin-2(1H)-one
CAS No. 220114-82-9
项目整合开发状态: Preclinical
项目研究机构: Ajinomoto (Originator)
合成路线:Reduction of N-methyl-2-pyrid...
参考文献标题:Novel B-ring modified combretastatin analogues: Synthesis and antineoplastic activity
文献作者:Hatanaka,T.; Fujita,K.; Ohsumi,K.; Nakagawa,R.; Fukuda,Y.; Nihei,Y.; Suga,Y.; Akiyama,Y.; Tsuji,T.
参考来源:Bioorg Med Chem Lett 1998,8(23),3371

新产品编号:502003

Chemical Name: (Z)-2-Methoxy-5-[2-(3,4,5-trimethoxyphenyl)vinyl]pyridine
CAS No. 220114-73-8
项目整合开发状态: Preclinical
项目研究机构: Ajinomoto (Originator)
合成路线:Reduction of N-methyl-2-pyridone-4-ca...
参考文献标题:Novel B-ring modified combretastatin analogues: Synthesis and antineoplastic activity
文献作者:Hatanaka,T.; Fujita,K.; Ohsumi,K.; Nakagawa,R.; Fukuda,Y.; Nihei,Y.; Suga,Y.; Akiyama,Y.; Tsuji,T.
参考来源:Bioorg Med Chem Lett 1998,8(23),3371

YJA-20379-8

Chemical Name: (+)-1-[8-Ethoxy-4-[1(R)-phenylethylamino]-1,7-naphthyridin-3-yl]-1-butanone
CAS No. 187654-40-6
项目整合开发状态: Preclinical
项目研究机构: Yung-Jin (Originator)
合成路线:The condensation of ...
参考文献标题:4-Amino-3-acylnaphthyridine derivs.
文献作者:Sohn,S.K.; Chang,M.S.; Kim,S.G.; Chung,K.J.; Kang,D.P.; Kim,Y.H.; Kang,B.G.; Choi,W.S.; Seo,K.H.; Yoo,H.Y.; Paek,J.H.(Yung-Jin Pharmaceutical Co.,Ltd.)
参考来源:WO 9703074

MP-2269

Chemical Name: Tetrasodium [6-[2-[bis(carboxylatomethyl)amino]ethyl]-7-carboxylato-3-(carboxylatomethyl)-12-[(4-pentylbicyclo[2.2.2]oct-1-ylcarbonyl)-L-aspartyl-L-aspartyl]-3,6,12-triazadodecanoato(7-...
参考文献标题:Magnetic resonance blood pool agents
文献作者:Woulfe,S.R.(Mallinckrodt Medical Inc.)
参考来源:WO 9820908

新产品编号:389681

Chemical Name: (1R,2R,3R,5S)-8-Methyl-3-(4-methylphenyl)-2-phenyl-8-azabicyclo[3.2.1]octane
CAS No. 208989-27-9
项目整合开发状态: Preclinical
项目研究机构: Georgetown University (Originator), UT Medical Br...
参考文献标题:Synthesis and biological properties of new 2beta-alkyl- and 2beta-aryl-3-(substituted phenyl)tropane derivatives: Stereochemical effect of C-3 on affinity and selectivity for neuronal dopamine and serotonin transporters
文献作者:Kozikowski,A.P.; Araldi,G.L.; Prakash,K.R.; Zhang,M.; Johnson,K.M.
参考来源:J Med Chem 1998,41(25),4973