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

LY-382924

Chemical Name: 2,6-Di-tert-butyl-4-[4-[4-[2-(N-ethyl-N-methylamino)ethyl]phenoxymethyl]oxazol-2-yl]phenol hydrochloride; 2-(3,5-Di-tert-butyl-4-hydroxyphenyl)-4-[4-[2-(N-ethyl-N-methylamino)ethyl]phen...
参考文献标题:Synthesis and biological evaluation of a novel series of antioxidants for the treatment of global cerebral ischemia
文献作者:Heinz,L.J.; et al.
参考来源:217th ACS Natl Meet (March 21 1999,Anaheim) 1998,Abst MEDI 130

N276-15

Chemical Name: 4-Isopropyl-2-methyl-6-[4-(2-methyl-1H-imidazo[4,5-c]pyridin-1-yl)phenyl]-1,4-dihydropyridine-3,5-dicarboxylic acid 5-ethyl 3-[3-(3-pyridyl)propyl] diester
CAS No. 208194-73-4
项目整...
参考文献标题:1,4-Dihydropyridine derivs.
文献作者:Tasaka,S.; Tanabe,H.; Omori,H.; Kiue,A.(Nikken Chemicals Co.,Ltd.)
参考来源:EP 0943615; JP 1998204061; WO 9823607

新产品编号:361205

Chemical Name: 2-[5-[2(E)-(N,N-Diethylcarbamoyl)-1-methylvinyl]-2-(2,6-difluorobenzyloxy)phenyl]acetic acid
CAS No. 205317-69-7
项目整合开发状态: Preclinical
项目研究机构: Novartis (Originator)
合成路线:3',...
参考文献标题:Carboxy-substituted cinnamides: A novel series of potent,orally active LTB4 receptor antagonists
文献作者:Greenspan,P.D.; Fujimoto,R.A.; Marshall,P.J.; Raychaudhuri,A.; Lipson,K.E.; Zhou,H.; Doti,R.A.; Coppa,D.E.; Zhu,L.; Pelletier,R.; Uziel-Fusi,S.; Jackson,R.H.; Chin,M.H.; Kotyuk,B.L.; Fitt,J.J.
参考来源:J Med Chem 1999,42(1),164

NNC-92-1687

Chemical Name: 2-(1H-Benzimidazol-2-ylsulfanyl)-1-(3,4-dihydroxyphenyl)-1-ethanone
CAS No. 22903-37-3, 22903-39-5 (monoHCl)
项目整合开发状态: Biological Testing
项目研究机构: Novo Nordisk (Originator)
合...
参考文献标题:Discovery and structure-activity relationship of the first non-peptide competitive human glucagon receptor antagonists
文献作者:Madsen,P.; Knudsen,L.B.; Wiberg,F.C.; Carr,R.D.
参考来源:J Med Chem 1998,41(26),5150

MHP-46

Chemical Name: (3R,5aS,6R,8aS,9R,10R,12S,12aR)-Octahydro-3,6,9-trimethyl-10-(2-furyl)-3,12-epoxy-12H-pyrano[4,3-j][1,2]benzodioxepin
CAS No. 204503-68-4
项目整合开发状态: Biological Testing
项目研究机构: J...
参考文献标题:Orally active,hydrolytically stable,semisynthetic,antimalarial trioxanes in the artemisinin family
文献作者:Posner,G.H.; Parker,M.H.; Northrop,J.; Elias,J.S.; Ploypradith,P.; Xie,S.; Shapiro,T.A.
参考来源:J Med Chem 1999,42(2),300

DW-2282

Chemical Name: (+)-(S)-1-[1-(4-Aminobenzoyl)indolin-5-ylsulfonyl]-4-phenylimidazolidin-2-one
CAS No. 203861-05-6 (monoHCl), 203860-97-3 (racemic monoHCl)
项目整合开发状态: Preclinical
项目研究机构: Dong-Wh...
参考文献标题:Arylsulfonylimidazolone derivs.as an antitumor agent
文献作者:Yoon,S.J.; Chung,Y.H.; Lee,M.S.; Choi,D.R.; Lee,J.A.; Lee,H.S.; Yun,H.R.; Lee,D.K.; Moon,E.Y.; Hwang,H.S.; Choi,C.H.; Jung,S.H.(Dong-Wha Pharmaceuticals Industry Co.Ltd)
参考来源:EP 1021437; JP 2000505096; US 5929103; WO 9807719

SA-862

Chemical Name: 3-(3-Amidinophenyl)-N-(2'-sulfamoylbiphenyl-4-yl)isoxazole-4-carboxamide
CAS No. 209730-58-5, 209730-59-6 (monotrifluoroacetate)
项目整合开发状态: Preclinical
项目研究机构: Bristol-Myers Squ...
参考文献标题:Oxygen or sulfur containing heteroaromatics as fac
文献作者:Quan,M.L.; Pinto,D.J.P.; Fevig,J.M.; Pruitt,J.R.(DuPont Pharmaceuticals Co.)
参考来源:WO 9828282

DMP-695

Chemical Name: N-(2-Chloro-4,6-dimethylphenyl)-1-[2-methoxy-1-(methoxymethyl)ethyl]-6-methyl-1H-[1,2,3]triazolo[4,5-c]pyridin-4-amine methanesulfonate
CAS No. 197802-63-4, 197799-44-3 (free base) 参考文献标题:Arylamino fused pyridines and pyrimidines
文献作者:Bakthavatchalam,R.; Arvanitis,A.G.; Beck,J.P.; Cain,G.A.; Chorvat,R.J.; Gilligan,P.J.; Olson,R.E.(DuPont Pharmaceuticals Co.)
参考来源:EP 0935601; WO 9735539

SB-237596

Chemical Name: N-Benzyl-4,5alpha-epoxy-N-isopropyl-3-methoxy-4',17-dimethyl-6,7-didehydropyrrolo[2',3':6,7]morphinan-5'-carboxamide
CAS No. 193612-32-7 (monoHCl)
项目整合开发状态: Preclinical
项目研究机构:...
参考文献标题:Heterocycle-condensed morphinoid derivs.(II)
文献作者:Dondio,G.; Ronzoni,S.; Gatti,P.A.; Graziani,D.(SmithKline Beecham SpA)
参考来源:EP 0880526; JP 2000503019; WO 9725331

SB-235863A, SB-235863

Chemical Name: 4,5alpha-Epoxy-3-methoxy-4',17-dimethyl-6,7-didehydropyrrolo[2',3':6,7]morphinan-5'-carboxylic acid isobutyl ester
CAS No. 177284-77-4 (monoHCl)
项目整合开发状态: Preclinical
项目研究机构: G...
参考文献标题:Heterocycle-condensed morphinoid derivs.(II)
文献作者:Dondio,G.; Ronzoni,S.; Gatti,P.A.; Graziani,D.(SmithKline Beecham SpA)
参考来源:EP 0880526; JP 2000503019; WO 9725331