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

842470, GW-842470, AWD-12-281

Chemical Name: N-(3,5-Dichloro-4-pyridinyl)-2-[1-(4-fluorobenzyl)-5-hydroxy-1H-indol-3-yl]-2-oxoacetamide
CAS No. 247584-20-9
项目整合开发状态: Phase II
项目研究机构: elbion (Originator), GlaxoSmithKline (...
参考文献标题:New hydroxyindoles,their use as phosphodiesterase 4 inhibitors and method for producing same
文献作者:H鰂gen,N.; Kronbach,T.; Plymeropoulos,E.; Marx,D.; Heer,S.; Szelenyi,S.; Egerland,U.; Poppe,H.(Arzneimittelwerk Dresden GmbH)
参考来源:CA 2270301; DE 19818964; WO 9955696

LY-367366

Chemical Name: 4-[1-Amino-1-carboxy-2-(9H-thioxanthen-9-yl)ethyl]benzoic acid
CAS No. 209332-61-6
项目整合开发状态: Preclinical
项目研究机构: Lilly (Originator)
合成路线:The condensation of ethyl 2-(4-cyano...
参考文献标题:Pharmaceutical substd.propanoic acid derivs.
文献作者:Purdey,J.A.; et al.(Eli Lilly and Company)
参考来源:EP 0849263; JP 10194734; US 5965103

MRS-1523

Chemical Name: 6-Ethyl-5-(ethylsulfanylcarbonyl)-2-phenyl-4-propylpyridine-3-carboxylic acid propyl ester
CAS No. 212329-37-8
项目整合开发状态: Biological Testing
项目研究机构: National Institutes of Healt...
参考文献标题:Structure-activity relationships and molecular mod
文献作者:Li,A.-H.; Moro,S.; Melman,N.; Ji,X.D.; Jacobson,K.A.
参考来源:J Med Chem 1998,41(17),3186

ABT-546, A-216546

Chemical Name: (2S,3R,4S)-1-[2-(Dibutylamino)-2-oxoethyl]-2-(2,2-dimethylpentyl)-4-(7-methoxy-1,3-benzodioxol-5-yl)tetrahydro-1H-pyrrole-3-carboxylic acid
CAS No. 195707-49-4 (stereoisomer)
项目整合...
参考文献标题:Novel benzo-1,3-dioxolyl- and benzofuranyl substd.pyrrolidine derivs.as endothelin antagonists
文献作者:Winn,M.; Boyd,S.A.; Hutchins,C.W.; Tasker,A.S.; Von Geldern,T.W.; Kester,J.A.; Sorensen,B.K.; Szczepankiewicz,B.G.; Henry,K.J.Jr.; Liu,G.; Wittenberger,S.J.; King,S.A.(Abbott Laboratories Inc.)
参考来源:EP 0885215; WO 9730045

J-104129

Chemical Name: 2(R)-Cyclopentyl-2-hydroxy-N-[1-(4-methyl-3-pentenyl)-4-piperidinyl]-2-phenylacetamide
CAS No. 185029-36-1 (fumarate (1:1)), 185029-08-7 (undefined isomer)
项目整合开发状态: Preclinical 参考文献标题:1,4-Disubstd.piperidine derivs.
文献作者:Tsuchiya,Y.; Nomoto,T.; Ohsawa,H.; Kawakami,K.; Ohwaki,K.; Nishikibe,M.(Banyu Pharmaceutical Co.,Ltd.)
参考来源:EP 0823423; US 5750540; WO 9633973

SB-226882

Chemical Name: 4-[4-(4-Fluorophenyl)-1-(4-piperidinyl)-1H-imidazol-5-yl]-N-methylpyrimidine-2-amine
CAS No. 180869-16-3
项目整合开发状态: Biological Testing
项目研究机构: GlaxoSmithKline (Originator)
合成...
参考文献标题:Certain 1,4,5-tri-substd.imidazole cpds.useful as cytokine
文献作者:Adams,J.L.; Gallagher,T.F.; Garigipati,R.S.; Boehm,J.C.; Sisko,J.; Peng,Z.-Q.; Lee,J.C.-L.(SmithKline Beecham plc)
参考来源:EP 0809499; JP 1998512555; US 5593992; WO 9621452

LY-393675

Chemical Name: 2(S)-Amino-2-(cis-3-carboxycyclobutyl)-3-(9-thioxanthyl)propionic acid
CAS No. 206444-77-1, 206444-76-0 (trans-isomer), 206444-72-6 (undefined stereoch.)
项目整合开发状态: Preclinical
...
参考文献标题:Pharmaceutical acidic cpds.
文献作者:Clark,B.P.; Harris,J.R.(Eli Lilly and Company)
参考来源:EP 0837061; JP 1998120635; US 6054448

Org-37432

Chemical Name: 2-[N-(Carboxymethyl)-3-cyclohexyl-D-alanyl-L-prolyl-L-lysyl]thiazole
CAS No. 190904-27-9
项目整合开发状态: Preclinical
项目研究机构: Organon (Originator)
合成路线:Treatment of protected lysin...
参考文献标题:A polar pharmacophore for oral bioavailability in thrombin inhibitors
文献作者:Rewinkel,J.B.M.; Smit,M.J.; Noach,A.B.J.; van Dinther,T.G.; Grootenhuis,P.D.J.; Peters,J.A.M.; Kelser,J.; Visser,A.; van Boeckel,C.A.A.; Vogel,G.M.T.; van Aelst,S.F.; Adang,A.E.P.
参考来源:15th European Federation for Medicinal Chemistry International Symposium on Medicinal Chemistry (Sept 6 1998,Edinburgh) 1998,Abst P.157

LY-339476

Chemical Name: 2-Amino-2-(2-benzyl-3,5-dihydroxyphenyl)acetic acid
CAS No. 198420-11-0
项目整合开发状态: Biological Testing
项目研究机构: Lilly (Originator)
合成路线:Alkylation of methyl 3,5-dihydroxybenzoa...
参考文献标题:Derivs.of phenylglycine and use thereof as pharmaceuticals
文献作者:Baker,S.R.; Clark,B.P.; Goldsworthy,J.; Harris,J.R.(Eli Lilly and Company)
参考来源:EP 0807621; JP 1998067723; US 5863947

LK-423

Chemical Name: 2-[2-(1,3-Dioxo-1,3-dihydro-2H-isoindol-2-yl)ethoxy]acetyl-L-alanyl-D-glutamic acid 1-amide; 2-(2-Phathalimidoethoxy)acetyl-L-alanyl-D-isoglutamine
CAS No. 142489-46-1
项目整合开发状态: P...
参考文献标题:Novel N-acyldipeptides,processes for the preparation thereof and pharmaceutical compsns.containing the same
文献作者:Pecar,S.; Sollner,M.; Urleb,U.; Kikelj,D.; Marc,G.; Krbavcic,A.; Kotnik,V.; Wraber-Herzog,B.; Simcic,S.; Ihan,A.; Klamfer,L.; Provsic,L.; Kopitar,Z.; Stalc,A.(LEK Pharmaceutical and Chemical Co.; University of Ljubljana)
参考来源:EP 0477912; JP 1994220087