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

SSR-146977

N'-[1-[3-[(3R)-1-苯甲酰基-3-(3,4-二氯苯基)-3-哌啶基]丙基]-4-苯基-4-哌啶基]-N,N-二甲基脲Chemical Name: N-[1-[3-[1-Benzoyl-3(R)-(3,4-dichlorophenyl)piperidin-3-yl]propyl]-4-phenylpiperidin-4-yl]-N',N'-dimethylurea
CAS No....
参考文献标题:Ureidopiperidine derivs.as selective human NK3 receptor antagonists
文献作者:Proietto,V.; Van Broeck,D.; Edmonds-Alt,X.; Aulombard,A.(Sanofi-Synthabo)
参考来源:EP 1119552; JP 2002527423; US 6465489; WO 0021931

Etacizin, Ethacizin, NIK-244

N-[10-(3-二乙基氨基丙酰基)吩噻嗪-2-基]氨基甲酸乙酯Chemical Name: 2-(Ethoxycarbonylamino)-10-[3-(diethylamino)propionyl]phenothiazine; [10-[3-(Diethylamino)-1-oxopropyl]-10H-phenothiazin-2-yl]carbamic acid ethyl ester 参考文献标题:Agent for treating myocardial infarction
文献作者:Cazov,E.I.; Valdman,A.V.; Kaverine,N.V.; Penke,I.C.; Rozenstrauch,L.V.; Cicharev,V.N.; Prjanisnikova,N.T.; Senota,Z.P.; Lyskovcev,V.V.; Grigorieva,E.K.; Skoldinov,A.P.; Gricenko,A.N.; Ermakova,Z.I.; et al.(Nauchno-Issledovatelsky Institut)
参考来源:DE 3314142

ZK-34228, CGP-28237

N-[1-氧代-6-(苯氧基)-2,3-二氢茚-5-基]甲烷磺酰胺Chemical Name: 5-Methylsulfonylamino-6-phenoxy-1-indanone
CAS No. 75360-85-9
项目整合开发状态: Phase I
项目研究机构: Novartis (Originator), Schering AG (Originator)
合成路线...
参考文献标题:CGP-28237
文献作者:Ferrini,P.G.; B鰐tcher,I.
参考来源:Drugs Fut 1987,12(1),9

GW-544, GW-409544X

N-[1-甲基-3-氧基-3-苯基-1(Z)-丙基]-O-[2-(5-甲基-2-苯洛克唑-4-基)乙基]-L-酪氨酸Chemical Name: N-[1-Methyl-3-oxo-3-phenyl-1(Z)-propenyl]-O-[2-(5-methyl-2-phenyloxazol-4-yl)ethyl]-L-tyrosine
CAS No. 258345-41-4
项目整合开发...
参考文献标题:Substd.oxazoles and thiazoles derivs.as hPPAR gamma and hPPAR alpha activators
文献作者:Oplinger,J.A.; Dezube,M.; Willson,T.M.; Collins,J.L.(Glaxo Group Ltd.)
参考来源:EP 1102757; WO 0008002

NK-3201

N-[1-苄基-2,3-二氧基-6-(2-吡啶氧基)己基]-2-[5-(甲酰胺)-6-氧基-2-苯基-1,6-二氢嘧啶-1-基]乙酰胺Chemical Name: N-[1-Benzyl-2,3-dioxo-6-(2-pyridyloxy)hexyl]-2-[5-(formylamino)-6-oxo-2-phenyl-1,6-dihydropyrimidin-1-yl]acetamide
...
参考文献标题:Novel acetamide derivs.and protease inhibitors
文献作者:Suzuki,Y.; Ishida,K.(Nippon Kayaku Co.,Ltd.)
参考来源:EP 0936216; US 6271238; WO 9809949

CI-1021, Cam-4261, PD-154075

N-[2-(1H-吲哚-3-基)-1(R)-甲基-1-[1(S)-苯基乙基氨基甲酰]乙基]氨甲酸苯并呋喃-2-基甲基酯Chemical Name: N-[2-(1H-Indol-3-yl)-1(R)-methyl-1-[1(S)-phenylethylcarbamoyl]ethyl]carbamic acid benzofuran-2-ylmethyl ester
CAS No. 15899...
参考文献标题:Tachykinin antagonists
文献作者:Horwell,D.C.; Howson,W.; Rees,D.C.; Roberts,E.; Pritchard,M.C.(Pfizer Inc.)
参考来源:EP 0655055; EP 1000930; US 5594022; WO 9404494

SK-946

N-[2-(1-氮杂双环[3.3.0]辛烷-5-基)乙基]-2-硝基苯胺富马酸盐Chemical Name: N-[2-(1-Azabicyclo[3.3.0]octan-5-yl)ethyl]-2-nitroaniline fumarate
CAS No. 167889-18-1, 167889-05-6 (free base), 167889-17-0 (monoHCl), 167889...
参考文献标题:1-Azabicyclo[3.3.0]octane derivs.and their use
文献作者:Baba,Y.; Suzuki,T.; Hirooka,K.; Kurono,M.; Sawai,K.(Sanwa Kagaku Kenkyusho Co.,Ltd.)
参考来源:EP 0647642; US 5530138

YM-44778(fumarate salt (1:1))

N-[2-(3,4-二氯苯基)-4-[3-氧基-1,2,3,4-四氢螺蓄[异喹啉-1,4'-哌啶]-1'-基]丁基]-3,4,5-三甲氧基-N-甲基苯甲酰Chemical Name: N-[2-(3,4-Dichlorophenyl)-4-[3-oxo-1,2,3,4-tetrahydrospiro[isoquinoline-1,4'-piperidin]-1'-yl]butyl]-3,4,5-t...
参考文献标题:Spiro-substituted piperidines as neurokinin receptor antagonists.III.Synthesis of (?-N-[2-(3,4-dichlorophenyl)-4-(spiro-substituted piperidin-1'-yl)butyl]-N-methylbenzamides and evaluation of NK1-NK2 dual antagonistic activities
文献作者:Kubota,H.; Kakefuda,A.; Okamoto,Y.; Fujii,M.; Yamamoto,O.; Yamagiwa,Y.; Orita,M.; Ikeda,K.; Takeuchi,M.; Shibanuma,T.; Isomura,Y.
参考来源:Chem Pharm Bull 1998,46(10),1538

RU-24213

N-[2-(3-羟基苯基)乙基]-N-(2-苯乙基)丙基胺Chemical Name: N-[2-(3-Hydroxyphenyl)ethyl]-N-(2-phenylethyl)propylamine
CAS No. 315209-09-7, 67383-44-2 (hydrochloride)
项目整合开发状态: Preclinical
项目研究机构: Aventis Pha...
参考文献标题:Synthesis of study of the dopaminergic activity of di(phenylethyl)amine derivatives
文献作者:Nedelec,L.; et al.
参考来源:Eur J Med Chem - Chim Ther 1978,13(6),553-556

ABT-770

N-[2-(4,4-二甲基-2,5-二氧硅咪唑酮-1-基)-1(S)-[4'-(三氟甲氧基)双苯基-4-酰氧甲基]乙基]-N-羟基甲酰胺Chemical Name: N-[2-(4,4-Dimethyl-2,5-dioxoimidazolidin-1-yl)-1(S)-[4'-(trifluoromethoxy)biphenyl-4-yloxymethyl]ethyl]-N-hydroxyform...
参考文献标题:Reverse hydroxamate inhibitors of matrix metalloproteinases
文献作者:Dellaria,J.F.Jr.; Gong,J.; Steinman,D.H.; Michaelides,M.R.; Giesler,J.; Davidsen,S.K.; Curtin,M.L.; Florjancic,A.S.; Xu,L.; Guo,Y.; Holms,J.H.; Wada,C.K.; Heyman,H.R.(Abbott Laboratories Inc.)
参考来源:JP 2001523272; WO 9906361