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

SME-308, SLV-308

盐酸帕多芦诺帕多芦诺 Chemical Name: 7-(4-Methyl-1-piperazinyl)benzoxazol-2(3H)-one monohydrochloride
CAS No. 269718-83-4, 269718-84-5 (free base)
项目整合开发状态: Phase II
项目研究机构: Solvay (Originator), Meiji...
参考文献标题:New piperazine and piperidine cpds.
文献作者:Feenstra,R.W.; Visser,G.M.; Van der Heijden,J.A.M.; Long,S.K.; Toorop,G.P.; Van Scharrenburg,G.J.M.; Kruse,C.G.; Mos,J.; Toorop,A.G.(Duphar International Research BV)
参考来源:WO 0029397

Palonosetron hydrochloride, RS-25259-197, Onicita, Onicit, Aloxi

盐酸帕洛诺司琼帕洛诺司琼 Chemical Name: 2-[1-Azabicyclo[2.2.2]oct-3(S)-yl]-2,3,3a(S),4,5,6-hexahydro-1H-benz[de]isoquinolin-1-one hydrochloride; 2-[Quinuclidin-3(S)-yl]-2,3,3a(S),4,5,6-hexahydro-1H-benz[de]isoqu...
参考文献标题:New tricyclic cpds
文献作者:Berger,J.; Clark,R.D.; Eglen,R.M.; Smith,W.L.; Weinhardt,K.K.(Syntex (USA),Inc.)
参考来源:AU 9166963; EP 0430190; US 5202333

Ecenofloxacin hydrochloride, CFC-222

盐酸恩诺沙星Chemical Name: (+)-(1R,5S,6S)-7-(6-Amino-1-methyl-3-azabicyclo[3.2.0]hept-3-yl)-1-cyclopropyl-6-fluoro-4-oxo-1,4-dihydro-1,8-naphthyridine-3-carboxylic acid hydrochloride
CAS No. 162424-67-1,...
参考文献标题:Novel pyridone carboxylic acid derivs
文献作者:Kim,C.S.; Kim,J.W.; Lee,J.M.; Cho,I.H.; Youn,Y.S.; Shin,Y.J.; Lee,K.H.; Kim,J.H.; Jung,Y.H.; An,S.H.(Cheil Jedang Corporation)
参考来源:JP 1996505384; US 5527910; WO 9415933

Xaliproden hydrochloride, SR-57746A, Xaprila

盐酸扎利罗登扎利罗登 Chemical Name: 1-[2-(2-Naphthyl)ethyl]-4-[3-(trifluoromethyl)phenyl]-1,2,3,6-tetrahydropyridine hydrochloride
CAS No. 90494-79-4, 135354-02-8 (free base)
项目整合开发状态: Phase III
项目研究机...
参考文献标题:Trifluoromethylphenyltetrahydropyridines with anorexigenic activity,a process for their preparation and compsns
文献作者:Nisato,D.; Frigerio,M.; Miranda,G.F.(Midy SpA; Sanofi-Synthabo )
参考来源:EP 0101381

Topotecan hydrochloride, E-89/001, NSC-609699, SK&F-S-104864-A, Evotropin, Hycamtin

盐酸拓扑替康托泊替康醋酸盐拓扑替康Chemical Name: (S)-10-Dimethylaminomethyl-9-hydroxycamptothecin monohydrochloride; (4S)-10-(Dimethylaminomethyl)-4-ethyl-4,9-dihydroxy-3,4,12,14-tetrahydro-1H-pyrano[3',4':6,7]indol...
参考文献标题:Water soluble camptothecin analogs
文献作者:Boehm,J.C.; Johnson,R.K.; Hecht,S.M.; Kingsbury,W.D.; Holden,K.G.(SmithKline Beecham plc)
参考来源:AU 8826394; EP 0321122; JP 1989186893; US 5004758

Pramipexole hydrochloride, SND-919, PNU-98528E, SND-919CL2Y(free base), U-98528E(free base), SND-919Y, Mirapexin, Sifrol, Mirapex

盐酸普拉克索 (R)-普拉克索普拉克索杂质DChemical Name: (S)-(-)-2-Amino-6-(propylamino)-4,5,6,7-tetrahydrobenzothiazole dihydrochloride
CAS No. 104632-25-9, 104632-28-2 ((R)-isomer), 104632-27-1 ((R)-isomer, diHCl)...
参考文献标题:Tetrahydrobenzothiazoles,their preparation and their use as intermediates or as medicines
文献作者:Griss,G.et al.(Dr.Karl Thomae GmbH)
参考来源:AU 8551544; DE 3447075; DE 3508947; EP 0186087; ES 8707513; ES 8707514; ES 8707515; JP 1986155377; US 4731374

Trequinsin hydrochloride, HL-725

盐酸曲林菌素Chemical Name: 9,10-Dimethoxy-2-mesitylimino-3-methyl-3,4,6,7-tetrahydro-2H-pyrimido[6,1-a]isoquinolin-4-one hydrochloride; 9,10-Dimethoxy-3-methyl-2-(2,4,6-trimethylphenylimino)-2,3,6,7-tetrahy...
参考文献标题:HL-725
文献作者:Arya,V.P.
参考来源:Drugs Fut 1982,7(6),390

Tizanidine hydrochloride, DS-103282 ch, AN-021A, DS-103282, Zanaflex, Ternelin, Sirdalud

盐酸替扎尼定替扎尼定 Chemical Name: 5-Chloro-4-(2-imidazolin-2-ylamino)-2,1,3-benzothiadiazole hydrochloride; 5-Chloro-N-(4,5-dihydro-1H-imidazol-2-yl)-2,1,3-benzothiadiazole hydrochloride
CAS No. 64461-82-...
参考文献标题:DS-103-282
文献作者:Unterhalt,B.
参考来源:Drugs Fut 1980,5(1),27

Tirofiban hydrochloride, MK-383, L-700462, Aggrastat

盐酸替罗非班替罗非班盐酸替罗非班Chemical Name: N-(Butylsulfonyl)-4-O-[4-(4-piperidyl)butyl]-L-tyrosine monohydrochloride
CAS No. 142373-60-2, 144494-65-5 (free base), 150915-40-5 (monoH2O)
项目整合开发状态: Launched-...
参考文献标题:Novel sulfonamide fibrinogen receptor antagonists
文献作者:Egbertson,M.S.; Laswell,W.L.; Hartman,G.D.; Duggan,M.E.; Halczenko,W.(Merck & Co.,Inc.)
参考来源:EP 0478363; EP 0743302; JP 1992288051; US 5292756

Temocapril hydrochloride, CS-622, RS-5142, Acecol

盐酸替莫普利替莫普利 Chemical Name: 2-[(2S,6R)-6-[1(S)-(Ethoxycarbonyl)-3-phenylpropylamino]-5-oxo-2-(2-thienyl)perhydro-1,4-thiazepin-4-yl]acetic acid hydrochloride
CAS No. 110221-44-8, 111902-57-9 (free b...
参考文献标题:Perhydrothiazepine derivatives,their preparation and their therapeutical use
文献作者:Yanagisawa,H.; Ishihara,S.; Ando,A.; Kanazaki,T.; Koike,H.; Tsujita,Y.(Sankyo Co.,Ltd.)
参考来源:AU 8541058; EP 0161801; ES 8702388; ES 8801229; JP 85215678; JP 86267579