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

Tandospirone citrate, SM-3997, Sediel

枸橼酸坦度螺酮坦度螺酮 Chemical Name: 3aalpha,4alpha,5,6,7alpha,7aalpha-Hexahydro-2-[4- [4-(2-pyrimidinyl)-1-piperazinyl]butyl]-4,7-methano-1H-isoindole-1,3(2H)-dione dihydrogen citrate; (1R*,2S*,3R*,4S*)-N-[4-...
参考文献标题:Succimide derivatives,compositions and method of use
文献作者:Ishizumi,K.; Antoku,F.; Asami,Y.(Sumitomo Chemical Co.,Ltd.)
参考来源:CA 1184915; EP 0082402

Sildenafil citrate, UK-92480-10, UK-92480(free base), Penegra, Patrex, Wan Ai Ke, Viagra

枸橼酸西地那非西地那非 Chemical Name: 5-[2-Ethoxy-5-(4-methylpiperazin-1-ylsulfonyl)phenyl]-1-methyl-3-propyl-6,7-dihydro-1H-pyrazolo[4,3-d]pyrimidin-7-one citrate
CAS No. 171599-83-0, 139755-83-2 (free base...
参考文献标题:Pyrazolopyrimidinone antianginal agents
文献作者:Bell,A.S.; Brown,D.; Terrett,N.K.(Pfizer Inc.)
参考来源:EP 0463756; JP 1994041133; US 5250534; US 5346901

Ranitidine Bismutrex, Ranitidine bismuth citrate, GR-122311-X, Tritec, Pylorid

枸橼酸铋雷尼替丁Chemical Name: N-[2-[5-(Dimethylaminomethyl)furan-2-ylmethylsulfanyl]ethyl]-N'-methyl-2-nitroethene-1,1-diamine 2-hydroxypropane-1,2,3-tricarboxylate bismuth(3+) complex (1:1:1); N-[2-[5-[(Dim...
参考文献标题:Ranitidine derivs
文献作者:Clitherow,J.W.(Glaxo Wellcome plc)
参考来源:BE 1003254; CH 679582; GB 2220937; JP 1990117684; US 5008256

Bervastatin, LS-2904

柏伐他汀Chemical Name: (?-erythro-7-[4-(4-Fluorophenyl)spiro[2H-1-benzopyran-2,1'-cyclopentan]-3-yl]-3,5-dihydroxy-6(E)-heptenoic acid ethyl ester; (?-(3R*,5S*,6E)-7-[4-(4-Fluorophenyl)spiro[2H-1-benzopyr...
参考文献标题:Derivs.of benzocycloalkenyldihydroxyalkanoic acids,inhibitors of HMG-CoA reductase,antagonists of thromboxane A2 receptors and antifungals
文献作者:Festal,D.; Nioche,J.-Y.; Descours,D.; Bellemin,R.; Decerprit,J.(Lipha Sant?
参考来源:AU 9048797; EP 0380392; FR 2642065; JP 1990258738; US 5082859; US 5183924

Naringenin

柚皮素; 4',5,7-三羟基黄烷酮Chemical Name: (-)-5,7-Dihydroxy-2(S)-(4-hydroxyphenyl)-3,4-dihydro-2H-1-benzopyran-4-one
CAS No. 480-41-1
项目整合开发状态: Preclinical
项目研究机构:
合成路线:The condensation of phlorog...
参考文献标题:躡er die synthese des naringenins und phloretins
文献作者:Rosenmund,M.; Rosenmund,K.W.
参考来源:Ber 1928,612608-13

Salazodine, Salazopyridazin

柳氮定Chemical Name: 5-[[p-[(6-Methoxy-3-pyridazinyl)sulfamoyl]phenyl]azo]salicylic acid
CAS No. 22933-72-8
项目整合开发状态: Phase II
项目研究机构: Russian Academy of Medical Sciences (Originator)
合成路线:Th...
参考文献标题:SALAZODINE < Rec INN; NFN >
文献作者:Prous,J.; Castar,J.
参考来源:Drugs Fut 1989,14(1),33

Labetalol hydrochloride, AH-5158A, Sch-15719W, Amipress, Trandate, Normodyne

柳胺苄心定拉贝洛尔 Chemical Name: 2-Hydroxy-5-[1-hydroxy-2-(1-methyl-3-phenylpropylamino)ethyl]benzamide monohydrochloride
CAS No. 32780-64-6, 36894-69-6 (free base)
项目整合开发状态: Launched-1977
项目研究机构: ...
参考文献标题:Labetalol
文献作者:Castar,J.; Blancafort,P.
参考来源:Drugs Fut 1976,1(3),125

(+)-Resiniferatoxin, Resiniferatoxin, RTX-107, RTX

树脂毒素Chemical Name: 4-Hydroxy-3-methoxybenzeneacetic acid (2S,3aR,3bS,6aR,9aR,9bR,10R,11aR)-2-benzyl-6a-hydroxy-8,10-dimethyl-11a-(1-methylethenyl)-7-oxo-3a,3b,6,6a,9a,10,11,11a-octahydro-7H-2,9b-epoxy...
参考文献标题:The first synthesis of a daphnane diterpene: The enantiocontrolled total synthesis of resiniferatoxin
文献作者:Wender,P.A.; et al.
参考来源:J Am Chem Soc 1997,119(52),12976

Glimepiride, Hoe-490, Roname, Amaryl

格列美脲Chemical Name: 1-[4-[2-(3-Ethyl-4-methyl-2-oxo-2,5-dihydro-1H-pyrrol-1-carboxamido)ethyl]phenylsulfonyl]-3-(trans-4-methylcyclohexyl)urea
CAS No. 93479-97-1
项目整合开发状态: Launched-1996
项目研究机构...
参考文献标题:Sulfonylureas,process for their preparation,pharmaceutical compsns.containing them and their use
文献作者:Weyer,R.; Hitzel,V.; Geisen,K.; Regitz,G.(Aventis SA)
参考来源:EP 0031058; US 4379785

Glipalamide, SPC-703

格列酰胺Chemical Name: (?-5-Methyl-N-(p-tolylsulfonyl)-2-pyrazoline-1-carboxamide; (?-5-Methyl-1-(N-tosylcarbamoyl)-2-pyrazoline
CAS No. 37598-94-0
项目整合开发状态: Preclinical
项目研究机构: Med. Acad. (Origi...
参考文献标题:SPC-703
文献作者:Kolwas,J.
参考来源:Drugs Fut 1981,6(4),241