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

(+)-Calanolide A, Calanolide A, NSC-675451, NSC-664737(racemate)

(10R,11S,12S)-11,12-二氢-12-羟基-6,6,10,11-四甲基-4-丙基-2H,6H,10H-苯并(1,2-b:3,4-b':5,6-b'')三吡喃-2-酮 (10S,11R,12R)-12-羟基-6,6,10,11-四甲基-4-丙基-11,12-二氢-2H,6H,10H-二吡喃并[2,3-f:2',3'-h]色烯-2-酮 Chemical Name: (+)-(10R,11...
参考文献标题:Calanolide antiviral cpds.,compsns.and uses ther
文献作者:Boyd,M.R.; Cardellina,J.H.II; Gustafson,K.R.; McMahon,J.B.; Fuller,R.W.; Cragg,G.M.; Kashman,Y.(US Department of Health & Human Services)
参考来源:EP 0633887; JP 1996502948; JP 1996507311; US 5591770; WO 9320082; WO 9428000

NSC-694501, UP-2001, NSC-D694501, SJG-136, SP-2001

(11AS,11A'S)-8,8'-(丙烷-1,3-二基双(氧))双(7-甲氧基-2-亚甲基-2,3-二氢-1H-苯并[E]吡咯[1,2-A][1,4]二氮杂卓-5(11AH)-酮)Chemical Name: (11aS,11'aS)-8,8'-(1,3-Propanediyl)bis(oxy)bis(7-methoxy-2-methylene-1,2,3,11a-tetrahydro-5H-p...
参考文献标题:Compounds
文献作者:Thurston,D.E.; Howard,P.W.(University of Portsmouth)
参考来源:EP 1109812; WO 0012508

RU-58668

(11β,17β)-11-[4-({5-[(4,4,5,5,5-五氟戊基)磺酰基]戊基}氧基)苯基]雌二醇-1,3,5(10)-三烯-3,17-二醇Chemical Name: 11beta-[4-[5-(4,4,5,5,5-Pentafluoropentylsulfonyl)pentyloxy]phenyl]estra-1,3,5(10)-trien-3,17beta-diol
CAS N...
参考文献标题:Novel 19-nor steroids having a thiocarbon-containing chain in the 11beta position,a method for preparing same and intermediates therefor,medicinal uses thereof and compsns.containing said steroids
文献作者:Claussner,A.; Nique,F.; Teutsch,J.-G.; Van De Velde,P.(Aventis Pharma SA)
参考来源:EP 0623140; JP 1995502281; WO 9313123

RU 16117

(17R)-11alpha-甲氧基-19-去甲孕甾-1,3,5(10)-三烯-20-炔-3,17-二醇Chemical Name: (11alpha,17alpha)-11-Methoxy-19-norpregna-1,3,5(10)-trien-20-yne-3,17-diol
CAS No. 61665-15-4
项目整合开发状态: Biological Testing
项目...
参考文献标题:RU-16117
文献作者:Azadian-Boulanger,G.; Raynaud,J.P.
参考来源:Drugs Fut 1985,10(5),926

Diepoxin-sigma, Sch-49209, LL-07F275-sigma

(1aS-(1aalpha,2abeta,6alpha,6abeta,7aalpha))-6-羟基-螺(2a,6a-环氧萘并(2,3-b)环氧乙烯-2(1aH),2'-萘并(1,8-去)(1,3)二恶英)-3,7(6H,7aH)-二酮Chemical Name: (+)-(2R,3S,4aR,5S,8aR)-2,3:4a,8a-Diepoxy-5-hydroxy-1,2,3,4,4a,5,8,8a...
参考文献标题:Formal total synthesis of (+)-diepoxin sigma
文献作者:Wipf,P.; Jung,J.-K.
参考来源:J Org Chem 2000,65(20),6319

FR-66973, FK-973

(1aS,3S,8R,9S,9aS)-1-乙酰基-7,9-二(乙酰氧基)-8-(((氨基羰基)氧基)甲基)-1,1a,2,8,9,9a-六氢-3,9-环氧-3H-氮丙啶并(2,3-c)苯并氮杂环辛四烯-5-甲醛 3,9-环氧-3H-阿锹铉[2,3-c][1]苯扎唑辛-5-羧醛,1-乙酰-7,9-双(乙酰氧)-8-[[(氨基羰基)氧]甲基]-1,1a,2,8,9,9a-六氢-(9CI) Chemic...
参考文献标题:New tetracyclo cpds.,a process for their production and a pharmaceutical compsn.containing the same
文献作者:Kohsaka,M.; Terano,H.; Komori,T.; Iwami,M.; Yamashita,M.; Hashimoto,M.; Uchida,I.; Takase,S.(Fujisawa Pharmaceutical Co.,Ltd.)
参考来源:AU 8543728; EP 0166389; ES 8703477; ES 8707961; ES 8707962; JP 1986010590; JP 1989199975; JP 1995067623; US 4645765; US 4861774

Chlorocitrate, Ro-21-7716

(1R,2R)-1-氯-2-羟基丙烷-1,2,3-三羧酸Chemical Name: (1R,2R)-1-Chloro-2-hydroxy-1,2,3-propanetricarboxylic acid; (-)-threo-Chlorocitric acid
CAS No. 76432-78-5
项目整合开发状态: Biological Testing
项目研究机构: Roch...
参考文献标题:Chlorocitric acids
文献作者:Guthrie,R.W.; Kierstead,R.W.; Mennona,F.A.; Sullivan,A.C.(Hoffmann-La Roche,Inc.)
参考来源:JP 1010496B; JP 1528137C; JP 55089243; US 4312885

S-23906, S-23906-1

(1R,2R)-REL-1,2-二(乙酰氧基)-1,2,3,14-四氢-6-甲氧基-3,3,14-三甲基-7H-苯并[B]吡喃并[3,2-H]吖啶-7-酮Chemical Name: (?-cis-1,2-Bis(acetoxy)-6-methoxy-3,3,14-trimethyl-2,3,7,14-tetrahydro-1H-benzo[b]pyrano[3,2-h]acridin-7-one...
参考文献标题:Novel acronycine derivs.,preparation method and pharmaceutical compsns.
文献作者:Pfeiffer,B.; Michel,S.; Koch,M.; Pierre,A.; Renard,P.; Tillequin,F.; Atassi,G.(ADIR et Cie.)
参考来源:EP 1042326; FR 2772765; WO 9932491

Altropane, IACFT, Altropane

(1R,2S,3S,5S)-3-(4-氟苯基)-8-[(E)-3-碘丙-2-烯基]-8-氮杂双环[3.2.1]辛烷-2-羧酸甲酯Chemical Name: (1R,2S,3S,5S)-3-(4-Fluorophenyl)-8-[3-iodo-2(E)-propenyl]-8-azabicyclo[3.2.1]octane-2-carboxylic acid methyl ester
CAS...
参考文献标题:Substd.2-carboxyalkyl-3-(fluorophenyl)-8-(3-haloprofen-2-yl) nortropanes and their use as imaging agents for neurodegenerative disorders
文献作者:Elmaleh,D.R.; Madras,B.K.; Meltzer,P.; Hanson,R.N.(General Hospital Corporation; Harvard College; Northeastern University)
参考来源:EP 0734385; EP 1081147; WO 9511901

Iometopane, GPI-200, beta-CIT, RTI-55, Dopascan

(1R,2S,3S,5S)-3-(4-碘苯基)-8-甲基-8-氮杂双环[3.2.1]辛烷-2-羧酸甲酯 (123I)-2beta-甲氧羰基-3beta-(4-碘苯基)莨菪烷 Chemical Name: (-)-1(R)-3-exo-(4-Iodophenyl)-8-methyl-8-azabicyclo[3.2.1]octan-2-exo-yl-carboxylic acid methyl es...
参考文献标题:Synthesis,ligand binding,QSAR,and CoMFA study of 3beta-(p-substituted phenyl)tropane-2beta-carboxylic acid methyl esters
文献作者:Carroll,F.I.; Gao,Y.G.; Rahman,M.A.; Abraham,P.; Parham,K.; Lewin,A.H.; Boja,J.W.; Kuhar,M.J.
参考来源:J Med Chem 1991,34(9),2719