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

(-)-Laulimalide, Fijianolide B, Laulimalide

(1R,3S,7S,8S,10S,12S,15Z,18R)-12-[(1S,2E)-3-[(2S)-3,6-dihydro-4-methyl-2H-pyran-2-基]-1-羟基-2-丙烯-1-基]-7-羟基-3-甲基-5-亚甲基-9,13,22-三氧三环[16.3.1.08,10]docosa-15,19-dien-14一Chemical Name: (1R,3S,7S,8S,10S,12S,1...
参考文献标题:Synthesis of the macrocyclic core of laulimalide
文献作者:Paterson,I.; De Savi,C.; Tudge,M.
参考来源:Org Lett 2001,3(2),213

MLN-519, LDP-519, PS-519

(1R,4R,5S)-1-[1(S)-羟基-2-甲基丙基]-4-丙基-6-氧-2-阿氮双环[3.2.0]庚烷-3,7-二酮Chemical Name: (1R,4R,5S)-1-[1(S)-Hydroxy-2-methylpropyl]-4-propyl-6-oxa-2-azabicyclo[3.2.0]heptane-3,7-dione
CAS No. 211866-70-5
项目整...
参考文献标题:Synthesis of clasto-lactacystin beta-lactone and analogs thereof
文献作者:Plamondon,L.; Soucy,F.; Behnke,M.; Roush,W.
参考来源:WO 9909006

LY-379268

(1R,4R,5S,6R)-4-氨基-2-氧杂双环[3.1.0]己烷-4,6-二羧酸 2-氧双环[3.1.0]己烷-4,6-二羧酸,4-氨基-, (1R,4R,5S,6R)-rel- (6Z)-4-氯-6-[(2-氯苯基)(丙基氨基)甲亚基]环己-2,4-二烯-1-酮Chemical Name: (1R,4R,5S,6R)-4-Amino-2-oxabicyclo[3.1.0]hexane-4,6...
参考文献标题:Excitatory amino acid derivs.
文献作者:Massey,S.M.; Monn,J.A.; Valli,M.J.(Eli Lilly and Company)
参考来源:EP 0774461; JP 2000500748; WO 9718199

Pd-Bacteriopheophorbide, WST-09, Pd-BPheid, Tookad

(1R,5S)-8-甲基-8-氮杂二环[3.2.1]辛-3-基2-甲基丙酸酯Chemical Name: Hydrogen [(22R,7R,8R,17S,18S)-3-[12-acetyl-7-ethyl-22-(methoxycarbonyl)-3,8,13,17-tetramethyl-21-oxo-21,22,7,8,17,18-hexahydrocyclopenta[at]porphyr...
参考文献标题:Palladium-substd.bacteriochlorophyll derivs.and use thereof
文献作者:Scherz,A.; Salomon,Y.; Scheer,H.; Brandis,A.(Yeda Research & Development Co.Ltd.)
参考来源:JP 2002531497; WO 0033833

PNU-109291

(1S)-1-{2-[4-(4-甲氧基苯基)-1-哌嗪基]乙基}-N-甲基-3,4-二氢-1H-异苯并吡喃-6-甲酰胺Chemical Name: (-)-1(S)-[2-[4-(4-Methoxyphenyl)piperazin-1-yl]ethyl]-N-methyl-3,4-dihydro-1H-2-benzopyran-6-carboxamide
CAS No. 187665-60-...
参考文献标题:1,6-Disubstd.isochromans for treatment of migraine headaches
文献作者:Ennis,M.D.; Tenbrink,R.E.(Pharmacia & Upjohn AB)
参考来源:EP 0836599; JP 1999509532; WO 9702259

BMS-187745

(1S)-4-(3-苯氧基苯基)-1-膦酰基丁烷-1-磺酸Chemical Name: (S)-(-)-4-(3-Phenoxyphenyl)-1-phosphonobutanesulfonic acid
CAS No. 157126-18-6
项目整合开发状态: Phase II
项目研究机构: Bristol-Myers Squibb (Originator)
合成路线...
参考文献标题:Alpha-phosphorous substd.sulfonate derivs.as squalene synthetase inhibitors
文献作者:Magnin,D.R.; Biller,S.A.; Dickson,J.K.Jr.; Lawrence,M.R.; Sulsky,R.B.(Bristol-Myers Squibb Co.)
参考来源:EP 0595635; JP 1994199879; US 5712396

RPR-100579, AMP-579

(1S,2R,3S,4R)-4-[7-[1(R)-(3-氯-2-噻基甲基)丙吡胺基]-3H-伊咪唑[4,5-b]吡啶-3-基]-N-乙基-2,3-二羟基环戊烷-1-羧酰胺Chemical Name: (1S,2R,3S,4R)-4-[7-[1(R)-(3-Chloro-2-thienylmethyl)propylamino]-3H-imidazo[4,5-b]pyridin-3-yl]-N-eth...
参考文献标题:Cpds.having antihypertensive and anti-ischemic pr
文献作者:Spada,A.P.; Fink,C.A.; Myers,M.R.(Aventis Pharma SA)
参考来源:EP 0550631; JP 1993508864; US 5217982; US 5364862; WO 9205177

EM-523

(1S,2R,3S,4S,5R,8R,9S,10R,11R)-8-乙基-2-[(2S,3R,4S,6R)-4-(乙基-甲基氨基)-3-羟基-6-甲基四氢吡喃-2-基]氧基-9,10-二羟基-4-[(2R,4R,5S,6S)-5-羟基-4-甲氧基-4,6-二甲基四氢吡喃-2-基]氧基-1,3,5,9,11,13-六甲基-7,15-二氧杂双环[10.2.1]十五碳-12-烯-6-酮Chemical N...
参考文献标题:Erythromycin derivs.and process for preparing the same
文献作者:Omura,S.; Itoh,Z.(Kitasato Institute)
参考来源:AU 8661583; EP 0215355; JP 1988099092; US 5175150

Tridolgosir hydrochloride, Swainsonine hydrochloride, GD-0039

(1S,2R,8R,8aR)-1,2,8-辛氢吲啰二烯酰盐酸盐八倾吲嗪三醇 Chemical Name: (-)-(1S,2R,8R,8aR)-Perhydroindolizine-1,2,8-triol hydrochloride; (-)-[5R-(5alpha,6alpha,7beta,8beta)]-1-Azabicyclo[4.3.0]nonane-5,7,8-triol hydroc...
参考文献标题:New chiral route to (-)-swainsonine via an aqueous acylnitroso cycloaddition approach
文献作者:Naruse,M.; et al.
参考来源:J Org Chem 1994,59(6),1358

Eglumetad hydrate, Eglumegad hydrate, LY-314582(racemate), LY-354740 monohydrate

(1S,2S,5R,6S)-2-氨基二环[3.1.0]己烷-2,6-二羧酸羊毛甾烷-18-酸,3b,11b-二羟基-,g-内酯,乙酸酯(8CI)Chemical Name: (+)-(1S,2S,5R,6S)-2-Aminobicyclo[3.1.0]hexane-2,6-dicarboxylic acid monohydrate
CAS No. 176199-48-7 (anhydrous...
参考文献标题:Bicyclohexane derivs.
文献作者:Dominguez Fernandez,C.; Ezquerra Carrera,J.; Baker,S.R.; Monn,J.A.(Eli Lilly and Company; Lilly SA)
参考来源:WO 0004010