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

EMD-57439((-)-enantiomer), EMD-53998(racemate), EMD-57033

(+)-5-[1-(3,4-二甲氧基苯甲酰)-1,2,3,4-四氢喹啉-6-基]-6-甲基-3,6-二氢-2H-1,3,4-噻二嗪-2-酮Chemical Name: (+)-5-[1-(3,4-Dimethoxybenzoyl)-1,2,3,4-tetrahydroquinolin-6-yl]-6-methyl-3,6-dihydro-2H-1,3,4-thiadiazin-2-one
C...
参考文献标题:Thiadiazinones
文献作者:Jonas,R.; Piulats,J.; Lues,I.; Klockow,M.(Merck Patent GmbH)
参考来源:AU 8816646; DE 3719031; DE 3744149; EP 0294647; JP 1988310886; US 4916128

Himbacine

(+)-喜巴辛Chemical Name: (+)-(3S,3aR,4S,4aS,8aR,9aS)-4-[(E)-2-[1,6(S)-Dimethylpiperidin-2(R)-yl]vinyl]-3-methyldecahydronaphtho[2,3-c]furan-1(3H)-one
CAS No. 6879-74-9
项目整合开发状态: Preclinical
项目研究...
参考文献标题:A novel total synthesis of (+)-himbacine,a potent antagonist of the muscarinic receptor of M-2 subtype
文献作者:Takadoi,M.; et al.
参考来源:Tetrahedron Lett 1999,40(17),3399

CV-3988

(±)-[3-(N-十八烷基氨基甲酰氧)-2-甲氧基]丙基-2- 噻唑乙基磷酸Chemical Name: (?-3-(4-Hydroxy-7-methoxy-10-oxo-3,5,9-trioxa-11-aza-4-phosphanonacos-1-yl)thiazolium hydroxide,inner salt P-oxide
CAS No. 85703-73-7
项目整合开发...
参考文献标题:Carbamic acid esters,their production and use
文献作者:Nomura,H.; Hozumi,M.; Yoshioka,Y.(Takeda Chemical Industries,Ltd.)
参考来源:EP 0035375

Proxodolol

(±)-1-(叔丁胺)-3-[2-(3-甲基-1,2,4-噁二唑-5-甲氧基)苯氧基]-2-盐酸丙醇 2-丙醇,1-[(1,1-二甲基乙基)氨基]-[2-[(3-甲氧基-1,2,4-噁二唑-5-基)甲氧基]-,盐酸盐(1:1) 1-(叔丁基乙氨基)-3-{2-[(3-甲基-1,2,4-噁二唑-5-基)甲氧基]苯氧基}丙烷-2-醇Chemical Name: (?-1-(tert-Butylamin...
参考文献标题:The hydrochlorides of derivs.of 5-phenoxymethyl-1,2,4-oxadiaxole,possessing beta- and alpha-adrenoblocking activities
文献作者:Sokolov,S.D.; Vinogradova,S.M.; Azarevich,O.G.; Berg,M.V.; Mashkovski,M.D.; Yuzhakov,S.D.; Morozov,A.V.(Center for Chemistry of Drugs)
参考来源:SU 1132505

ICI-118551

(±)-1-[2,3-(二氢-7-甲基1H-茚-4-基)氧]-3-[(1-甲基乙基)氨基]-2-丁醇盐酸盐Chemical Name: erythro-DL-1-(7-Methylindan-4-yloxy)-3-isopropylamino-2-butanol; (R*,S*)-(?-1-[(2,3-Dihydro-7-methyl-1H-inden-4-yl)oxy]-3-[(1-methyl...
参考文献标题:Alkanolamine derivs.,process for their preparation and pharmaceutical compsns.containing them
文献作者:Tucker,H.(AstraZeneca plc)
参考来源:EP 0003664

Dabelotine mesilate, S-12024-2

(±)-1-甲基-8-(吗啡烯-2-甲氧基)-1,2,3,4-四氢喹啉甲烷磺酸盐达贝洛汀 Chemical Name: (?-1-Methyl-8-(morpholin-2-ylmethoxy)-1,2,3,4-tetrahydroquinoline methanesulfonate
CAS No. 153049-48-0, 118976-38-8 (free base)
项目整合开...
参考文献标题:Novel morpholine derivs.,process for their preparation and pharmaceutical compsns.containing them
文献作者:R間nier,G.; Guillonneau,C.; Lepagnol,J.(ADIR et Cie.)
参考来源:AU 8813520; EP 0286495; FR 2612926; JP 1988255279; US 4782054

SK&F-38393

(±)-1-苯基-2,3,4,5-四氢-(1H)-3-苯并ze庚因-7,8-二醇氢溴酸盐1H-3-苯甲西平-7,8-二醇,2,3,4,5-四氢-1-苯基-,(1R)-Chemical Name: 2,3,4,5,-Tetrahydro-7,8-dihydroxy-1-phenyl-1H-3-benzazepine; 2,3,4,5-Tetrahydro-1-phenyl-1H-3-benzazep...
参考文献标题:SKF-38393
文献作者:Castar,J.; Hillier,K.
参考来源:Drugs Fut 1980,5(10),507

8-OH-DPAT HBr

(±)-8-羟基-2-(二丙基氨基)四氢萘氢溴酸盐Chemical Name: 8-Hydroxy-2-(di-N-propylamino)tetralin hydrobromide; 7-(Di-N-propylamino)-5,6,7,8-tetrahydro-1-naphthalenol hydrobromide
CAS No. 87394-87-4, 80300-08-9 (fre...
参考文献标题:8-OH-DPAT Hydrobromide
文献作者:Arvidsson,L.-E.
参考来源:Drugs Fut 1985,10(11),916

Epibatidine, CMI-477(enantiomer), CMI-545(racemate (exo)-isomer), CMI-488

(±)-三色素蛙素 (1S,4R,6S)-6-(6-氯吡啶-3-基)-7-氮杂双环[2.2.1]庚烷 Chemical Name: (1R,2R,4S)-2-(6-Chloro-3-pyridyl)-7-azabicyclo[2.2.1]heptane; (1R-exo)-2-(6-Chloro-3-pyridyl)-7-azabicyclo[2.2.1]heptane
CAS No. 14...
参考文献标题:Total synthesis of epibatidine
文献作者:Broka,C.A.
参考来源:Tetrahedron Lett 1993,34(20),3251-4

Butaclamol hydrochloride, AY-23028

(±)-盐酸丁那莫尔布他拉莫 Chemical Name: 3alpha-tert-Butyl-2,3,4,4abeta,8,9,13balpha,14-octahydro-1H-benzo[6,7]cyclopenta-[1,2,3-de]pyrido[2,1-a]isoquinolin-3-ol hydrochloride; [4a,13b-trans][3(OH),13b(H)-trans...
参考文献标题:Butaclamol
文献作者:Chatterjee,S.S.; Castar,J.
参考来源:Drugs Fut 1976,1(4),171