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

21-Aminoepothilone B, BMS-310705

21-氨基埃坡霉素 BChemical Name: [1S,3S(E),7S,10R,11S,12S,16R]-3-[2-[2-(Aminomethyl)thiazol-4-yl]-1-methylvinyl]-7,11-dihydroxy-8,8,10,12,16-pentamethyl-4,17-dioxabicyclo[14.1.0]heptadecane-5,9-dione; (4S,7R...
参考文献标题:C-21 modified epothilones
文献作者:Kim,S.-H.; Glaser,N.; Leibold,T.; Hoefle,G.; Vite,G.(Bristol-Myers Squibb Co.; Gesellschaft f黵 Biotechnologische Forschung mbH)
参考来源:DE 19907588; EP 1157023; US 6262094; WO 0050423

Lodenosine, NSC-613792, DDG-1, 2'-F-dd-ara-A, FddA

2'-BETA-氟-2',3'-二脱氧腺苷Chemical Name: 2',3'-Dideoxy-2'beta-fluoroadenosine; 9-(2,3-Dideoxy-2-fluoro-beta-D-threo-pentofuranosyl)adenine; 9-(2,3-Dideoxy-2-fluoro-beta-D-arabinofuranosyl)adenine
CAS No...
参考文献标题: D-Xylofuranose derivs.,method of preparing them,their use,and novel intermediate compounds for the method
文献作者:Saischek,E.; Dax,K.; Braun,W.; Fuchs,F.; Saischek,G.(Chevron Research Co.)
参考来源:WO 9606851

RPR-110754((-)-enantiomer), RPR-110750((+)-enantiomer), RPR-104632

2H-1,2,4-苯并噻二嗪-3-羧酸,2-[(3-溴苯基)甲基]-6,8-二氯-3,4-二氢-,1,1-二氧化物Chemical Name: 2-(3-Bromobenzyl)-6,8-dichloro-3,4-dihydro-2H-1,2,4-benzothiadiazine-3-carboxylic acid 1,1-dioxide
CAS No. 154106-92-0
项目整...
参考文献标题:RPR 104632,a novel antagonist at the glycine site of the N-methyl-D-aspartate receptor-channel complex
文献作者:Doble,A.; Boireau,A.; et al.
参考来源:Can J Physiol Pharmacol 1994,72(Suppl.1),333

Perfosfamide, NPC-15520, 4-HPCy, 40,487, NSC-181815, 4-HC

2H-1,3,2-氧氮磷-2-胺,N,N-双(2-氯乙基)四氢-4-氢过氧-,2-氧化物,(2R,4R)-rel- 培磷酰胺 Chemical Name: (?-cis-2-[Bis(2-chloroethyl)amino]tetrahydro-2H-1,3,2-oxazaphosphorin-4-yl hydroperoxide P-oxide; (?-cis-2-[Bis(2-chloroet...
参考文献标题:Hydroperoxy substituted cyclic phosphamides
文献作者:Takamizawa,A.; Iwata,T.(Shionogi & Co.Ltd.)
参考来源:DE 2231311; FR 2147956; US 3808297

Bemoradan, RWJ-22867, Orf-22867

2H-1,4-苯并嗪-3(4H)-酮,7-(1,4,5,6-四氢-4-甲基-6-氧-3-吡啶达肼)- 贝莫拉旦 Chemical Name: (?-5-Methyl-6-(3-oxo-3,4-dihydro-2H-1,4-benzoxazin-7-yl)-2,3,4,5-tetrahydropyridazin-3-one; (?-7-(1,4,5,6-Tetrahydro-4-methyl-6-o...
参考文献标题:Bemoradan and related pyridazinone cardiotonics
文献作者:Combs,D.W.
参考来源:Drugs Fut 1993,18(2),139

SC-41930

2H-1-苯并吡啶-2-羧酸,7-[3-(4-乙酰-3-甲氧基-2-丙基苯氧基)丙氧]-3,4-二氢-8-丙基-Chemical Name: 7-[3-(4-Acetyl-3-methoxy-2-propylphenoxy)propoxy]-8-propyl-3,4-dihydro-2H-1-benzopyran-2-carboxylic acid
CAS No. 120072-59-5 参考文献标题:7-[3-(4-Acetyl-3-methoxy-2-propylphenoxy)propoxy]-3,4-dihydro-8-propyl- 2H-1-benzopyran-2-carboxylic acid: An orally active selective leukotriene B4 receptor antagonist
文献作者:Djuric,S.W.; Collins,P.W.; Jones,P.H.; et al.
参考来源:J Med Chem 1989,32(6),1145-7

Picumast dihydrochloride, BM-15100, Auteral

2H-1-苯并吡喃-2-1,7-[3-[4-[(4-氯苯基)甲基]-1-吡嗪基丙氧盐]-3,4-二甲基-盐酸盐(1:2)Chemical Name: 1-(4-Chlorobenzyl)-4-[3-(3,4-dimethylcoumarin-7-yloxy)propyl]piperazine dihydrochloride; 7-[3-[4-[(4-Chlorophenyl)methyl]-1-p...
参考文献标题:Coumarin-7-yloxyalkyl piperazine compounds
文献作者:Witte,E.C.; et al.(Boehringer Ingelheim GmbH)
参考来源:DE 2123924; FR 2137731; GB 1335946; JP 58219176; US 3810898

Ensaculin hydrochloride, Anseculin hydrochloride, KA-672.HCl

2H-1-苯甲基-2-1,7-甲氧基-6-[3-[4-(2-甲氧基苯基)-1-吡喃嗪基]丙氧盐]-3,4-二甲基-Chemical Name: 7-Methoxy-6-[3-[4-(2-methoxyphenyl)piperazin-1-yl]propoxy]-3,4-dimethyl-2H-1-benzopyran-2-one hydrochloride
CAS No. 155773-59...
参考文献标题:Benzopyranones,a method for producing them and uses therefor
文献作者:Chatterjee,S.S.; N鰈dner,M.; Hauer,H.(Willmar Schwabe GmbH)
参考来源:DE 4111861; JP 1994506922; US 5428038; WO 9218493

BPDZ-44

2H-吡啶[4,3-e]-1,2,4-噻二嗪-3-胺,N-(1,2-二甲基丙基)-,1,1-二氧化物Chemical Name: 3-(1,2-Dimethylpropylamino)-4H-pyrido[4,3-e]-1,2,4-thiadiazine-1,1-dioxide
CAS No. 152382-67-7
项目整合开发状态: Preclinical
项目研究机构: U...
参考文献标题:Preparation and pharmacological evaluation of the R- and S-enantiomers of 3-(2'-butylamino)-4H- and 3-(3'-methyl-2'-butylamino)-4H-pyrido[4,3-e]-1,2,4-thiadiazine 1,1-dioxide,two tissue selective ATP-sensitive potassium channel openers
文献作者:Khelili,S.; de Tullio,P.; Lebrun,P.; Fillet,M.; Antoine,M.H.; Ouedraogo,R.; Dupont,L.; Fontaine,J.; Felekidis,A.; Leclerc,G.; Delarge,J.; Pirotte,B.
参考来源:Bioorg Med Chem 1999,7(8),1513

AA-2379

2H-吡拉唑[3,4-d]嘧啶-2-羧酸,7-丁基-4,5,6,7-四氢-3-(甲基氨基)-4,6-二氧基-5-丙基-,甲基酯Chemical Name: 7-Butyl-3-(methylamino)-4,6-dioxo-5-propyl-4,5,6,7-tetrahydro-2H-pyrazolo[3,4-d]pyrimidine-2-carboxylic acid methyl ester<...
参考文献标题:3-Aminopyrazolo(3,4-d)pyrimidine derivs.and production thereof
文献作者:Furukawa,Y.; Maki,Y.(Takeda Chemical Industries,Ltd.)
参考来源:EP 0166054