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

Azidothymidine phosphonate, Nicavir, Phosphazid, phAZT

3'-叠氮-3'-脱氧-5'-O-(羟基磷羧基酰)胸苷Chemical Name: 3'-Azido-3'-deoxy-5'-O-(hydroxyphosphonoyl)thymidine; 3'-Azido-3'-deoxythymidine 5'-(hydrogen phosphonate)
CAS No. 124930-59-2
项目整合开发状态: Phase I
项目研究...
参考文献标题:5'-Hydrogenphosphonates and 5'-methylphosphonates of sugar modified nucleosides,compsns.and uses thereof
文献作者:Krayevsky,A.A.; Tarussova,N.B.; Watanabe,K.A.; Matulic-Adamic,J.(Sloan-Kettering Institute)
参考来源:WO 9119727

MZPES

3-叠氮基乙胺嘧啶Chemical Name: 5-(3-Azido-4-chlorophenyl)-6-ethyl-2,4-pyrimidine-diamine monoethanesulfonate
CAS No. 95458-43-8, 95458-42-7 (diacetate), 95458-40-5 (free base), 95458-41-6 (monoHCl), 95458...
参考文献标题:Pyrimidine derivs.
文献作者:Bliss,E.A.; Griffin,R.J.; Stevens,M.F.G.(Aston University; Glaxo Wellcome plc)
参考来源:EP 0147443; GB 2152508; JP 1985502255; WO 8404746

A-192621

3-吡咯烷羧酸,4-(1,3-苯并二噁唑-5-基)-1-[2-[(2,6-二乙基苯基)氨基]-2-羰基乙基]-2-(4-丙氧基苯基)-,(2R,3R,4S)-Chemical Name: (2R,3R,4S)-4-(1,3-Benzodioxol-5-yl)-1-[N-(2,6-diethylphenyl)carbamoylmethyl]-2-(4-propoxyphenyl)pyrrolidin...
参考文献标题:4-(Benzo-1,3-dioxolyl)-pyrrolidine-3-carboxylic acid derivs.as endothelin antagonists
文献作者:Tasker,A.S.; Boyd,S.A.; Sorensen,B.K.; Winn,M.; Jae,H.-S.; Von Geldern,T.W.; Henry,K.J.(Abbott Laboratories Inc.)
参考来源:EP 0888340; JP 2000504727; WO 9730046

FK-687, TF-505, FR-146687

3-吲哚-丁酸,1-[4-[(1S)-1-[4-(2-甲基丙基)苯基]丁氧基]苯甲酰]-Chemical Name: 4-[1-[4-[1(S)-(4-Isobutylphenyl)butoxy]benzoyl]indolizin-3-yl]butyric acid
CAS No. 146939-64-2
项目整合开发状态: Phase II
项目研究机构: Fujisawa (...
参考文献标题:Indolizin derivs.,process for their preparation and pharmaceutical compsn.containing them
文献作者:Okada,S.; Sawada,K.; Kuroda,A.; Watanabe,S.; Tanaka,H.(Fujisawa Pharmaceutical Co.,Ltd.)
参考来源:EP 0519353; JP 1993178856; US 5334716

C-75

3-呋兰羧酸,四氢-4-甲基-2-辛基-5-氧-,(2R,3R)-rel- C75反式 Chemical Name: 4-Methylene-2-octyl-5-oxotetrahydrofuran-3-carboxylic acid
CAS No. 191282-49-2 (cis-isomer), 191282-48-1 (trans-isomer)
项目整合开发状态: Precl...
参考文献标题:Inhibition of fatty acid synthase as a means to reduce adipocyte mass
文献作者:Kuhajda,F.P.; Mani,N.S.; Pasternack,G.R.; Townsend,C.A.(Johns Hopkins University)
参考来源:WO 9718806

Y-34867

3-喹喹羧酸,1-环丙基-7-[2-[(二甲基氨基)甲基]-4-甲基苯丙基]-6-氟-1,4-二氢-8-甲氧基-4-氧基-Chemical Name: (-)-1-Cyclopropyl-7-[2(S)-(dimethylaminomethyl)morpholin-4-yl]-6-fluoro-8-methoxy-4-oxo-1,4-dihydro-3-quinolinecarboxylic ac...
参考文献标题:Synthesis and anti-Helicobacter pylori activity of Y-34867,a new 7-morpholinoquinolone
文献作者:Uemori,S.; Hirayama,F.; Moriguchi,A.; Sano,M.; Yokoyama,Y.; Ikeda,Y.; Miyoshi,M.; Sakurai,N.; Yamamoto,K.; Kawakita,T.
参考来源:38th Intersci Conf Antimicrob Agents Chemother (Sept 24 1998,San Diego) 1998,Abst F-85

TAK-603

3-喹喹羧酸,4-(3,4-二甲氧基苯基)-6,7-二甲氧基-2-(1H-1,2,4-三唑-1-酰甲基)-,乙酯Chemical Name: 4-(3,4-Dimethoxyphenyl)-6,7-dimethoxy-2-(1,2,4-triazol-1-ylmethyl)quinoline-3-carboxylic acid ethyl ester
CAS No. 158146-85-1<...
参考文献标题:Studies on disease-modifying antirheumatic drugs.III.Bone resorption inhibitory effects of ethyl 4-(3,4-dimethoxyphenyl)-6,7-dimethoxy-2-(1,2,4-triazol-1-ylmethyl)quinoline-3-carboxylate (TAK-603) and related compounds
文献作者:Baba,A.; Oda,T.; Taketomi,S.; Notoya,K.; Nishimura,A.; Makino,H.; Sohda,T.
参考来源:Chem Pharm Bull 1999,47(3),369

UR-7247

3-异丙基-1-丙基-5-[2'-(1H-四唑-5-基)双苯-4-甲基]-1H-吡拉唑-4-羧酸Chemical Name: 3-Isopropyl-1-propyl-5-[2'-(1H-tetrazol-5-yl)biphenyl-4-ylmethyl]-1H-pyrazole-4-carboxylic acid
CAS No. 177847-28-8
项目整合开发状态: Phase...
参考文献标题:New pyrazole derivs.as angiotensin II antagonists
文献作者:Almansa,C.; Gonzales,C.; Torres,M.C.; Carceller,E.; Bartroli,J.(J.Uriach & C韆.,SA)
参考来源:EP 0721454; ES 2105939; JP 1997504804; WO 9604273

Bemesetron, MDL-72222

3-托烷-3,5-二氯苯甲酸Chemical Name: 1alphaH,3alpha,5alphaH-Tropan-3-yl-3,5-dichlorobenzoate; 3,5-Dichlorobenzoic acid endo-8-methyl-8-azabicyclo[3.2.1]oct-3-yl ester
CAS No. 40796-97-2
项目整合开发状态: Phase ...
参考文献标题:Treatment og migraine with substituted tropyl benzoate derivatives
文献作者:Fozard,J.R.; Gittos,M.W.(Aventis Pharma SA)
参考来源:EP 0067770; JP 58000978

Butylidenephthalide

3-正丁烯基苯酞; 3-亚丁基-1(3H)-异苯并呋喃酮Chemical Name: 3-Butylidene-1(3H)-isobenzofuranone; 3-Butylidenephthalide
CAS No. 551-08-6
项目整合开发状态: Biological Testing
项目研究机构:
合成路线:This compound can be obtai...
参考文献标题:Butylidenephthalide
文献作者:Castar,J.; Blancafort,P.; Hillier,K.; Serradell,M.N.
参考来源:Drugs Fut 1981,6(4),216