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

4,6,4'-Trimethylangelicin, TMA

4,6,9-三甲基-2H-呋喃并[2,3-H]色满-2-酮Chemical Name: 4,6,9-Trimethyl-2H-furo[2,3-h]-1-benzopyran-2-one; 4-Hydroxy-beta,3,7-trimethyl-5-benzofuranacrylic acid delta-lactone
CAS No. 90370-29-9
项目整合开发状态: Bi...
参考文献标题:4,6,4'-Trimethylangelicin
文献作者:Bordin,F.; Dall'Acqua,F.; Cristofolini,M.; Guiotto,A.
参考来源:Drugs Fut 1985,10(4),307

KBG, BG

4,6-O-亚苄基d-葡萄糖 O4,O6-((R)-亚苄基)-D-葡萄糖 Chemical Name: 4,6-O-Benzylidene-D-glucose
CAS No. 30688-66-5, 83212-64-0 (R-isomer)
项目整合开发状态: Phase II
项目研究机构: Kaken (Originator)
合成路线:By reaction of ...
参考文献标题:KBG
文献作者:Prous,J.; Castar,J.
参考来源:Drugs Fut 1988,13(9),829

Gavestinel sodium, GV-150526A

4,6-二氯-3-[(1e)-3-氧代-3-(苯氨基)-1-丙基]-1h-吲哚-2-羧酸钠Chemical Name: 4,6-Dichloro-3-[2(E)-(N-phenylcarbamoyl)vinyl]-1H-indole-2-carboxylic acid sodium salt
CAS No. 153436-22-7 (free acid)
项目整合开发状态: Phase...
参考文献标题:3-(2-Carboxyindol-3-yl)propionic acid derivatives: Antagonists of the strychnine-insensitive glycine receptor associated with the N-methyl-D-aspartate receptor complex
文献作者:Salituro,F.G.; et al.
参考来源:J Med Chem 1990,33(11),2946-8

GV-196771A

4,6-二氯-3-[(E)-(2-氧代-1-苯基吡咯烷-3-亚基)甲基]-1H-吲哚-2-羧酸钠 4,6-二氯-3-[(E)-(2-氧代-1-苯基-3-吡咯烷基亚基)甲基]-1H-吲哚-2-羧酸 Chemical Name: (E)-4,6-Dichloro-3-(2-oxo-1-phenylpyrrolidin-3-ylidenemethyl)-1H-indole-2-carboxylic ac...
参考文献标题:Substituted indole-2-carboxylates as in vivo potent antagonists acting at the strychnine-insensitive glycine binding site
文献作者:Di Fabio,R.; Capelli,A.M.; Conti,N.; Cugola,A.; Donati,D.; Feriani,A.; Gastaldi,P.; Gaviraghi,G.; Hewkin,C.T.; Micheli,F.; Missio,A.; Mugnaini,M.; Pecunioso,A.; Quaglia,A.M.; Ratti,E.; Rossi,L.; Tedesco,G.; Trist,D.G.; Reggiani,A.
参考来源:J Med Chem 1997,40(6),841-850

Oxipurinol, Oxypurinol, NSC-76239, Oxyprim

4,6-二羟基吡唑啉[3,4-d]嘧啶Chemical Name: 1H-Pyrazolo[3,4-d]pyrimidine-4,6-diol
CAS No. 2465-59-0
项目整合开发状态: Pre-Registered
项目研究机构: Cardiome (Proprietary), Cardiome (Orphan Drug), Ilex Oncology (Orpha...
参考文献标题:Treatment of hyperuricemia in humans
文献作者:Hitchings,G.H.; Falco,E.A.(GlaxoSmithKline Inc.)
参考来源:GB 0798646; US 3624205

AS-601811

4,8-二甲基-2,3,5,6-四氢-1H-苯二氮卓[c]喹喹-3-酮Chemical Name: 4,8-Dimethyl-2,3,5,6-tetrahydro-1H-benzo[c]quinolizin-3-one
CAS No. 194979-95-8
项目整合开发状态: Phase I
项目研究机构: Serono (Originator), Universit?degl...
参考文献标题:Benzo[c]quinolizine derivs.,their preparation and use as 5alpha-reductases inhibitors
文献作者:Guarna,A.; Serio,M.(Applied Research Systems ARS Holdings NV)
参考来源:EP 0880520; JP 2000504680; WO 9729107

SCH-60663

4-[(2S,3R)-1-(4-氟苯基)-3-[(3S)-3-(4-氟苯基)-3-羟基丙基]-4-氧代-2-氮杂环丁基]苯基beta-D-吡喃葡糖苷酸Chemical Name: 1-O-[4-[(2S,3R)-1-(4-Fluorophenyl)-3-[3(S)-(4-fluorophenyl)-3-hydroxypropyl]-4-oxo-2-azetidinyl]phenyl]-beta-D...
参考文献标题:Sugar-substd.2-azetidinones useful as hypocholesterolemic agents
文献作者:Yumibe,N.P.; Alton,K.B.; Van Heek,M.; Davis,H.R.; Vaccaro,W.D.(Schering Corp.)
参考来源:EP 0877750; JP 1998512592; WO 9716455

YM-274, PG-490-88

4-[(3bS,4aS,5aR,6R,6aS,7aS,7bS,8aS,8bS)-6a-异丙基-8b-甲基-1-氧代-1,3,3b,4,4a,6,6a,7a,7b,8b,9,10-十二氢三氧基酸盐[6,7:8a,9:4b,5]phenanthro[1,2-c]呋喃-6-酰氧基]-4-氧丁酸钠盐昂曲托来 Chemical Name: 4-[(3bS,4aS,5aR,6R,6aS,7aS,7bS,8...
参考文献标题:Immunosuppressive cpds.and methods
文献作者:Qi,Y.M.; Musser,J.H.; Fidler,J.M.(Pharmagenesis,Inc.)
参考来源:EP 0907652; JP 2001504437; US 5663335; US 5962516; WO 9731920; WO 9731921

Z-4105

4-[(3-甲基-1,2-恶唑-5-羰基)氨基]丁酸Chemical Name: N-(3-Carboxypropyl)-3-methylisoxazole-5-carboxamide; 4-(3-Methylisoxazol-5-ylcarboxamido)butyric acid
CAS No. 119737-52-9
项目整合开发状态: Preclinical
项目研究机构...
参考文献标题:Isoxazoles with nootropic activity
文献作者:Carenzi,A.; Chiarino,D.; Della Bella,D.; Napoletano,M.; Sala,A.(Zambon Group SpA)
参考来源:AU 8817869; EP 0317588; JP 1990500365; US 4985428; WO 8809330

YM-511

4-[(4-溴苯基)甲基-(1,2,4-三唑-4-基)氨基]苯甲腈Chemical Name: 4-[N-(4-Bromobenzyl)-N-(4-cyanophenyl)amino]-4H-1,2,4-triazole; 4-[N-(4-Bromobenzyl)-N-(1,2,4-triazol-4-yl)amino]benzonitrile
CAS No. 148869-05-0
...
参考文献标题:Triazolylated tertiary amine cpds.or salts thereof
文献作者:Okada,M.; Kawaminami,E.; Yoden,T.; Kudo,M.; Isomura,Y.(Yamanouchi Pharmaceutical Co.,Ltd.)
参考来源:EP 0641785; JP 1993505096; US 5674886; WO 9305027