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

L-784506

3-[4-(甲基磺酰)苯基]-2-(3-吡啶)-2-环戊烯-1-酮Chemical Name: 3-[4-(Methylsulfonyl)phenyl]-2-(3-pyridyl)-2-cyclopenten-1-one
CAS No. 190966-40-6, 198985-43-2 (hydrochloride), 198985-44-3 (methanesulfonate)
项目...
参考文献标题:Pyridinyl-2-cyclopenten-1-ones as selective cyclooxygenase-2 inhibitors
文献作者:Black,C.; Hughes,G.; Wang,Z.(Merck Frosst Canada Inc.)
参考来源:EP 0900201; JP 2000509032; US 5922742; WO 9740012

SB-219994

3-[4-[2-[N-(2-苯氧基)-N-甲基氨基]苯基]-2(S)-(2,2,2-三氟乙氧基)丙酸Chemical Name: 3-[4-[2-[N-(2-Benzoxazolyl)-N-methylamino]ethoxy]phenyl]-2(S)-(2,2,2-trifluoroethoxy)propionic acid
CAS No. 177785-17-0
项目整合开发状态:...
参考文献标题:Benzoxazoles and pyridine derivs.useful in the treatment of type II diabetes
文献作者:Haigh,D.; Rami,H.K.(SmithKline Beecham plc)
参考来源:EP 0772605; JP 1998503508; WO 9604260; WO 9604261

KF-38789

3-[7-(2,4-二甲氧基苯基)-2,3,6,7-四氢-1,4-硫氮杂卓-5-基]-4-羟基-6-甲基-2H-吡喃-2-酮Chemical Name: 3-[7-(2,4-Dimethoxyphenyl)-2,3,6,7-tetrahydro-1,4-thiazepin-5-yl]-4-hydroxy-6-methyl-2H-pyran-2-one
CAS No. 257292-29-8<...
参考文献标题:Substd.1,4-thiazepine and analogs as activators of caspases and inducers of apoptosis and the use thereof
文献作者:Cai,S.X.; Spencer,J.R.; Litvak,J.; Drewe,J.A.; Shelton,E.J.; Sperandio,D.(Cytovia,Inc.)
参考来源:WO 0179187

Flubichin methanesulfonate, VUFB-12950

3-{2-[(2',4'-二氟be苯基-4-基)氧]乙基}喽那唑仑-4(3H)-酮Chemical Name: 3-[2-(2',4'-Difluorobiphenyl-4-yloxy)ethyl]quinazoline-4(3H)-one methanesulfonate
CAS No. 131587-93-4 (free base), 131587-94-5 (HCl)
项目整合开...
参考文献标题:Ether deriv.of 4-[3H]-quinazoline,a process for the preparation thereof,and pharmaceutical compsns
文献作者:Fisnerov? L.; Brunov? B.; Maturov? E.; Grimov? J.(SPOFA - United Pharmaceutical Works)
参考来源:AU 8942880; EP 0367944; JP 1990172977

FK-3657, FR-173657

3-6-(乙酰胺)-3-吡啶-N-2-2,4-二氯-3-(2-甲基-8-喹啉基)氧甲基苯基甲基氨基-2-氧乙基-(E)-2-丙胺Chemical Name: 3-(6-Acetamido-3-pyridyl)-N-[N-[2,4-dichloro-3-(2-methylquinolin-8-yloxymethyl)phenyl]-N-methylcarbamoylmethyl]-2(E)-prop...
参考文献标题:Pyridopyrimidones,quinolines and fused N-heterocycles as bradykinin antagonists
文献作者:Oku,T.; Kayakiri,H.; Satoh,S.; Abe,Y.; Sawada,Y.; Inoue,T.; Tanaka,H.(Fujisawa Pharmaceutical Co.,Ltd.)
参考来源:EP 0807105; JP 1998507764; WO 9613485

R-1559, BN-80927

3H,15H-氧西环醇[3',4':6,7]吲哚啉[1,2-b]喹啉-3,15-二酮,9-氯-5-乙基-1,4,5,13-四氢-5-羟基-10-甲基-12-[(4-甲基-1-哌啶基)甲基]-盐酸盐(1:1),(5R)- 依洛替康 Chemical Name: (+)-9-Chloro-5(R)-ethyl-5-hydroxy-10-methyl-12-(4-methylpiperidin-1-y...
参考文献标题:Optically pure camptothecin analogues,optically pure synthesis intermediate and method for preparing same
文献作者:Cazaux,J.-B.; Manginot,E.; Lavergne,O.; Le Breton,C.; Bigg,D.(SCRAS (Societ?de Conseils de Recherches et d'Applications Scientifiques))
参考来源:EP 1007527; FR 2768431; WO 9911646

FTC-092

3'-O-苄基-2'-脱氧-5-三氟甲基尿苷Chemical Name: 1-(3-O-Benzyl-2-deoxy-beta-D-ribofuranosyl)-5-(trifluoromethyl)-2,4(1H,3H)-pyrimidinedione; 3'-O-Benzyl-2'-deoxy-5-(trifluoromethyl)uridine; alpha,alpha,alpha-Trif...
参考文献标题:Novel 2'-deoxy-5-substd.uridine derivs.,processes for preparing the same and antitumor agent containing the same
文献作者:Fujii,S.; Yamashita,J.; Matsumoto,H.; Takeda,S.; Terada,T.; Yasumoto,M.; Unemi,N.(Taiho Pharmaceutical Co.,Ltd.)
参考来源:EP 0129984; ES 8606381; ES 8606382; ES 8607982; ES 8706715; JP 1984216899; JP 1985061591

Umespirone, KC-9172

3-丁基-7-[4-[4-(2-甲氧基苯基)哌嗪-1-基]丁基]-9,9-二甲基-3,7-二氮杂双环[3.3.1]壬烷-2,4,6,8-四酮Chemical Name: 3-Butyl-7-[4-[4-(2-methoxyphenyl)-1-piperazinyl]butyl]-9,9-dimethyl-3,7-diazabicyclo[3.3.1]nonan-2,4,6,8-tetraone; ...
参考文献标题:Novel tetraoxo cpds
文献作者:Sch鰊,U.; Kehrbach,W.; Benson,W.; Fuchs,A.; Ruhland,M.(Kali-Chemie AG)
参考来源:AU 8661619; DE 3529872; EP 0212551; ES 8801271; ES 8801272; US 4771044

新产品编号:28985

3-丁酰-4-(2-甲基苯基氨基)-8-(2-羟基乙氧基)喹啉Chemical Name: 3-Butyryl-8-(2-hydroxyethoxy)-4-(2-methylphenylamino)quinoline
CAS No. 125500-29-0
项目整合开发状态: Biological Testing
项目研究机构: GlaxoSmithKline (Originat...
参考文献标题:Synthetic routes to quinoline derivatives: Novel syntheses of 3-butyryl-8-methoxy-4-[(2-methylphenyl)amini]quinoline and 3-butyryl-8-(2-hydroxyethoxy)-4-[(2-methylphenyl)amino]quin
文献作者:Atkins,R.J.; et al.
参考来源:Org Process Res Dev 1997,1(3),185

Altinicline maleate, SIB-1508Y, (S)-SIB-1765F(fumarate)

3-乙炔基-5-[(2S)-1-甲基-2-吡咯烷基]吡啶马来酸盐Chemical Name: (-)-3-Ethynyl-5-[1-methylpyrrolidin-2(S)-yl]pyridine maleate
CAS No. 192231-16-6, 179120-94-6 ((R)-isomer, free base), 179120-92-4 (free base), 179120...
参考文献标题:Pyridine modulators of acetylcholine receptors
文献作者:McDonald,I.A.; Whitten,J.P.; Cosford,N.D.(SIBIA Neurosciences,Inc.)
参考来源:EP 0739342; JP 1997508648; US 5594011; WO 9615123