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

LY-255262

Chemical Name: 7(S)-[2-(2-Aminothiazol-4-yl)-2(Z)-(methoxyimino)acetamido]-3-cyano-8-oxo-1,5-diazabicyclo[3.3.0]oct-2-ene-2-carboxylic acid
CAS No. 122620-16-0
项目整合开发状态: Biological Testing
项目...
参考文献标题:Substd.diazolidinones
文献作者:Jungheim,L.N.; Holmes,R.E.(Eli Lilly and Company)
参考来源:US 4826993

SH-D515, ZK-91587

Chemical Name: 7alpha-Methoxycarbonyl-15beta,16beta-methylene-3-oxo-17alpha-pregn-4-ene-21,17-carbolactone; 15beta,16beta-Methylenemexrenone
CAS No. 84542-26-7
项目整合开发状态: Phase II
项目研究机构: Sche...
参考文献标题:Aldosterone antagonists.3.Synthesis and activities of steroidal 7alpha -(alkoxycarbonyl)-15,16-methylene spirolactones
文献作者:Nishino,Y.; Wiechert,R.; Laurent,H.; Bittler,D.; Losert,W.; Nickisch,K.; Schillinger,E.
参考来源:J Med Chem 1990,33(2),509-13

FPL-62129XX

Chemical Name: 3-Methyl 5-isopropyl 4-[3-chloro-6-fluoro-2-(trifluoromethyl)phenyl]-2-(fluoromethyl)-6-methyl-1,4-dihydropyridine-3,5-dicarboxylate
CAS No. 95445-79-7
项目整合开发状态: Phase II
项目研究机...
参考文献标题:Pharmaceutically active dihydropyridines
文献作者:Baxter,A.J.G.; Dixon,J.; Gould,K.J.; McInally,T.; Tinker,A.C.(Celltech Group plc)
参考来源:EP 0125803

E-5110

Chemical Name: 3-[3,5-Di(tert-butyl)-4-hydroxybenzylidene]-1-methoxypyrrolidin-2-one; N-Methoxy-3-[3,5-di(tert-butyl)-4-hydroxybenzylidene]-2-pyrrolidone
CAS No. 107746-52-1
项目整合开发状态: Phase II 参考文献标题:2-Pyrrolidone derivatives,process for preparing them,pharmaceutical compositions and use
文献作者:Ikuta,H.; Yamagishi,Y.; Akasaka,K.; Yamatsu,I.; Kobayashi,S.; Shirota,H.; Katayamaa,K.(Eisai Co.,Ltd.)
参考来源:AU 8656766; EP 0204964; ES 8800148; JP 1986257967; US 4833160

HWA-152

Chemical Name: 3-Cyano-2,6-dimethyl-4-(4-thiomorpholinyl)pyridine N-oxide hydrochloride
CAS No. 106101-15-9, 106101-47-7 (free base)
项目整合开发状态: Clinical
项目研究机构: Cassella (Originator)
合成路线:T...
参考文献标题:Substd.pyridin-1-oxides,process for their preparation,medicines containing them and their use
文献作者:Greve,W.; Schindler,U.; Elben,U.; Rudolphi,K.(Aventis Pharma AG)
参考来源:DE 3514073

AS-2646, AD-2646

Chemical Name: 2-(4-Ethyl-1-piperazinyl)-4-phenylquinoline dimaleate
CAS No. 94788-64-4, 72320-60-6 (diHCl), 72320-59-3 (free base)
项目整合开发状态: Phase II
项目研究机构: Dainippon Pharmaceutical (Origin...
参考文献标题:2-(4-Ethyl-1-piperazinyl)-4-phenylquinoline and its salts with acids,process for their preparation and their use as antidepressant agents
文献作者:Uno,H.; Nagai,Y.; Karasawa,T.; Furukawa,K.(Dainippon Pharmaceutical Co.,Ltd.)
参考来源:DE 2912414

CPI-[(99m)-Tc], Tc-CPI, (99m)-Tc-CPI

Chemical Name: Hexakis(carbomethoxyisopropylisonitrile)technetium[(99m)Tc](1+); Hexakis(methyl 2-isocianoisobutyrate)[(99m)Tc]technetium (1+); Hexakis(methyl 2-isociano-2-methylpropanoate)[(99mTc)]tec...
参考文献标题:Carboxy,carboalkoxy and carbamile substd.isonitrile radionuclide complexes
文献作者:Jones,A.G.; Davison,A.; Kronauge,J.; Abrams,M.J.(Harvard College; Massachusetts Institute of Technology)
参考来源:EP 0213945

Clofurenadine hydrochloride, (?-BN-1267

Chemical Name: (?-3-(4-Chlorophenyl)-1,3-dihydro-3,6-dimethylfuro[3,4-c]pyridin-7-ol hydrochloride
CAS No. 91868-84-7 (free base)
项目整合开发状态: Phase I
项目研究机构: Institut Henri Beaufour (Originator...
参考文献标题:Furo[3,4-c]pyridine derivatives and therapeutic compositions containing the same
文献作者:Esanu,A.(SCRAS (Societ?de Conseils de Recherches et d'Applications Scientifiques))
参考来源:BE 0899222; CH 660191; GB 2137618; JP 1984193888; US 4581363; US 4735950

Thyrsiferyl 18-acetate, TF-18A

Chemical Name: Acetic acid 4(S)-[(2R,4aR,6R,8aS)-6-[5(R)-bromo-2(S),6,6-trimethyltetrahydro-2H-pyran-2-yl]-8a-methyloctahydropyrano[3,2-b]pyran-2-yl}-4-hydroxy-1(S)-[5(R)-(1-hydroxy-1-methylethyl)-2(R...
参考文献标题:Total synthesis of tryrsiferyl 23-acetate,a specific inhibitor of protein phosphatase 2A and anti-leukemic inducer of apoptosis
文献作者:Forsyth,G.J.; Gonz醠ez,I.C.
参考来源:J Am Chem Soc 2000,122(38),9099

AA-193

Chemical Name: 5-Chloro-3-phenyl-7,8-dihydrofuro[2,3-g]-1,2-benzisoxazole-7-carboxylic acid
CAS No. 107804-48-8
项目整合开发状态: Phase II
项目研究机构: Chugai (Originator)
合成路线:1) The Friedel-Crafts co...
参考文献标题:Furobenzisoxazole derivs
文献作者:Sato,H.; Koga,H.; Dan,T.; Onuma,E.(Chugai Pharmaceutical Co.Ltd.)
参考来源:EP 0205872; US 4791209