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

Exemestane, FCE-24304, Aromasin, Nikidess

依西美坦Chemical Name: 6-Methyleneandrosta-1,4-dien-3,17-dione
CAS No. 107868-30-4
项目整合开发状态: Launched-1999
项目研究机构: Pfizer (Originator), National Cancer Institute of Canada (Not Determined)
合成路...
参考文献标题:Process for the preparation of methylene derivatives of androsta-1,4-diene-3,17-dione
文献作者:Longo,A.; Lombardi,P.(Pharmacia Corp.)
参考来源:US 4876045

Fenoximone, Enoximone, MDL-17043, RMI-17043, Perfan, Perfane

依诺昔酮Chemical Name: 4-Methyl-5-[p-(methylthio)benzoyl]-4-imidazolin-2-one; 1,3-Dihydro-4-methyl-5-[4-(methylthio)benzoyl]-2H-imidazol-2-one
CAS No. 77671-31-9
项目整合开发状态: Launched-1988
项目研究机构: A...
参考文献标题:4-Aroylimidazol-2-ones
文献作者:Dage,R.C.; Schnettler,R.A.; Grisar,J.M.(Aventis Pharmaceuticals,Inc.)
参考来源:BE 0883856; DE 3021792; FR 2459233; GB 2055364; JP 56005463

Enoxacin, PD-107779, CI-919, AT-2266, Almitil, Enoxor, Penetrex, Comprecin, Flumark

依诺沙星Chemical Name: 1-Ethyl-6-fluoro-1,4-dihydro-4-oxo-7-(1-piperazinyl)-1,8-naphthyridine-3-carboxylic acid
CAS No. 74011-58-8
项目整合开发状态: Launched-1986
项目研究机构: Dainippon Pharmaceutical (Origin...
参考文献标题:Novel naphthyridine derivatives,intermediates thereof,processes for preparation thereof and use thereof
文献作者:Matsumoto,J.; et al.(Aventis Pharma SA; Dainippon Pharmaceutical Co.,Ltd.)
参考来源:EP 0009425; ES 483629; US 4359578

Edaravone, MCI-186, Radicut

依达拉奉Chemical Name: 3-Methyl-1-phenyl-2-pyrazolin-5-one
CAS No. 89-25-8, 94489-23-3 (NH3 salt)
项目整合开发状态: Launched-2001
项目研究机构: Mitsubishi Pharma (Originator)
合成路线:By direct cyclization of p...
参考文献标题:Prophylactic and therapeutic agent for circulatory disorders
文献作者:Nishi,H.; Watanabe,T.; Yuki,S.; Morinaka,Y.; Iseki,K.; Sakurai,H.(Mitsubishi Chemical Corp.)
参考来源:EP 0208874; JP 1987108814; US 4857542

Edatrexate, CGP-30694, 10-EDAM

依达曲沙Chemical Name: 10-Ethyl-10-deazaaminopterin; N-[4-[1-(2,4-Diamino-6-pteridinylmethyl)propyl]benzoyl]-L-glutamic acid
CAS No. 80576-83-6
项目整合开发状态: Phase III
项目研究机构: SRI (Originator)
合成路...
参考文献标题:EDATREXATE
文献作者:DeGraw,J.I.
参考来源:Drugs Fut 1989,14(9),849

Enalaprilat, MK-422, Renitec, Vasotec I.V.

依那普利那二水依那普利拉 Chemical Name: 1-[N-[(S)-1-Carboxy-3-phenylpropyl]-L-alanyl]-L-proline dihydrate
CAS No. 84680-54-6, 76420-72-9 (anhydrous)
项目整合开发状态: Launched-1987
项目研究机构: Merck & Co. (Originat...
参考文献标题:Carboxyalkyl dipeptide derivs.,process for preparing them and pharmaceutical compsn.containing them
文献作者:Wyvratt,M.J.; Harris,E.E.; Patchett,A.A.; Tristram,E.W.(Merck & Co.,Inc.)
参考来源:EP 0012401

Eptaplatin, Heptaplatin, NSC-644591, NSC-D-644591, SKI-2053R, Sunpla

依铂(SKI-2053R)Chemical Name: cis-[(4R,5R)-2-Isopropyl-1,3-dioxolane-4,5-bis(methylamine)-N,N'][malonato(2-)-O,O']platinum; (SP-4-2)-[(4R,5R)-2-Isopropyl-1,3-dioxolane-4,5-bis(methanamine)-N,N'][propane...
参考文献标题:Synthesis and antitumor activity of a series of [2-substituted-4,5-bis(aminomethyl)-1,3-dioxolane]platinum(II) complexes
文献作者:Kim,D.-K.; Kim,G.; Gam,J.; Cho,Y.-B.; Kim,H.-T.; Tai,J.-H.; Kim,K.H.; Hong,W.-S.; Park,J.-G.
参考来源:J Med Chem 1994,37(10),1471-85

Emapunil, SX-5216, AC-5216

依马普尼Chemical Name: N-Benzyl-N-ethyl-2-(7-methyl-8-oxo-2-phenyl-7,8-dihydro-9H-purin-9-yl)acetamide
CAS No. 226954-04-7
项目整合开发状态: Phase I
项目研究机构: Dainippon Pharmaceutical (Originator), Novarti...
参考文献标题:2-Aryl-8-oxodihydropurine derivs.,process for producing the same,medicinal compsns.containing the same,and intermediates thereof
文献作者:Matsumoto,K.; Kondo,K.; Furukawa,K.; Murata,T.; Oka,M.(Dainippon Pharmaceutical Co.,Ltd.)
参考来源:EP 1036794; WO 9928320

Elgodipine hydrochloride, IQB-875

依高地平Chemical Name: (?-2,6-Dimethyl-4-(2,3-methylenedioxyphenyl)-1,4-dihydropyridine-3,5-dicarboxylic acid 3-isopropyl 5-[2-[N-(4-fluorobenzyl)-N-methylamino]ethyl] diester monohydrochloride
CAS No....
参考文献标题:1,4-Dihydropyridines,process for their preparation and their use as medicaments
文献作者:Fern醤dez Torija,C.; Galiano Ramos,J.A.(IIDQB (Madrid))
参考来源:AU 8820330; BE 1001055; CH 675999; EP 0302980; GB 2208861; JP 1989294675; US 4952592

Elziverine, Ro-224839

依齐维林Chemical Name: 1-(3,4-Dimethoxybenzyl)-6,7-dimethoxy-4-[4-(2-methoxyphenyl)piperazin-1-ylmethyl]isoquinoline
CAS No. 95520-81-3
项目整合开发状态: Phase II
项目研究机构: Roche (Originator)
合成路线:The c...
参考文献标题:Substd.isoquinolines
文献作者:Bruderer,H.; Kierstead,R.W.; Mullin,J.G.Jr.; Nakamura,K.; O'Brien,J.P.; Sidney,T.; Tateishi,M.(F.Hoffmann-La Roche AG)
参考来源:EP 0126480; ES 8601141; JP 1984222478; US 4544657