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

S-5751

治疗哮喘药物S-5751中间体Chemical Name: (1R,2R,3S,5S)-7-[2-(5-Hydroxybenzothiophen-3-ylcarboxamido)-6,6-dimethylbicyclo[3.1.1]hept-3-yl]-5(Z)-heptenoic acid
CAS No. 209268-36-0, 209268-44-0 (E-isomer), 20927...
参考文献标题:Benzothiophenecarboxamide derivs.and PGD2 antagonists comprising them
文献作者:Arimura,A.; Honma,T.; Hiramatsu,Y.(Shionogi & Co.Ltd.)
参考来源:EP 0944614; JP 2000514824; US 6083974; WO 9825919

Posatirelin, pAad-Leu-Pro-NH2, RGH-2202, Pyladox

泊替瑞林Chemical Name: N-[6-Oxopiperidin-2(S)-ylcarbonyl]-L-leucyl-L-prolinamide
CAS No. 78664-73-0
项目整合开发状态: Discontinued
项目研究机构: Gedeon Richter (Originator), Dainippon Pharmaceutical (Licensee)...
参考文献标题:RGH-2202
文献作者:N骻r醖i,M.
参考来源:Drugs Fut 1988,13(5),420

Posaconazole, SCH-56592, Noxafil

泊沙康唑Chemical Name: (3R,5R)-4-[4-[4-[4-[5-(2,4-Difluorophenyl)-5-(1,2,4-triazol-1-ylmethyl)tetrahydrofuran-3-ylmethoxy]phenyl]piperazin-1-yl]phenyl]-2-[1(S)-ethyl-2(S)-hydroxypropyl]-3,4-dihydro-2H-1,2...
参考文献标题:Tetrahydrofuran antifungals
文献作者:Saksena,A.K.; Girijavallabhan,V.M.; Lovey,R.G.; Pike,R.E.; Wang,H.; Liu,Y.-T.; Ganguly,A.K.; Bennett,F.(Schering Corp.)
参考来源:EP 0736030; JP 1997500658; US 5661151; US 5703079; WO 9517407

Falipamil, AQ-A-39

法利帕米Chemical Name: 5,6-Dimethoxy-2-[3-[[2-(3,4-dimethoxyphenyl)ethyl]methylamino]propyl]phthalamidine; 2-[3-[[2-(3,4-Dimethoxyphenyl)ethyl]methylamino]propyl]-2,3-dihydro-5,6-dimethoxy-1H-isoindol-1-o...
参考文献标题:AQ-A-39
文献作者:Castar,J.; Koch,H.
参考来源:Drugs Fut 1981,6(7),402

T-705

法匹拉韦Chemical Name: 6-Fluoro-3-hydroxypyrazine-2-carboxamide
CAS No. 259793-96-9
项目整合开发状态: Preclinical
项目研究机构: Toyama (Originator)
合成路线:Treatment of methyl 6-bromo-3-amino-2-pyrazinecarboxy...
参考文献标题:Nitrogenous heterocyclic carboxamide derivs.or salts thereof and antiviral agents containing both
文献作者:Furuta,Y.; Egawa,H.(Toyama Chemical Co.,Ltd.)
参考来源:EP 1112743; WO 0010569

Fadolmidine hydrochloride, Radolmidine hydrochloride, MPV-2426

法多咪定盐酸盐Chemical Name: 3-(1H-Imidazol-4-ylmethyl)indan-5-ol hydrochloride
CAS No. 189353-32-0, 189353-31-9 (free base)
项目整合开发状态: Preclinical
项目研究机构: Orion Corp. (Originator)
合成路线:Reductive ...
参考文献标题:Imidazole derivs.having affinity for alpha2 receptors activity
文献作者:Karjalainen,A.; Huhtala,P.; Savola,J.-M.; Wurster,S.; Eloranta,M.; Savola,M.; Saxlund,R.; Cockcroft,V.(Orion Corporation)
参考来源:EP 0888309; JP 2000507914; WO 9712874

Fazarabine, Aza-5-C, Aza-A, NSC-281272, ara-AC

法扎拉滨Chemical Name: 4-Amino-1-beta-D-arabinofuranosyl-1,3-5-triazin-2(1H)-one; 1-beta-D-Arabinofuranosyl-5-azacytosine; Arabinosyl-5-azacytosine
CAS No. 65886-71-7
项目整合开发状态: Phase II
项目研究机构: N...
参考文献标题:Synthesis and antitumor activity of 5-azacytosine arabinoside
文献作者:Beisler,J.A.; Abbasi,M.M.; Driscoll,J.S.
参考来源:J Med Chem 1979,22(10),1230-4

Falintolol oxalate

法林洛尔Chemical Name: O-[2-Hydroxy-3-(tert-butylamino)propyl]cyclopropylmethyl ketone oxime oxalate
CAS No. 90581-63-8 (free base)
项目整合开发状态: Phase III
项目研究机构: Alcon (Originator)
合成路线:This com...
参考文献标题:Falintolol oxalate
文献作者:Castar,J.; Serradell,M.N.
参考来源:Drugs Fut 1984,9(7),510

Fasoracetam, NS-105, LAM-105

法索西坦 (5S)-5-(哌啶-1-羰基)吡咯里丁-2-1 5-(哌啶-1-羰基)吡咯烷-2-酮Chemical Name: (R)-1-[(5-Oxo-2-pyrrolidinyl)carbonyl]piperidine; (R)-5-(Piperidin-1-ylcarbonyl)pyrrolidin-2-one
CAS No. 110958-19-5, 110958-23-1 ((S)...
参考文献标题:Pyroglutamide derivs
文献作者:Kimura,K.; Chokai,S.; Tomita,T.; Kise,M.; Nakamura,K.(Nippon Shinyaku Co.,Ltd.)
参考来源:DE 3701494; FR 2597100; GB 2185483; JP 1987252761; JP 1987252762; JP 1988146857; US 5102882

Faropenem daloxate, BAY-56-6854, SUN-A0026, SUN-208

法罗培南酯Chemical Name: (5R,6S)-6-[1(R)-Hydroxyethyl]-2-[2(R)-tetrahydrofuryl]-2-penem-3-carboxylic acid 5-methyl-2-oxo-1,3-dioxol-4-ylmethyl ester
CAS No. 141702-36-5
项目整合开发状态: Phase III
项目研究机构:...
参考文献标题:Penem cpds
文献作者:Ishiguro,M.; Iwata,H.; Nakatsuka,T.(Suntory Ltd.)
参考来源:AU 8654460; EP 0199446; JP 1994128267; US 4997829