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

Ranimustine, MCNU, NSC-270516, Cymerine

雷莫司汀Chemical Name: Methyl 6-[[[(2-chloroethyl)nitrosoamino]carbonyl]amino]-6-deoxy-alpha-D-glucopyranoside
CAS No. 58994-96-0
项目整合开发状态: Launched-1987
项目研究机构: Mitsubishi Pharma (Originator) 参考文献标题:Alkyl amino-glucopyranoside derivative and process for producing the same
文献作者:Kimura,G.; Sekine,J.(Tokyo Tanabe Co.,Ltd.)
参考来源:CA 1044228; CH 610334; DE 2530416; FR 2276828; GB 1499760; JP 7606925; JP 77125126; JP 7797915; NL 7507973

Resiquimod, VML-600, R-848, S-28463

雷西莫特Chemical Name: 1-[4-Amino-2-(ethoxymethyl)-1H-imidazo[4,5-c]quinolin-1-yl]-2-methylpropan-2-ol; 4-Amino-2-(ethoxymethyl)-alpha,alpha-dimethyl-1H-imidazo[4,5-c]quinoline-1-ethanol
CAS No. 144875...
参考文献标题:1-Substd.,2-substd.1H-imidazo[4,5-c]quinolin-4-amines
文献作者:Gerster,J.F.; Crooks,S.L.; Lindstrom,K.J.(3M Pharmaceuticals)
参考来源:EP 0582581; JP 1994504789; US 5389640; WO 9215582

Ranolazine, CVT-303, KEG-1295, RS-43285(diHCl), Ranexa

雷诺嗪 N-(2,6-二甲基苯基)-2-(4-(2-羟基-3-(2-甲氧基苯氧基)-丙基)哌嗪-1-基)乙酰胺二盐酸盐 Chemical Name: 1-[3-(2-Methoxyphenoxy)-2-hydroxypropyl]-4-[(2,6-dimethylphenyl)aminocarbonylmethyl]piperazine; N-(2,6-Dimethylphenyl)-4-[2-...
参考文献标题:Ethanamine derivs.,their preparation and use in pharmaceutical compsns
文献作者:Ainsworth,A.T.; Smith,D.G.(SmithKline Beecham plc)
参考来源:EP 0023385

Pariprazole sodium, Rabeprazole sodium, LY-307640, E-3810, Aciphex, Pariet

雷贝拉唑钠雷贝拉唑 Chemical Name: 2-[4-(3-Methoxypropoxy)-3-methylpyridin-2-ylmethylsulfinyl]benzimidazole 1-sodium salt
CAS No. 117976-90-6, 117976-89-3 (free acid)
项目整合开发状态: Launched-1997
项目研究机构: E...
参考文献标题:Pyridine derivs.,pharmaceutical compsns.comprising the same,the use of the same for the manufacture of medicaments having therapeutic or preventative value,and a process for preparing the same
文献作者:Souda,S.; Ueda,N.; Miyazawa,S.; Tagami,K.; Nomoto,S.; Okita,M.; Shimomura,N.; Kaneko,T.; Fujimoto,M.; Murakami,M.; Oketani,K.; Fujisaki,H.; Shibata,H.; Wakabayashi,T.(Eisai Co.,Ltd.)
参考来源:AU 8781138; EP 0268956; EP 0475456; EP 0654471; EP 0786461; JP 1989006270; JP 1993247035; JP 1995291967; US 5045552; US 5998445

Ramatroban, Bay-u-3405, Baynas

雷马曲班Chemical Name: (+)-3-[3(R)-(4-Fluorophenylsulfonamido)-1,2,3,4-tetrahydrocarbazol-9-yl]propionic acid
CAS No. 116649-85-5
项目整合开发状态: Launched-2000
项目研究机构: Bayer (Originator), Kyorin (Licen...
参考文献标题:Bay u 3405
文献作者:Gardiner,P.J.; Boberg,M.; Fiedler,V.B.; Perzborn,E.; Bhagen,H.; B黨ner,K.; M鷏ler,U.; Rosentreter,U.; Seuter,F.; Weber,H.; Norman,P.; Ritter,W.
参考来源:Drugs Fut 1991,16(8),701

Mycophenolic acid, NSC-129185, Melbex

霉酚酸Chemical Name: 6-(4-Hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-5-isobenzofuranyl)-4-methyl-4(E)-hexenoic acid
CAS No. 24280-93-1
项目整合开发状态: Not Determined
项目研究机构:
合成路线:The cyclization...
参考文献标题:Total synthesis of mycophenolic acid
文献作者:Covarrubias-Ziga,A.; Gonz醠ez-Lucas,A.; Dom韓guez,M.M.
参考来源:Tetrahedron 2003,59(11),1989

Artemisine, Artemisinin, Qinghaosu, Artesin, Cotexin

青蒿素Chemical Name: (3R,5aS,6R,8aS,9R,12S,12aR)-Octahydro-3,6,9-trimethyl-3,12-epoxy-12H-pyrano[4,3-j]-1,2-benzodioxepin-10(3H)-one
CAS No. 63968-64-9
项目整合开发状态: Launched-1986
项目研究机构: Walter Ree...
参考文献标题:New synthetic strategies towards (+)-artemisinin
文献作者:Deshpande,V.H.; Bhonsle,J.B.; Pandey,B.; Ravindranathan,T.
参考来源:Tetrahedron Lett 1994,35(30),5489

Indirubin

靛玉红Chemical Name: 3-(1,3-Dihydro-3-oxo-2H-indol-2-ylidene)-1,3-dihydro-2H-indol-2-one
CAS No. 479-41-4
项目整合开发状态: Clinical
项目研究机构: Chinese Academy of Sciences (Originator), Institute of Materi...
参考文献标题:Indirubin
文献作者:Ru-yun,J.
参考来源:Drugs Fut 1984,9(4),266

Fidexaban, ZK-807834, BX-807834, ZK-807191(diHCl), PD-200022, CI-1031

非地沙班Chemical Name: N-[2-(5-Amidino-2-hydroxyphenoxy)-3,5-difluoro-6-[3-(1-methyl-4,5-dihydroimidazol-2-yl)phenoxy]pyridin-4-yl]-N-methylglycine
CAS No. 183305-24-0, 213839-64-6 (diHCl), 183304-36-1...
参考文献标题:Benzamidine derivs.their preparation and their use as anti-coagulants
文献作者:Buckman,B.O.; Davey,D.D.; Guilford,W.J.; Morrissey,M.M.; Ng,H.P.; Phillips,G.B.; Wu,S.C.; Xu,W.(Berlex Laboratories,Inc.)
参考来源:EP 0813525; US 5691364; WO 9628427

Febuprol, K-10033, Valbil

非布丙醇Chemical Name: 1-Butoxy-3-phenoxy-2-propanol; (3-n-Butoxy-2-hydroxypropyl)phenyl ether
CAS No. 3102-00-9
项目整合开发状态: Launched-1983
项目研究机构: Fujisawa Deutschland (Originator)
合成路线:1) By co...
参考文献标题:Febuprol
文献作者:Janiak,P.St.
参考来源:Drugs Fut 1978,3(3),191