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

Trebenzomine, CI-686(hydrochloride)

曲苯佐明Chemical Name: 3,4-Dihydro-N,N,2-trimethyl-1-benzopyran-3-amine
CAS No. 23915-73-3
项目整合开发状态: Not Determined
项目研究机构:
合成路线:The reduction of 2-methyl-3-nitro-2H-1-benzopyran (I) with LiA...
参考文献标题:
文献作者:Lockhart,J.M.
参考来源:DE 1919560; FR 2007481; GB 1151474; ZA 6902723

Trimoprostil, Ro-216937, Ro-216937/000, Ulstar

曲莫前列素Chemical Name: (5Z,11alpha,13E,15R)-15-Hydroxy-11,16,16-trimethyl-9-oxoprosta-5,13-dien-1-oic acid
CAS No. 69900-72-7
项目整合开发状态: Phase III
项目研究机构: Alcon (Originator), Roche (Originator) 参考文献标题:RO-21-6937/000
文献作者:Hillier,K.; Blancafort,P.; Serradell,M.N.; Castar,J.
参考来源:Drugs Fut 1981,6(1),42

Trabectedin, Ecteinascidin 743, NSC-684766, ET-743, Yondelis

曲贝替定Chemical Name: (1'R,6R,6aR,7R,13S,14S,16R)-5-Acetoxy-6',8,14-trihydroxy-7',9-dimethoxy-4,10,23-trimethyl-1',2',3',4',6a,7,12,13,14,16-decahydro-6H-spiro[6,16-(epithiopropanoxymethano)-7,13-imino-1...
参考文献标题:A new,more efficient,and effective process for the synthesis of a key pentacyclic intermediate for production of ecteinascidin and phthalascidin antitumor agents
文献作者:Martinez,E.J.; Corey,E.J.
参考来源:Org Lett 2000,2(7),993

Ganciclovir, DHPG, RS-21592, BW-795, 2'-NDG, BIOLF-62, BW-759U, Cymeven, Cymevan, Citovirax, Vitrasert, Cymevene, Cytovene, Virgan

更昔洛韦更昔洛韦钠 Chemical Name: 2-Amino-1,9-dihydro-9-[2-hydroxy-1-(hydroxymethyl)ethoxymethyl]-6H-purin-6-one; 9-[2-Hydroxy-1-(hydroxymethyl)ethoxymethyl]guanine
CAS No. 82410-32-0, 107910-75-8 (Na salt...
参考文献标题:Purine and pyrimidine compounds and their use as anti-viral agents
文献作者:Ogilvie,K.K.(Bio Logicals Inc.)
参考来源:EP 0049072; EP 0243670; JP 57085373; US 4347360

Telenzepine hydrochloride, SK-871, B-818-04(hemifumarate), B-803-32(free base), B-818-03

替仑西平Chemical Name: 3-Methyl-4-[2-(4-methylpiperazin-1-yl)acetyl]-9,10-dihydro-4H-thieno[3,4-b][1,5]benzodiazepin-10-one dihydrochloride
CAS No. 80880-90-6 (free base)
项目整合开发状态: Phase III
项目研究...
参考文献标题:Process for the preparation of 2-bromo-8-ergolinyl
文献作者:Bner,H.; Haffer,G.; Sauer,G.(Schering AG)
参考来源:DE 3340025; US 4970314

Tilisolol hydrochloride, N-696, Daim, Selecal

替利洛尔盐酸替利洛尔 Chemical Name: (?-4-[3-(tert-Butylamino)-2-hydroxypropoxy]-N-methylisocarbostyril monohydrochloride; (?-4-[3-(tert-Butylamino)-2-hydroxypropoxy]-2-methylisoquinolin-1(2H)-one monohydrochlo...
参考文献标题:Isocarbostyril derivatives
文献作者:Fukushima,H.; Suzuki,Y.(Nisshin Flour Milling Co.,Ltd.)
参考来源:DE 2631080; GB 1501149; JP 52012178

Telinavir, SC-52151

替利那韦Chemical Name: N-(Quinolin-2-ylcarbonyl)-asparagine 1(S)-benzyl-3-(3-tert-butyl-1-isobutylureido)-2(R)-hydroxypropylamide
CAS No. 143224-34-4
项目整合开发状态: Phase III
项目研究机构: Pfizer (Originato...
参考文献标题:Retroviral protease inhibitors
文献作者:Clare,M.; DeCrescenzo,G.A.; Freskos,J.N.; Getman,D.P.; Heintz,R.M.; Lin,K.-C.; Mueller,R.A.; Reed,K.L.; Talley,J.J.; Vazquez,M.L.; Sun,E.T.O.(Pharmacia Corp.)
参考来源:EP 0558630; WO 9208701

Tigilcycline, Tigecycline, WAY-GAR-936, GAR-936, TBG-MINO, Tygacil

替加环素Chemical Name: (4S,4aS,5aR,12aS)-9-(N-tert-Butyl-glycylamino)-4,7-bis(dimethylamino)-3,10,12,12a-tetrahydroxy-1,11-dioxo-1,4,4a,5,5a,6,11,12-octahydronaphthacene-2-carboxamide; 9-(N-tert-Butylglyc...
参考文献标题:Method of producing 7-(substd.)-9-[(substd.glycyl)amidol]-6-demethyl-6-deoxytetracyclines
文献作者:Sum,P.-E.; Lee,V.J.(American Cyanamid Co.)
参考来源:EP 0582790; US 5284963

Tibolone, KB-889, Org-OD14, Xyvion, Boltin, Livial

替勃龙Chemical Name: 7alpha-Methyl-17alpha-ethynyl-17beta-hydroxy-19-norandrost-5(10)-en-3-one
CAS No. 5630-53-5
项目整合开发状态: Launched-1988
项目研究机构: Organon (Originator), Kanebo (Licensee)
合成路线:B...
参考文献标题:Tibolone
文献作者:Castar,J.; Serradell,M.N.; Blancafort,P.; Hillier,K.
参考来源:Drugs Fut 1981,6(5),302

DJ-927

替司他赛Chemical Name: Benzoic acid (2aS,2bR,3S,4S,6S,8aR,10S,11aS,11bR,13aR)-2a-acetoxy-6-[3(S)-(tert-butoxycarboxamido)-3-(3-fluoropyridin-2-yl)-2(R)-hydroxypropanoyloxy]-10-(dimethylaminomethyl)-4-hydr...
参考文献标题:Pentacyclic taxane cpds.
文献作者:Soga,T.; Takeda,Y.; Uoto,K.(Daiichi Pharmaceutical Co.,Ltd.)
参考来源:EP 1221445; WO 0127115