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

Vorozole, R-76713(undefined isomer), R-83842, Rivizor

伏氯唑伏罗唑 Chemical Name: (S)-(+)-6-[4-Chloro-alpha-(1,2,4-triazol-1-yl)benzyl]-1-methyl-1H-benzotriazole
CAS No. 129731-10-8, 118949-22-7 (undefined isomer)
项目整合开发状态: Pre-Registered
项目研究机构: Jan...
参考文献标题:(1H-Arol-1-ylmethyl)substd.Benzotriazole derivatives
文献作者:Raeymaekers,A.H.M.; Freyne,E.J.E.; Van Gelder,J.L.H.; Vener,M.G.(Janssen Pharmaceutica NV)
参考来源:AU 8816537; EP 0293978; JP 1988316775

Suberoylanilide hydroxamic acid, Suberanilohydroxamic acid, SW-064652, SAHA

伏立诺他Chemical Name: N-Hydroxy-N'-phenyloctanediamide; 8-(Phenylamino)-8-oxooctanohydroxamic acid
CAS No. 149647-78-9
项目整合开发状态: Phase II/III
项目研究机构: Aton Pharma (Orphan Drug), Columbia Universi...
参考文献标题:Novel potent inducers of terminal differentiation and methods of use thereof
文献作者:Breslow,R.; Rifkind,R.A.; Jursic,B.(Columbia University; Sloan-Kettering Institute)
参考来源:WO 9307148

Valspodar, SDZ-PSC-833, PSC-833, Amdray

伐司扑达Chemical Name: 6-[(2S,4R,6E)-4-Methyl-2-(methylamino)-3-oxo-6-octenoic acid]-7-L-valine-cyclosporin A; Cyclo[[(2S,4R,6E)-4-methyl-2-(methylamino)-3-oxo-6-octenoyl]-L-valyl-N-methylglycyl-N-methyl-...
参考文献标题:Cyclosporins and their use as pharmaceuticals
文献作者:Bollinger,P.; B鰈sterli,J.J.; Borel,J.-F.; Krieger,M.; Payne,T.G.; Traber,R.P.; Wenger,R.(Novartis AG)
参考来源:AU 8817679; EP 0296122; JP 1989045396; JP 1996048696; US 5525590

Vadocaine hydrochloride, K-242-HCl, ORK-242-HCl

伐多卡因Chemical Name: 2',4'-Dimethyl-6'-methoxy-3-(2-methylpiperidino)propionanilide hydrochloride; 3-(2-Methylpiperidino)-N-(2,4-dimethyl-6-methoxyphenyl)propionamide hydrochloride
CAS No. 72005-58-4...
参考文献标题:Novel anilides,their process of preparation and t
文献作者:Kaila,J.O.W.; Honkanen,E.J.; Alberty,J.E.; Hukki,J.J.(Orion Corporation)
参考来源:BE 0873957; US 4353914

Valaciclovir, Valacyclovir, ValACV, BW-256U, 256U87, Virval, Zelitrex, Valtrex(HCl)

伐昔洛韦盐酸伐昔洛韦 Chemical Name: L-Valine 2-(guanin-9-ylmethoxy)ethyl ester
CAS No. 124832-26-4, 124832-27-5 (monoHCl)
项目整合开发状态: Launched-1995
项目研究机构: GlaxoSmithKline (Originator), Aventis Pharma (...
参考文献标题:Therapeutic nucleosides
文献作者:Krenitsky,T.A.; Beauchamp,L.M.(GlaxoSmithKline plc)
参考来源:AU 8820978; EP 0308065; EP 0596542; JP 1989068373; JP 1991115284; US 4957924; US 5061708

Vanoxerine hydrochloride, I-893, GBR-12909

伐诺司林Chemical Name: 1-[2-[Bis(4-fluorophenyl)methoxy]ethyl]-4-(3-phenylpropyl)piperazine dihydrochloride
CAS No. 67469-69-6 (free base)
项目整合开发状态: Phase I
项目研究机构: Yamanouchi (Originator), Natio...
参考文献标题:Piperazine derivs.,process for their preparation and their use
文献作者:Gootjes,J.(Gist-Brocades NV)
参考来源:DE 2755752; US 4202896

Fentiapril, Rentiapril, DE-040, SA-446

伦唑普利Chemical Name: (2R,4R)-2-(2-Hydroxyphenyl)-3-(3-mercaptopropanoyl)-4-thiazolidinecarboxylic acid; (2R,4R)-2-(Hydroxyphenyl)-3-(3-mercapto-1-oxopropyl)-4-thiazolidinecarboxylic acid
CAS No. 8083...
参考文献标题:SA-446
文献作者:Sneddon,J.M.; Castar,J.; Blancafort,P.; Serradell,M.N.
参考来源:Drugs Fut 1983,8(1),36

Renzapride hydrochloride, ATL-1251, AZM-112, BRL-24924

伦扎必利 4-氨基-N-[(1S,4R,5S)-1-氮杂双环[3.3.1]壬烷-4-基]-5-氯-2-甲氧基-苯甲酰胺 Chemical Name: (?-endo-4-Amino-5-chloro-2-methoxy-N-(1-azabicyclo[3.3.1]non-4-yl)benzamide hydrochloride
CAS No. 112727-80-7 (free base),...
参考文献标题:Azabicyclo compounds,useful as intermediates
文献作者:King,F.D.(SmithKline Beecham plc)
参考来源:EP 0094742; JP 5194513; JP 58188885; US 4857647

LY-267108

伪红霉素 A 烯醇醚Chemical Name: 3(S)-(2,6-Dideoxy-3-C,3-O-dimethyl-alpha-L-altropyranosyloxy)-11(R)-[1(R),2(R)-dihydroxy-1-methylbutyl]-6(R),9-epoxy-2(R),4(S),6,8,10(R)-pentamethyl-5(R)-[3,4,6-trideoxy-3-(di...
参考文献标题:Synthesis of ring-contracted derivatives of erythromycin
文献作者:Kirst,H.A.; Wind,J.A.; Paschal,J.W.
参考来源:J Org Chem 1987,52(19),4359-62

SKI-606

伯舒替尼Chemical Name: 4-(2,4-Dichloro-5-methoxyphenylamino)-6-methoxy-7-[3-(4-methylpiperazin-1-yl)propoxy]quinoline-3-carbonitrile
CAS No. 380843-75-4
项目整合开发状态: Preclinical
项目研究机构: Wyeth Pharma...
参考文献标题:Substituted 3-cyano quinolines
文献作者:Tsou,H.-R.; Wissner,A.; Johnson,B.D.; Reich,M.F.; Floyd,M.B.Jr.; Kitchen,D.B.(American Cyanamid Co.)
参考来源:US 6002008