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

Pergolide mesylate, LY-141-B(free base), LY-127809, Pharken, Nopar, Parkotil, Celance, Permax

甲磺酸培高利特培高利特 Chemical Name: 8beta-[(Methylthio)methyl]-6-propylergoline monomethanesulfonate; 9beta-(Methylthiomethyl)-7-propyl-4,6,6abeta,7,8,9,10,10aalpha-octahydroindolo[4,3-fg]quinoline methanesul...
参考文献标题:6-N-Propyl-8-methoxymethyl or methylmercaptomethylergolines and related compounds
文献作者:Kornfeld,E.C.; Bach,N.J.(Eli Lilly and Company)
参考来源:AT 371817B; DD 141928; EP 0003667; FR 2416891; GB 2014140; US 4166182

Dolasetron mesilate, MDL-73147EF, Anzemet, Anemet

甲磺酸多拉司琼Chemical Name: 1H-Indole-3-carboxylic acid trans-2,6-methanooctahydro-3-oxo-2H-quinolizin-8-yl ester monomethanesulfonate monohydrate; 1H-Indole-3-carboxylic acid (2alpha,6alpha,8alpha,9abeta)-...
参考文献标题:Esters of hexahydro-8-hydroxy-2,6-methano-2H-quinolizin-3(4H)-one and related compds.
文献作者:Gittos,M.W.(Merrell Pharmaceuticals,Inc.)
参考来源:AU 8780596; EP 0266730; JP 1988258476

Nelfinavir mesilate, LY-312857, AG-1346(free base), AG-1343, Viracept

甲磺酸奈非那韦奈非那韦 Chemical Name: N-tert-Butyl-2-[2(R)-Hydroxy-3(R)-[(3-hydroxy-2-methylbenzoyl)amino]-4-(phenylsulfanyl)butyl]decahydro-(4aS,8aS)-isoquinoline-3(S)-carboxamide monomethanesulfonate
CAS ...
参考文献标题:HIV protease inhibitors
文献作者:Dressman,B.A.; Fritz,J.E.; Hammond,M.; Hornback,W.J.; Kaldor,S.W.; Kalish,V.J.; Munroe,J.E.; Reich,S.H.; Tatlock,J.H.; Shepherd,T.A.; Rodriguez,M.J.(Agouron Pharmaceuticals,Inc.)
参考来源:EP 0889036; JP 1997501443; JP 1999310573; US 5484926; WO 9509843

Patamostat mesylate, E-3123

甲磺酸帕莫司他4-(2-琥珀酰亚胺基乙硫基)苯基4-胍基苯甲酸酯Chemical Name: 4-(2-Succinimidoethylthio)phenyl 4-guanidinobenzoate methanesulfonate
CAS No. 114568-32-0, 114568-45-5 (carbonate ester (1:1)), 114568-26-2 (free base...
参考文献标题:Guanidinobenzoic ester deriv.,a process for preparing same and pharmaceutical compsns.containing same
文献作者:Hishinuma,I.; Kawashima,H.; Kawata,T.; Miyamoto,K.; Miyazawa,S.; Nagakawa,J.; Nagaoka,J.; Nagaoka,N.; Shimomura,N.; Souda,S.; Ueda,N.; Wakabayashi,T.; Yamanaka,T.(Eisai Co.,Ltd.)
参考来源:EP 0229370; JP 1987155253; JP 1994298730; US 4801603; US 5075335

Bitolterol mesylate, WIN-32784, S-1540, Asmalene, Produrol, Tornalate

甲磺酸比托特罗比托特罗 Chemical Name: 4-Methylbenzoic acid 4-[2-[(1,1-dimethylethyl)amino]-1-hydroxyethyl]-1,2-phenylene ester methanesulfonate (salt)
CAS No. 30392-41-7, 30392-40-6 (free base)
项目整合开发状态: ...
参考文献标题:Bitolterol
文献作者:Castar,J.; Weetman,D.F.
参考来源:Drugs Fut 1976,1(10),454

Saquinavir mesilate, Ro-31-8959/003, Fortovase, Fortovase(soft gel capsules), Invirase

甲磺酸沙奎那韦沙奎那韦 Chemical Name: N-tert-Butyl-2-[2(R)-hydroxy-4-phenyl-3(S)-[N-(2-quinolylcarbonyl)-L-asparaginylamino]butyl]decahydro-(4aS,8aS)-isoquinoline-3(S)-carboxamide methanesulfonate; N1-[1(S)-Ben...
参考文献标题:Ro-31-8959/003
文献作者:Martin,J.A.
参考来源:Drugs Fut 1991,16(3),210

Reboxetine mesilate, PNU-155950E, FCE-20124, Vestra, Norebox, Edronax

甲磺酸瑞波西汀瑞波西汀瑞波西汀Chemical Name: (?-(R*,R*)-[2-[alpha-(2-Ethoxyphenoxy)benzyl]morpholine methanesulfonate
CAS No. 98769-84-7, 98769-81-4 (free base), 71620-89-8 (undefined stereoch., free base)
项...
参考文献标题:Substituted morpholine derivatives and compositions
文献作者:Torre,A.D.; Carniel,G.; Rossi,A.; Melloni,P.(Pharmacia Corp.)
参考来源:DE 2901032; FR 2430412; FR 2442839; GB 2014981; JP 54148739; US 4229449

Bifeprunox mesilate, DU-127090

甲磺酸联苯芦诺7-(4-(联苯-3-甲基)哌嗪-1-基)苯并[d]噁唑-2(3h)-酮Chemical Name: 7-[4-(Biphenyl-3-ylmethyl)piperazin-1-yl]benzoxazol-2(3H)-one methanesulfonate
CAS No. 350992-13-1, 362524-71-8, 350992-10-8 (free base), 1...
参考文献标题:Piperazine and piperidine cpds.
文献作者:Feenstra,R.W.; Kruse,C.G.; Tulp,M.T.M.; Kuipers,W.; Long,S.K.(Duphar International Research BV)
参考来源:JP 2000507949; US 6225312; WO 9736893

Nafamostat mesilate, Nafamostat mesylate, FUT-175, Futhan

甲磺酸萘莫司他萘莫司他Chemical Name: 6-Amidino-2-naphthyl p-guanidinobenzoate dimethanesulfonate; 6-Amidino-2-naphthyl 4-guanidinobenzoate dimethanesulfonate
CAS No. 82956-11-4, 80251-32-7 (diHCl), 81525-10-2...
参考文献标题:Amidine compound
文献作者:Fujii,S.; Okutome,T.; Nakayama,T.; Yaegashi,T.; Kurumi,M.(Torii Pharmaceutical Co.,Ltd.)
参考来源:JP 82179146; JP 8253454; US 4454338

Phentolamine mesilate, Z-Max, Vasofem, Vasomax, Regitin

甲磺酸酚妥拉明酚妥拉明 Chemical Name: 3-[N-(2-Imidazolin-2-ylmethyl)-N-(4-methylphenyl)amino]phenol methanesulfonate
CAS No. 65-28-1, 50-60-2 (free base)
项目整合开发状态: Launched-1950
项目研究机构: Novartis (Origi...
参考文献标题:2-(N,N-Diphenyl-aminomethyl)imidazoles
文献作者:Miescher,K.; Marxer,A.; Urech,E.(Novartis Corp.)
参考来源:US 2503059