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

Rifaximin, alpha-0817185, L-105, Xifaxan, Lumenax, Flonorm, RedActiv, Rifacol, Normix

利福昔明Chemical Name: 4-Deoxy-4'-methylpyrido[1',2'-1,2]imidazo[5,4-c]rifamycin SV
CAS No. 80621-81-4
项目整合开发状态: Launched-1988
项目研究机构: Salix (Orphan Drug), Alfa Wassermann (Originator), Merckle (...
参考文献标题:L-105
文献作者:de Angelis,L.
参考来源:Drugs Fut 1982,7(4),260

AP-1903

利米多赛Chemical Name: Bis[1-[2(S)-(3,4,5-Trimethoxypheny)butyryl]piperidine-2(S)-carboxylic acid] ester with 1,2-ethanediylbis[imino(2-oxo-2,1-ethanediyl)oxy-3,1-phenylene[(1R)-3-(3,4-dimethoxyphenyl)pro...
参考文献标题:Synthetic derivs.of rapamycin as multimerizing agents for chimeric proteins with immunophilin-derived domains
文献作者:Yang,W.; Guo,T.; Keenan,T.P.; Laborde,E.; Holt,D.A.(Ariad Pharmaceuticals Inc.)
参考来源:JP 2000505475; WO 9731898

Lisofylline, CT-1501R, LSF, ProTec

利索茶碱(+/-)-1-(5-羟基己基)-3,7-二甲基黄嘌呤Chemical Name: 1-[5(R)-Hydroxyhexyl]-3,7-dimethylxanthine
CAS No. 100324-81-0, 151852-32-3 (racemate), 6493-06-7 (undefined isomer)
项目整合开发状态: Phase III
项目研究机构: ...
参考文献标题:Enantiomeric hydroxylated xanthine cpds
文献作者:Bianco,J.A.; Woodson,P.; Porubek,D.; Singer,J.(Cell Therapeutics,Inc.)
参考来源:JP 1994509584; JP 1996259565; WO 9317684

Rilmenidine dihydrogen phosphate, S-3341, Hyperium

利美尼啶Chemical Name: 2-(alpha,alpha-Dicyclopropylmethylamino)-2-oxazoline dihydrogen phosphate; 2-(alpha,alpha-Dicyclopropylmethylamino)-4,5-dihydrooxazole dihydrogen phosphate; alpha,alpha-Dicyclopropy...
参考文献标题:Cyclopropylamines as pharmaceuticals
文献作者:Malen,C.; Desnos,M.; Laubie,M.; Poignant,J.C.(Servier Laboratoires)
参考来源:DE 2362754; ES 421879; FR 2212143; GB 1453703; JP 50004084; JP 53056664; JP 53056665

Clanobutin

利胆丁酸Chemical Name: 4-[N-(4-Chlorobenzoyl)-N-(4-methoxyphenyl)amino]butyric acid
CAS No. 30544-61-7
项目整合开发状态: Biological Testing
项目研究机构:
合成路线:(4-Methoxyphenyl)-2-pyrrolidone (I) is reacted...
参考文献标题:Clanobutin
文献作者:Unterhalt,B.
参考来源:Drugs Fut 1979,4(6),411

Roquinimex, PNU-212616, FCF-89, LS-2616, Linomide

利诺安Chemical Name: 4-Hydroxy-N,1-dimethyl-2-oxo-N-phenyl-1,2-dihydro-3-quinolinecarboxamide
CAS No. 84088-42-6
项目整合开发状态: Phase III
项目研究机构: Leo (Originator), Pfizer (Originator)
合成路线:By cond...
参考文献标题:Novel morpholino derivs.of daunorubicins and doxorubicins
文献作者:Bargiotti,A.; Zini,P.; Penco,S.; Giuliani,F.(Pharmacia Corp.)
参考来源:BE 0904431; DE 3609052; GB 2172594; JP 1986221194; US 4672057

Linotroban, HN-11500, CL-871502

利诺曲班醋酸,2-[[5-[2-[(苯磺酰)氨基]乙基]-2-噻吩基]氧]- Chemical Name: 2-[5-[2-(Benzenesulfonamido)ethyl]thien-2-yloxy]acetic acid
CAS No. 120824-08-0, 141443-73-4 (HN-11500)
项目整合开发状态: Phase II
项目研究机构: Amers...
参考文献标题:Novel 2-thienyloxyacetic acid derivs.,a process for their preparation and pharmaceutical preparations containing them
文献作者:Binder,D.; Rovensky,F.; Ferber,H.P.(CL Pharma; Nycomed Pharma)
参考来源:EP 0284892; US 4877809

Lixivaptan, WAY-VPA-985, VPA-985

利赛伐坦Chemical Name: N-[3-Chloro-4-(10,11-dihydro-5H-pyrrolo[2,1-c][1,4]benzodiazepin-10-ylcarbonyl)phenyl]-5-fluoro-2-methylbenzamide
CAS No. 168079-32-1
项目整合开发状态: Phase II
项目研究机构: Wyeth Pharm...
参考文献标题:Tricyclic diazepine vasopressin antagonists and oxytocin antagonists
文献作者:Albright,J.D.; Reich,M.F.; Sum,F.-W.; Delos Santos,E.G.(American Cyanamid Co.)
参考来源:CA 2128956; EP 0636625; JP 1995157486; US 5516774

Risedronate sodium, NE-58095, Optinate Septimum, Benet, Optinate, Actonel

利赛膦酸钠利塞膦酸 Chemical Name: 2-(3-Pyridinyl)-1-hydroxyethane-1,1-biphosphonate monosodium salt; [2-(3-Pyridyl)ethylidene]hydroxydiphosphonate monosodium salt; 1-Hydroxy-2-(3-pyridyl)ethane-1,1-diphosphon...
参考文献标题:Pharmaceutical compsns.containing geminal diphosphonates
文献作者:Benedict,J.J.; Perkins,C.M.(The Procter & Gamble Co.)
参考来源:AU 8551534; EP 0186405; ES 8707543; JP 1995285976; JP 1997202794; US 5583122

Ridazolol

利达洛尔Chemical Name: (?-4-Chloro-5-[[2-[[3-(o-chlorophenoxy)-2-hydroxypropyl]amino]ethyl]amino]-3(2H)-pyridazinone
CAS No. 83395-21-5, 83394-57-4 (monoHCl)
项目整合开发状态: Phase II
项目研究机构: Cassella (...
参考文献标题:N-phenoxypropanol-N'-pyridazinyl ethylendiamines as beta -receptor blockers
文献作者:Raabe,T.; Bohn,H.; Martorana,P.A.; Nitz,R.-E.(Cassella AG)
参考来源:DD 202013; DE 3048487; EP 54946; JP 57128677; US 4532239