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

SB-737552, S-8510

(2Z)-2-异噻唑-3(2H)-亚基-2,6,7,9-四氢咪唑并[4,5-d]吡喃并[4,3-b]吡啶磷酸酯 Chemical Name: 2-(3-Isoxazolyl)-3,6,7,9-tetrahydroimidazo[4,5-d]pyrano[4,3-b]pyridine monophosphate monohydrate
CAS No. 151224-83-8 (anhydro...
参考文献标题:Condensed imidazopyridine derivs.with psychotropic activity
文献作者:Takada,S.; Sasatani,T.; Chomei,N.; Adachi,M.; Matsushita,A.(Shionogi & Co.Ltd.)
参考来源:EP 0556008; JP 1993286973; US 5378848; US 5461062

Trimazosin hydrochloride, CP-191061, Supres, Cardovar

(2-羟基-2-甲基丙基)4-(4-氨基-6,7,8-三甲氧基喹唑啉-2-基)哌嗪-1-羧酸酯盐酸盐三甲哌唑嗪Chemical Name: 4-(4-Amino-6,7,8-trimethoxy-2-quinazolinyl)-1-piperazinecarboxylic acid 2-hydroxy-2-methylpropyl ester monohydrochloride monohy...
参考文献标题:Trimazosin hydrochloride
文献作者:Castar,J.; Weetman,D.F.
参考来源:Drugs Fut 1978,3(4),325

Adrogolide hydrochloride, DAS-431, A-93431.1, ABT-431

(5aR,11bS)-4,5,5a,6,7,11b-六氢-2-丙基-苯并[f]噻吩并[2,3-c]喹啉-9,10-二醇9,10-二乙酸酯 Chemical Name: 9,10-Diacetoxy-2-propyl-4,5,5a(R),6,7,11b(S)-hexahydrobenzo[f]thieno[2,3-c]quinoline hydrochloride
CAS No. 16659...
参考文献标题:Tetracyclic cpds.as dopamine agonists
文献作者:Michaelides,M.R.; Hong,Y.(Abbott Laboratories Inc.)
参考来源:EP 0690863; JP 1996508487; US 5597832; WO 9422858

GW-1616A, GW-311616A

(6aR)-3-异丙基-1-(甲基磺酰基)-4-[(2E)-4-(1-哌啶基)-2-丁烯酰]六氢吡咯并[3,2-b]吡咯-2(1H)-酮盐酸盐(1:1) Chemical Name: (3S,3aS,6aR)-3-Isopropyl-1-(methanesulfonyl)-4-[4-(1-piperidinyl)-2(E)-butenoyl]perhydropyrrolo[3,2-b]pyrro...
参考文献标题:Pyrrolopyrrolone derivs.as inhibitors of neutrophil elastase
文献作者:Dowle,M.D.; Finch,H.; Harrison,L.A.; Inglis,G.G.A.; Johnson,M.R.; Macdonald,S.J.F.; Shah,P.; Smith,R.A.(Glaxo Wellcome plc)
参考来源:EP 0891362; JP 2000507950; US 5994344; WO 9736903

Asoprisnil, J-867

(8S,11R,13S,14S,17S)-11-[4-[(E)-羟基亚氨甲基]苯基]-17-甲氧基-17-(甲氧基甲基)-13-甲基-1,2,6,7,8,11,12,14,15,16-十氢环戊烯并[a]菲-3-酮 Chemical Name: 11beta-[4-[(E)-Hydroxyiminomethyl]phenyl]-17beta-methoxy-17alpha-(methoxymeth...
参考文献标题:11-Benzaldoximeestradiene-derivates,a process for their preparation and pharmaceutical compsns.containing them
文献作者:Schubert,G.; Kaufmann,G.; Sobeck,L.; Oettel,M.; Elger,W.; Kurischko,A.(Jenapharm GmbH)
参考来源:CA 2130516; DE 4322283; EP 0648778

Arundic acid, ONO-2506PO, ONO-2506, Proglia, Cereact

(R)-2-丙基辛酸 2-丙辛酸 Chemical Name: 2(R)-Propyloctanoic acid
CAS No. 185517-21-9, 31080-41-8 (racemate), 161089-52-7 (racemate, Na salt)
项目整合开发状态: Phase II
项目研究机构: Ono (Originator)
合成路线:The a...
参考文献标题:Novel intermediates and processes for the preparation of optically active octanoic acid derivs.
文献作者:Yamamoto,H.(Ono Pharmaceutical Co.,Ltd.)
参考来源:EP 1078921; US 6333415; WO 9958513

Dexibuprofen, (S)-(+)-Ibuprofen, Atriscal, Dolomin, Seractil, DexOptifen

(S)-(+)-布洛芬Chemical Name: (S)-(+)-p-Isobutylhydratropic acid; (S)-alpha-Methyl-4-(2-methylpropyl)benzeneacetic acid; 2(S)-(4-Isobutylphenyl)propionic acid
CAS No. 51146-56-6
项目整合开发状态: Launched-...
参考文献标题:Microbiological transformation 43.Epoxide hydrolaxes as tools for the synthesis of enantiopure alpha-methylstyrene oxides: A new and efficient synthesis of (S)-ibuprofen
文献作者:Cleij,M.; et al.
参考来源:J Org Chem 1999,64(14),5029

Esoxybutynin, (S)-Oxybutynin

(S)-奥昔布宁Chemical Name: (S)-2-Cyclohexyl-2-phenylglycolic acid 4-(diethylamino)but-2-ynyl ester
CAS No. 119618-22-3
项目整合开发状态: Phase III
项目研究机构: Sepracor (Originator)
合成路线:Racemic cyclohexy...
参考文献标题:Synthesis of optically active cyclohexylphenylglycolic acid and its esters
文献作者:Senanayake,C.H.; Bakale,R.P.; Vandenbossche,C.P.; McConville,F.X.; Lopez,J.L.(Sepracor Inc.)
参考来源:US 5973182; US 6140529; WO 0023414

Zoniporide hydrochloride, CP-597396

[1-(喹啉-5-基)-5-环丙基-1H-吡唑-4-甲酰基]胍 Chemical Name: N''-[5-Cyclopropyl-1-(5-quinolyl)-1H-pyrazol-4-ylcarbonyl]guanidine hydrochloride monohydrate
CAS No. 241800-97-5 (anhydrous), 241800-98-6 (free base...
参考文献标题:N-[(Substd.five-membered di- or triaza diunsaturated ring)carbonyl] guanidine derivs.for the treatment of ischemia
文献作者:Guzman-Perez,A.; Ruggeri,R.B.; Wester,R.T.; Hamanaka,E.S.; Mularski,C.J.(Pfizer Inc.)
参考来源:EP 1056729; WO 9943663

Nolomirole hydrochloride, CHF-1035

[6-甲基氨基-2-(2-甲基丙酰氧基)-5,6,7,8-四氢萘-1-基]2-甲基丙酸酯 Chemical Name: (?-5,6-Diisobutyryloxy-2-(methylamino)-1,2,3,4-tetrahydronaphthalene hydrochloride
CAS No. 138531-51-8, 90060-42-7 (free base)
项目整合开发...
参考文献标题:1,2,3,4-Tetrahydronaphthaline derivs.,process for their preparation and pharmaceutical compsns.containing them
文献作者:Chiesi,P.; Villani,V.(Chiesi Farmaceutici SpA)
参考来源:DE 3320936; GB 2123410