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

Dithiosteine, Erdosteine, KW-9144, RV-144, Erdotin, Tussol, Vectrine, Edirel

厄多司坦Chemical Name: (?-S-[2-Oxo-2-(2-oxothien-3-ylamino)ethyl]thioglucolicacid; (?-2-[2-Oxo-2-(oxothien-3-ylamino)ethylsulfanyl]acetic acid; (?-3-[2-(Carboxymethylsulfanyl)acetamido]tetrahydrothiophen-...
参考文献标题:ERDOSTEINE < Rec INN >
文献作者:Fregnan,G.B.; Pappalardo,M.
参考来源:Drugs Fut 1990,15(9),887

Erbulozole, R-55104

厄布洛唑Chemical Name: Ethyl (?-cis-p-[[[2-(Imidazol-1-ylmethyl)-2-(p-methoxyphenyl)-1,3-dioxolan-4-yl]methyl]thio]carbanilate; (?-cis-[4-[[2-((1H-Imidazol-1-ylmethyl)-2-(4-methoxyphenyl)-1,3-dioxolan-4-y...
参考文献标题:Tubulozole Hydrochloride
文献作者:Van Ginckel,R.; Geuens,G.; Heeres,J.
参考来源:Drugs Fut 1984,9(12),911

Irbesartan, BMS-186295, SR-47436, Avapro, Karvea, Aprovel

厄贝沙坦Chemical Name: 2-Butyl-1-[2'-(1H-tetrazol-5-yl)biphenyl-4-ylmethyl]spiro[2-imidazoline-4,1'-cyclopentane]-5-one
CAS No. 138402-11-6
项目整合开发状态: Launched-1997
项目研究机构: Sanofi-Aventis (Origina...
参考文献标题:Heterocyclic N-substd.derivs.,their preparation and the pharmaceutical compsns.containing them
文献作者:Bernhart,C.; Breliere,J.-C.; Clement,J.; Nisato,D.; Perreaut,P.(Sanofi-Synthabo )
参考来源:EP 0454511; FR 2659967; FR 2665702; JP 1992506222; JP 1998279566; US 5270317; WO 9114679

Procyanidin B-2

原花青素B2Chemical Name: (2R,2'R,3R,3'R,4R)-2,2'-Bis(3,4-dihydroxyphenyl)-3,3',4,4'-tetrahydro-2H,2'H-4,8'-bi-1-benzopyran-3,3',5,5',7,7'-hexaol
CAS No. 29106-49-8
项目整合开发状态: Phase II
项目研究机构: Kyow...
参考文献标题:Synthetic methods for polyphenols
文献作者:Lippman,M.E.; Kozikowski,A.P.; Tueckmantel,W.; Romanczyk,L.J.Jr.(Mars,Inc.)
参考来源:WO 9919319

Dehydrodidemnin B, Aplidine, DDB, Aplidin

去氢代代宁BChemical Name: (3S,6S,8S,12S,13R,16S,17R,20S,23S)-16-[N-(1,2-Dioxopropyl)-L-prolyl-D-(N-methyl)leucylamino]-12-hydroxy-3-isobutyl-8-isopropyl-20-(4-methoxybenzyl)-6,17,21-trimethyl-13-[1(S)-meth...
参考文献标题:Dehydrodidemnin B
文献作者:Rinehart,K.L.; Lithgow-Bertelloni,A.M.(PharmaMar,SA)
参考来源:WO 9104985

Dehydroepiandrosterone, Prasterone, IPL-1001, PB-007, EL-10, DHEA, GL-701, Fidelin, Anastar, Prestara, Inflabloc, Aslera

去氢表雄酮Chemical Name: 3beta-Hydroxyandrost-5-en-17-one; Dehydroepiandrosterone
CAS No. 53-43-0
项目整合开发状态: Recommended Approval
项目研究机构: Genelabs (Proprietary), Genelabs (Orphan Drug), Paladin (Or...
参考文献标题:Prasterone
文献作者:Castar,J.; Mealy,N.; Rabasseda,X.
参考来源:Drugs Fut 1995,20(6),575

Desogestrel, Org-2969, Cerazette

去氧孕烯Chemical Name: 13-Ethyl-11-methylene-18,19-dinorpregn-4-en-20-yn-17alpha-ol
CAS No. 54024-22-5
项目整合开发状态: Launched-1999
项目研究机构: Organon (Originator)
合成路线:The silylation of the hydroxyke...
参考文献标题:A short enantioselective total synthesis of the third-generation oral contraceptive desogestrel
文献作者:Huang,A.X.; Corey,E.J.
参考来源:J Am Chem Soc 1999,121(4),710

5-Fluorodeoxyuridine, Doxifluridine, 5-DFUR, Ro-21-9738, Furtulon

去氧氟尿苷Chemical Name: 5'-Deoxy-5-fluorouridine
CAS No. 3094-09-5
项目整合开发状态: Launched-1987
项目研究机构: Chugai (Originator), Roche (Originator)
合成路线:This compound can be prepared by several differe...
参考文献标题:5'-Deoxy-5-fluoropyrimidine nucleosides
文献作者:Cook,A.F.(Hoffmann-La Roche,Inc.)
参考来源:DE 2756653; ES 471584; FR 2374334; GB 1589688; JP 53095982; US 4071680

Desferrioxamine, Deferoxamine, ICL-749B(depot formulation), CGH-749B(depot formulation), DFO, Ba-33112(mesylate), Ba-29837(HCl), NSC-527604, Desferin, Desferal

去铁胺 N'-[5-[[4-[[5-(乙酰基羟基氨基)戊基]氨基]-1,4-二氧代丁基]羟基氨基]戊基]-N-(5-氨基戊基)-N-羟基琥珀酰胺单盐酸盐甲磺酸去铁胺Chemical Name: N-[5-[3-[(5-Aminopentyl)hydroxycarbamoyl]propionamido]pentyl]-3-[[5-(N-hydroxyacetamido)pentyl]carbamo...
参考文献标题:Liposome-Entrapped Desferrioxamine deferoxamine
文献作者:Blancafort,P.; Castar,J.; Serradell,M.N.; Hopkins,S.J.
参考来源:Drugs Fut 1979,4(7),500

Deferiprone, CP20, CGP-37391, CP020, L1, Ferriprox, Deferum, Kelfer

去铁酮Chemical Name: 3-Hydroxy-1,2-dimethyl-4(1H)-pyridone
CAS No. 30652-11-0
项目整合开发状态: Launched-1995
项目研究机构: BTG (Technology Transfer), Cipla (Originator), Royal Free Hospital (Originator), Chi...
参考文献标题:Synthesis,physicochemical properties,and biological evaluation of N-substituted 2-alkyl-3-hydroxy-4(1H)-pyridinones: Orally active iron chelators with clinical potential
文献作者:Dobbin,P.S.; Hider,R.C.; Hall,A.D.; Taylor,P.D.; Sarpong,P.; Porter,J.B.; Xiao,G.; Van der Helm,D.
参考来源:J Med Chem 1993,36(17),2448