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

IS-741

环己烷羧酰胺,N-[2-[(乙基磺酰)氨基]-5-(三氟甲基)-3-吡啶基]-,钙盐(2:1) 环己烷羧酰胺,N-[2-[(乙基磺酰)氨基]-5-(三氟甲基)-3-吡啶基]-Chemical Name: N-[2-(Ethylsulfonamido)-5-(trifluoromethyl)pyridin-3-yl]cyclohexanecarboxamide sodium salt
CAS...
参考文献标题:Diaminotrifluoromethylpyridine derivs.,process for their production and phospholipase A2 inhibitor containing them
文献作者:Haga,T.; Sugi,H.; Shigehara,I.; Odawara,S.; Yotsuya,S.; Kimura,H.; Yamamoto,K.(Ishihara Sangyo Kaisha,Ltd.)
参考来源:EP 0465913; JP 1993170742; JP 1994247934; JP 1994263735; US 5229403; US 5260320; US 5348967; US 5492908

Xemilofiban, CS-551, SC-54684A(HCl), SC-54684

珍米洛非班 4-戊酸,3-[[4-[[4-(氨基亚胺甲基)苯基]氨基]-1,4-二氧乙基]氨基,乙酯,一盐酸盐,(3S)-(9CI) Chemical Name: 3(S)-(4-Amidinophenylaminosuccinylamino)-4-pentynoic acid ethyl ester; 3(S)-[4-(4-Amidinophenylamino)succinylamino]-4...
参考文献标题:Substd.beta-amino acid derivs.useful as platelet aggregation inhibitors
文献作者:Bovy,P.R.; Rico,J.G.; Rogers,T.E.; Tjoeng,F.S.; Zablocki,J.A.(Pharmacia Corp.)
参考来源:EP 0542708; EP 0614360; JP 1995500111; US 5239113; WO 9307867

Bambuterol, KWD-2183, Bambec

班布特罗盐酸班布特罗 Chemical Name: Dimethylcarbamic acid (?-5-[2-(tert-butylamino)-1-hydroxyethyl]-1,3-phenylene diester; (?-5-[2-(tert-Butylamino)-1-hydroxyethyl]-m-phenylene bis(dimethylcarbamate)
CAS ...
参考文献标题:Bronchospamolytic carbamate derivatives
文献作者:Olsson,O.A.T.; Svensson,L.A.; Wetterlin,K.I.L.(Draco L鋕emedel AB)
参考来源:DD 202001; EP 0043807; JP 8240453; US 4419364; US 4451663

Sumatriptan succinate, SN-308, GR-43175C, Imigrane, Suminat, Imitrex, Imigran

琥珀酸舒马普坦舒马曲坦Chemical Name: 3-[2-(Dimethylamino)ethyl]-N-methyl-1H-indole-5-ylmethylsulfonamide succinate
CAS No. 103628-48-4 ((1:1) salt), 103628-47-3 ((2:1) salt), 103628-46-2 (free base)
项目整合开...
参考文献标题:SUMATRIPTAN SUCCINATE < Prop INNM; BAN >
文献作者:Humphrey,P.P.A.; Feniuk,W.; Perren,M.J.; Oxford,A.W.; Brittain,R.T.; Prous,J.; Castar,J.
参考来源:Drugs Fut 1989,14(1),35

Norfloxacin succinil, Eminor

琥诺沙星Chemical Name: 7-[4-(3-Carboxypropionyl)piperazin-1-yl]-1-ethyl-6-fluoro-4-oxo-1,4-dihydroquinoline-3-carboxylic acid
CAS No. 100587-52-8, 100587-53-9 (diNa salt)
项目整合开发状态: Launched-1984 参考文献标题:Cpds.having antibacterial activity,process for their preparation and pharmaceutical compsns.Containing them
文献作者:Di Schiena,M.(Farmades)
参考来源:EP 0155006

Revatropate, UK-112166-04(hydrobromide), UK-112166

瑞伐托酯Chemical Name: 2(S)-(Hydroxymethyl)-4-[(Rs)-methylsulfinyl]-2-phenylbutyric acid quinuclidin-3(R)-yl ester
CAS No. 149926-91-0
项目整合开发状态: Phase II
项目研究机构: Pfizer (Originator)
合成路线:The ...
参考文献标题:Quinuclidine esters process and intermediate for their preparation and pharmaceutical compsns.containing them
文献作者:Cross,P.E.; Stobie,A.(Pfizer Inc.)
参考来源:EP 0603229; JP 1994510991; JP 1997315970; WO 9306098

Mequitamium iodide, Mequitazium iodide, LG-30435

甲喹碘铵Chemical Name: 1-Methyl-3-(10H-phenothiazin-10-ylmethyl)azoniabicyclo[2.2.2]octane iodide
CAS No. 101396-42-3
项目整合开发状态: Phase II
项目研究机构: Guidotti (Originator)
合成路线:By quaternization o...
参考文献标题:Phenothiazine cpds.with anti-bronchospastic activ
文献作者:Subissi,A.(Guidotti Laboratori SpA)
参考来源:EP 0159059; JP 1985209521; US 4603132

Metronidazole, IDR-90105(Ophthalmic), Rosased, Zidoval, Metrogel, Flagyl

甲硝唑Chemical Name: 2-Methyl-5-nitro-1H-imidazole-1-ethanol
CAS No. 443-48-1, 133884-00-1 (deleted CAS)
项目整合开发状态: Launched-1960
项目研究机构: Pfizer (Originator), 3M Pharmaceuticals (Not Determined)...
参考文献标题:Process for the preparation of 1-hydroxyalkyl-2-methyl-5-nitro-imidazoles
文献作者:Buforn,A.; Massonneau,V.; Mulhauser,M.(Aventis SA)
参考来源:EP 0325513; FR 2625999

Amezinium methylsulfate, LU-1631, Risumic, Supratonin, Regulton

甲磺美嗪Chemical Name: 4-Amino-6-methoxy-1-phenylpyridazinium methylsulfate
CAS No. 30578-37-1, 51410-15-2 (chloride)
项目整合开发状态: Launched-1981
项目研究机构: Abbott (Originator), Dainippon Pharmaceutica...
参考文献标题:Amezinium metilsulfate
文献作者:Unterhalt,B.
参考来源:Drugs Fut 1981,6(4),207

Doxazosin mesylate, UK-33274, Dedralen, Carduran Neo, Zoxan, Progandol, Tensiobas, Cardenalin, Cardular, Cardura, Carduran

甲磺酸多沙唑嗪多沙唑嗪盐酸多沙唑嗪Chemical Name: 4-Amino-2-[4-(1,4-benzodioxan-2-ylcarbonyl)piperazin-1-yl]-6,7-dimethoxyquinazoline methanesulfonate; 1-(4-Amino-6,7-dimethoxyquinazolin-2-yl)-4-(1,4-benzodioxan-2-y...
参考文献标题:Antihypertensive 4-amino-2-[4-(1,4-benzodioxan-2-carbonyl) piperazin-1-yl or homopiperazin-1-yl]quinazolines
文献作者:Campbell,S.F.(Pfizer Inc.)
参考来源:DE 2847623; FR 24079529; US 4188390