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

Naxagolide hydrochloride, PHNO-(+), MK-458, N-0500-(+), L-647339

那高利特盐酸盐那高利特 Chemical Name: (4aR-trans)-4-Propyl-3,4,4a,5,6,10b-hexahydro-2H-naphth[1,2-b]-1,4-oxazin-9-ol hydrochloride; (+)-(4aR,10bR)-4-Propyl-3,4,4a,5,6,10b-hexahydro-2H-naphth[1,2-b]-1,4-oxazin-9...
参考文献标题:Hexahydronaphth(1,2-b)-1,4-oxazines,process for their preparation and pharmaceutical formulation containing them
文献作者:Jones,J.H.; McClure,D.E.; Grenda,V.J.(Merck & Co.,Inc.)
参考来源:EP 0080115

Rivastigmine tartrate, ENA-713, SDZ-212-713, SDZ-ENA-713, Exelon MR, Exelon TDS, Prometax, Exelon

酒石酸卡巴拉汀利凡斯的明 Chemical Name: (S)-N-Ethyl-N-methylcarbamic acid 3-[1-(dimethylamino)ethyl]phenyl ester hydrogen(R,R)-tartrate
CAS No. 129101-54-8, 123441-03-2 (free base)
项目整合开发状态: Launched-1997...
参考文献标题:Phenylcarbamate
文献作者:Enz,A.(Novartis Deutschland GmbH)
参考来源:AU 8812554; BE 1001467; CH 675720; DE 3805744; FR 2611707; GB 2203040; JP 1988238054; JP 1997118617; JP 1997165362

Tolterodine tartrate, Kabi-2234, PNU-200583E, Detrol LA, Detrusitol SR, Urotrol, Detrol, Detrusitol

酒石酸托特罗定托特罗定 Chemical Name: (+)-(R)-3-(2-Hydroxy-5-methylphenyl)-N,N-diisopropyl-3-phenylpropylamine L-tartrate (1:1)
CAS No. 124937-52-6, 124937-51-5 (free base)
项目整合开发状态: Launched-1997
项目研究...
参考文献标题:New amines,their use and preparation
文献作者:J鰊sson,N.A.; Sparf,B.A.; Mikiver,L.; Moses,P.; Nilvebrant,L.; Glas,G.(Pharmacia Corp.)
参考来源:EP 0325571; JP 1991503163; US 5382600; WO 8906644

Tyrphostin B42, AG-490

酪氨酸磷酸化抑制剂AG 490Chemical Name: N-Benzyl-2-cyano-3-(3,4-dihydroxyphenyl)-2-propenamide
CAS No. 133550-30-8
项目整合开发状态: Preclinical
项目研究机构: Chiba University (Originator), University of Texas Syste...
参考文献标题:Tyrphostins.2.Heterocyclic and alpha-substituted benzylidenemalononitrile tyrphostins as potent inhibitors of EGF receptor and ErbB2/neu tyrosine kinases
文献作者:Gazit,A.; Osherov,N.; Posner,I.; Yaish,P.; Poradosu,E.; Gilon,C.; Levitzki,A.
参考来源:J Med Chem 1991,34(6),1896

Ciglitazone, U-63287, ADD-3878

酪里达唑Chemical Name: (?-5-[[4-[(1-Methylcyclohexyl)methoxy]phenyl]methyl]-2,4-thiazolidinedione; 5-[4-(1-Methylcyclohexhylmethoxy)benzyl]thiazolidine-2,4-dione
CAS No. 74772-77-3
项目整合开发状态: Preclin...
参考文献标题:Ciglitazone
文献作者:Nohria,V.; Castar,J.; Serradell,M.N.
参考来源:Drugs Fut 1984,9(4),258

Ketorolac, RS-37619

酮咯酸酮咯酸氨丁三醇 Chemical Name: (?-5-Benzoyl-1,2-dihydro-3H-pyrrolo[1,2-a]pyrrole-1-carboxylic acid; (?-5-Benzoyl-2,3-dihydro-1H-pyrrolizine-1-carboxylic acid
CAS No. 74103-06-3, 74103-07-4 (tromethami...
参考文献标题:1,2-Dihydro-3H-pyrrolo[1,2-a]pyrrole-1-carboxylic acids derivatives and process for the production thereof
文献作者:Muchowski,J.M.; Kluge,A.F.(Roche Bioscience)
参考来源:DE 2731678; ES 460706; ES 470214; FR 2358406; FR 2375234; GB 1554075

Ketotifen, Zaditor(fumarate), Zaditen(fumarate)

酮替芬富马酸酮替芬 Chemical Name: 4-(1-Methyl-4-piperidinylidene)-4,9-dihydro-10H-benzo[4,5]cyclohepta[1,2-b]thiophen-10-one
CAS No. 34580-13-7, 34580-14-8 (fumarate salt)
项目整合开发状态: Launched-1978
项目...
参考文献标题:Process for the production of benzocycloheptathiophenone derivative
文献作者:Bourquin,J.P.; et al.(Novartis AG)
参考来源:DE 2302970; FR 2169091; FR 2401153; GB 1422443; GB 1422444; JP 48081869; JP 55129282

Hydrocortisone aceponate, BDF-6224, BDF-6122, Efficort, Retef

醋丙氢可的松Chemical Name: 11beta,17,21-Trihydroxypregn-4-ene-3,20-dione 21-acetate 17-propionate; 21-Acetoxy-11beta-hydroxy-17-propionyloxypregn-4-ene-3,20-dione
CAS No. 74050-20-7
项目整合开发状态: Launched...
参考文献标题:Hydrocortisone aceponate
文献作者:Castar,J.; Prous,J.
参考来源:Drugs Fut 1987,12(1),20

Aceclofenac, YT-919, Beofenac, Preservex, Gerbin, Falcon, Airtal

醋氯芬酸Chemical Name: Glycolic acid [2-(2,6-dichloroanilino)phenyl]acetate ester; 2-(2,6-Dichlorophenylamino)phenylacetic acid carboxymethyl ester; 2-[2-(2,6-Dichlorophenylamino)phenylacetoxy]acetic acid...
参考文献标题:2-[(2,6-Dichlorophenyl)amino]phenylacetoxyacetyl derivs.and therapeutic compsns.containing same
文献作者:Casas,A.V.(Almirall Prodesfarma,SA)
参考来源:EP 0119932; US 4548952

Erythromycin acistrate, Erasis

醋硬脂红霉素Chemical Name: 2'-Acetylerythromycin stearate; 13-Ethyl-2,4,6,8,10,12-hexamethyl-6,11,12-trihydroxy-9-oxo-3-(3-hydroxy-4-methoxy-2,4-dimethyltetrahydropyran-6-yloxy)-4-(3-acetoxy-4-dimethylamino...
参考文献标题:Acetyl erythromycin stearate,and compsns.contain
文献作者:Honkanen,E.J.; Kairisalo,P.J.; Marttila,E.V.; Marvola,M.L.A.; Pippuri,A.K.; Uotila,J.A.(Orion Corporation)
参考来源:CH 666275; DE 3500179; FR 2557878; GB 2152502; JP 1985158197; US 4599326