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

Tomoxiprole, MDL-035

托莫普罗Chemical Name: 3-Isopropyl-2-(4-methoxyphenyl)-3H-naphth[1,2-d]imidazole
CAS No. 76145-76-1
项目整合开发状态: Preclinical
项目研究机构: Lepetit (Originator)
合成路线:Reaction of 1-nitroso-2-naphthol (I)...
参考文献标题:Antimicrobial 3H-naphto[1,2-d]imidazoles
文献作者:Toja,E.; Omodei-Sale,A.; Selva,D.(Lepetit SpA)
参考来源:EP 0012866; JP 8092376; US 4340607; US 4435417

Tolrestatin, Tolrestat, AY-27773, Alrestin, Lorestat, Alredase

托雷斯萘Chemical Name: N-[6-Methoxy-5-(trifluoromethyl)-1-naphthylthiocarbonyl]-N-methylglycine
CAS No. 82964-04-3
项目整合开发状态: Withdrawn
项目研究机构: Wyeth Pharmaceuticals (Originator), Recordati (Licen...
参考文献标题:N-Naphtoylglycine derivatives
文献作者:Sestanj,K.; Abraham,N.A.; Bellini,F.; Treasurywala,A.; Humber,L.G.(Ayerst Laboratories Inc.)
参考来源:EP 0059596; JP 570158756; US 4391825

Zeniplatin, CL-286558

折尼铂Chemical Name: cis-[2,2-Bis(aminomethyl)-1,3-propanediol-N,N'][1,1-cyclobutanedicarboxylato(2-)-O,O']platinum (II); (SP-4-2)-[2,2-Bis(aminomethyl)-1,3-propanediol-N,N'][1,1-cyclobutanedicarboxylato...
参考文献标题:[2,2-Bis(aminomethyl)-1,3-propanediol-N,N']platinum complexes
文献作者:Grassing Child,R.; Bitha,P.; Hlavka,J.J.; Lin,Y.(Zyma)
参考来源:AU 8432572; EP 0140830; ES 8802308; GB 2145720; JP 1985149581; US 4665202

Zenarestat, CI-1014, FR-74366, FK-366

折那司他Chemical Name: 2-[3-(4-Bromo-2-fluorobenzyl)-7-chloro-2,4-dioxo-1,2,3,4-tetrahydroquinazolin-1-yl]acetic acid; 3-(4-Bromo-2-fluorobenzyl)-7-chloro-2,4-dioxo-1-2,3,4-tetrahydroquinazoline-1-acetic ...
参考文献标题:New quinazoline derivs.,process for their production and pharmaceutical compsns.comprising them
文献作者:Hashimoto,M.; Oku,T.; Ito,Y.; Namiki,T.; Sawada,K.; Kasahara,C.; Baba,Y.(Fujisawa Pharmaceutical Co.,Ltd.)
参考来源:EP 0218999; JP 1987096476; JP 1989125322; JP 1989131164; US 4734419; US 4883800

Lafutidine, FRG-8813, Stogar, Protecadin

拉呋替丁Chemical Name: (?-2-(Furan-2-ylcarbonylsulfinyl)-N-[4-[4-(piperidin-1-ylmethyl)pyridin-2-yloxy]-2(Z)-butenyl]acetamide
CAS No. 118288-08-7
项目整合开发状态: Launched-2000
项目研究机构: UCB Japan (Origi...
参考文献标题:Pyridyloxy derivs
文献作者:Hirakawa,N.; Kashiwaba,N.; Matsumoto,H.; Hosoda,A.; Sekine,Y.; Isowa,Y.; Yamaura,T.; Sekine,A.; Nishikawa,M.(UCB Japan)
参考来源:EP 0282077; JP 1988225371; JP 1989230556; JP 1989230576; US 4912101

Laquinimod, SAIK-MS compound, ABR-215062

拉喹莫德Chemical Name: 5-Chloro-N-ethyl-4-hydroxy-1-methyl-2-oxo-N-phenyl-1,2-dihydroquinoline-3-carboxamide
CAS No. 248281-84-7
项目整合开发状态: Phase II
项目研究机构: Active Biotech (Originator), Teva (Lice...
参考文献标题:Quinoline derivs.
文献作者:Bjk,A.; J鰊sson,S.; Fex,T.; Hedlund,G.(Active Biotech AB)
参考来源:EP 1073639; JP 2002513006; US 6077851; WO 9955678

Latanoprost, XA41, PhXA34 [as 15(R,S)-isomer], PhXA41, Xalatan

拉坦前列素Chemical Name: (15R)-17-Phenyl-13,14-dihydro-18,19,20-trinor-PGF2alpha isopropyl ester; [1R-[1alpha(Z),2beta(R),3alpha,5alpha]]-7-[3,5-Dihydroxy-2-(3-hydroxy-5-phenylpentyl)cyclopentyl]-5-hepteno...
参考文献标题:A new process for the preparation of latanoprost
文献作者:Gutman,A.; Nisnevich,G.; Etinger,M.; Zaltzman,I.; Judovich,L.; Pertsikov,B.
参考来源:WO 0155101

Lapatinib, 016, 572016, GW-2016, GW-572016

拉帕替尼二甲苯磺酸拉帕替尼 Chemical Name: N-[3-Chloro-4-(3-fluorobenzyloxy)phenyl]-6-[5-[2-(methylsulfonyl)ethylaminomethyl]furan-2-yl]quinazolin-4-amine
CAS No. 231277-92-2, 388082-78-8 (4-methylbenzenesulfon...
参考文献标题:Bicyclic heteroaromatic cpds.as protein tyrosine kinase inhibitors
文献作者:Guntrip,S.B.; Lackey,K.E.; Cockerill,G.S.; Carter,M.C.; Smith,K.J.(Glaxo Group Ltd.)
参考来源:EP 1047694; WO 9935146

Lazabemide hydrochloride, Ro-19-6327/001, Tempium, Pakio

拉扎贝胺盐酸盐拉扎贝胺 Chemical Name: N-(2-Aminoethyl)-5-chloropyridine-2-carboxamide hydrochloride
CAS No. 103878-83-7, 103878-84-8 (free base)
项目整合开发状态: Phase III
项目研究机构: Chugai (Originator), Roche (...
参考文献标题:Ethylenediaminemonoamide derivs.,pharmaceutical compsns.containing them and use of these cpds.As antidepressants or antiparkinsonians
文献作者:Imhof,R.; Kyburz,E.(F.Hoffmann-La Roche AG)
参考来源:AU 8546636; CH 661043; CH 664755; DE 3530046; ES 8705407; ES 8800158; FR 2569694; JP 1986060657; JP 1995300417; US 4764522

Moxalactam disodium, Latamoxef sodium, S-6059(free acid), LY-127935, Shiomarin, Moxam

拉氧头孢钠盐拉氧头孢 Chemical Name: (6R,7R)-7-[2-(4-Hydroxyphenyl)-3-oxido-3-oxopropionamido]-7-methoxy-3-(1-methyl-1H-tetrazol-5-ylsulfanylmethyl)-8-oxo-5-oxa-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid ...
参考文献标题:Arylmalonamido-1-oxadethiacephalosporins
文献作者:Nagata,W.; Narisada,M.(Shionogi & Co.Ltd.)
参考来源:US 4180571