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

Finrozole, MPV-2213ad

苯并腈,4-[(1R,2S)-3-(4-氟苯基)-2-羟基-1-(1H-1,2,4-三唑-1-基)丙基]-,rel- 4-[(1R,2R)-3-(4-氟苯基)-2-羟基-1-(1,2,4-三氮唑-1-基)丙基]苄腈 Chemical Name: (?-(R*,S*)-4-[3-(4-Fluorophenyl)-2-hydroxy-1-(1,2,4-triazol-1-yl)propyl]benzo...
参考文献标题:Cyanobenzyl heterocyclic aromatase-inhibiting cpds.
文献作者:Karjalainen,A.J.; Sodervall,M.-L.; Kalapudas,A.M.; Pelkonen,R.O.; Laine,A.M.; Lammintausta,R.A.S.; Salonen,J.S.(Orion Corporation)
参考来源:GB 2273704; JP 1996504424; US 5703109; US 5962495; WO 9413645

VUF-8504

苯扎米,4-甲氧基-N-[3-(2-吡啶基)-1-异喹啉基]-Chemical Name: 4-Methoxy-N-[3-(2-pyridinyl)-1-isoquinolinyl]benzamide
CAS No. 112575-50-5
项目整合开发状态: Biological Testing
项目研究机构: Vrije Universiteit (Originator) 参考文献标题:A novel class of adenosine A3 receptor ligands.2.Structure affinity profile of a series of isoquinoline and quinazoline compounds
文献作者:van Muijlwijk-Koezen,J.E.; Timmerman,H.; Link,R.; van der Goot,H.; Ijzerman,A.P.
参考来源:J Med Chem 1998,41(21),3994

XR-9051

苯扎米,N-[2-[(3,4-二氢-6,7-二甲氧基-2(1H)-异喹啉基)乙基]苯基]-3-[(Z)-[(5Z)-4-甲基-3,6-二氧基-5-(苯甲基)哌拉嗪酰idene]甲基]-,单盐酸盐Chemical Name: 3-[(3Z,6Z)-6-Benzylidene-1-methyl-2,5-dioxopiperazin-3-ylidenemethyl]-N-[4-[2-(6,7-dimet...
参考文献标题:Piperazine-2,5-dione derivs.as modulators of multidrug resistance
文献作者:Ashworth,P.A.; Hunjan,S.; Pretswell,I.A.; Ryder,H.; Brocchini,S.J.(Xenova Group plc)
参考来源:EP 0799210; GB 2311780; JP 1998511385; US 5935955; WO 9620180

Bezafibrate, BM-15075, Befizal, Bezalip Retard, Cedur, Bezatol, Bezalip

苯扎贝特Chemical Name: 2-[4-[2-(4-Chlorobenzamido)ethyl]phenoxy]-2-methylpropionic acid
CAS No. 41859-67-0
项目整合开发状态: Launched-1978
项目研究机构: Norwich Eaton (Originator), Roche (Originator), Kissei (...
参考文献标题:Phenoxyalkylcarbos鋟rederivate und Verfahren zur Herstellung derselben
文献作者:Witte,E.C.; et al.(Boehringer Ingelheim GmbH)
参考来源:DE 2149070; ZA 7206638

Nadolol, SQ-11725, Nadic, Corgaretic, Corgard

苯甲丁氮酮Chemical Name: cis-5-[3-(tert-Butylamino)-2-hydroxypropoxy]-1,2,3,4-tetrahydronaphthalene-2,3-diol
CAS No. 42200-33-9
项目整合开发状态: Launched-1978
项目研究机构: Bristol-Myers Squibb (Originator), S...
参考文献标题:Nadolol
文献作者:Weetman,D.F.; Castar,J.
参考来源:Drugs Fut 1976,1(9),434

Azalanstat dihydrochloride, Azalanstat hydrochloride, RS-21607-197

苯甲胺,4-[[[(2S,4S)-2-[2-(4-氯苯基)乙基]-2-(1H-吡唑-1-甲基)-1,3-二氧鐺-4-基]甲基硫]-盐酸盐(1:2) 阿扎兰司他 Chemical Name: (2S,4S)-4-(4-Aminophenylsulfanylmethyl)-2-[2-(4-chlorophenyl)ethyl]-2-(1H-imidazol-1-ylmethyl)-1,3-dioxol...
参考文献标题:1,3-Dioxolane derivs.as cholesterol lowering agents
文献作者:Walker,K.A.; Burton,P.M.; Swinney,D.C.(Syntex (USA),Inc.)
参考来源:JP 1992308588; US 5158949

Y-20811

苯甲酸,4-[羟基[5-(1-吡达唑-1-基)-2-甲基苯基]-3,5-二甲基-,钠盐(1:1)Chemical Name: 4-[alpha-Hydroxy-5-(1-imidazolyl)-2-methylbenzyl]-3,5-dimethylbenzoic acid sodium salt dihydrate
CAS No. 104363-98-6 (anhydrous)
项目...
参考文献标题:Imidazole derivative
文献作者:Mineo,T.(Welfide Corporation)
参考来源:JP 1986277670

ML-10375

苯甲酸,4-氨基-5-氯-2-甲氧基-, 2-[(3R,5S)-3,5-二甲基-1-哌啶基]乙基酯,rel-Chemical Name: cis-4-Amino-2-methoxy-5-chlorobenzoic acid 2-(3,5-dimethylpiperidin-1-yl)ethyl ester
CAS No. 174008-52-7, 174008-51-6 (trans-iso...
参考文献标题:Esters of 4-amino-5-chloro-2-methoxybenzoic acid,process for their preparation and pharmaceutical compsns.containing them
文献作者:Langlois,M.; Guzzi,U.; Cecchi,R.; Croci,T.(Midy SpA)
参考来源:EP 0683161

Rizatriptan benzoate, MK-462, MK-0462, Maxalt-MLT, Maxalt

苯甲酸利扎曲坦利扎曲坦 N,N-二甲基-2-[5-(1H-1,2,4-三唑-1-甲基)-1H-吲哚-3-基]乙氨酸硫酸盐水合物(2:1:1)Chemical Name: 3-[2-(Dimethylamino)ethyl]-5-(1,2,4-triazol-1-ylmethyl)indole benzoate
CAS No. 145202-66-0, 144034-80-0 (free b...
参考文献标题:Imidazole,triazole and tetrazole derivs
文献作者:Baker,R.; Matassa,V.G.; Street,L.J.(Merck Sharp & Dohme Ltd.)
参考来源:EP 0497512; EP 0778275; US 5298520; US 5451588; US 5602162; US 5602163

S-33138

苯磺酰氯化,3-(1,4-二氢-5-甲基-4-羰基-7-丙基咪唑并[5,1-f][1,2,4]三嗪-2-基)-4-乙氧基-Chemical Name: N-[4-[2-[(3aS,9bR)-8-Cyano-1,2,3,3a,4,9b-hexahydro[1]benzopyrano[3,4-c]pyrrol-2-yl]ethyl]phenyl]acetamide
CAS No. 245514-...
参考文献标题:Chromene derivs.,process for their preparation and pharmaceutical compsns.containing them
文献作者:Lejeune,F.; Hautefaye,P.; Millan,M.; Dubuffet,T.; Lavielle,G.(ADIR et Cie.)
参考来源:EP 0887350; JP 1999071376; US 6090837