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

Leteprinim potassium, AIT0082, AIT-082, Neotrofin, Neotrophin

苯甲酸,4-[[3-(1,6-二氢-6-氧-9H-普林-9-基)-1-氧丙基]氨基]- Chemical Name: 4-[3-(6-Oxo-1,6-dihydro-9H-purin-9-yl)propionamido]benzoic acid potassium salt
CAS No. 192564-13-9, 138117-50-7 (free acid)
项目整合开发状态: ...
参考文献标题:Multi-functional pharmaceutical cpds.and methods of use
文献作者:Glasky,A.J.
参考来源:WO 9114434

Fenoctimine sulfate

苯辛替明苯辛替明硫酸盐半水合物Chemical Name: N-[4-(1,1-Diphenylmethyl)piperidin-1-ylmethylidene]octan-1-amine sulfate
CAS No. 69365-67-9, 69365-65-7 (free base), 69365-66-8 (hemihydrate)
项目整合开发状态: Not Determ...
参考文献标题:
文献作者:Scott,M.; Rasmussen,C.
参考来源:BE 875164; DE 2912026; FR 2421169; GB 2017689; JP 79132580

Irindalone tartrate, LU-21-098

茚达酮 Chemical Name: (+)-(1R,3S)-1-[2-[4-(p-Fluorophenyl)-1-indanyl]-1-piperazinyl]ethyl]-2-imidazolidinone L-(+)-tartrate
CAS No. 104113-57-7, 96478-43-2 (free base)
项目整合开发状态: Phase II
项目研究机构...
参考文献标题:Antihypertensive activity in a series of 1-piperazino-3-phenylindans with potent 5-HT2-antagonistic activity
文献作者:Hyttel,J.; Bogeso,K.P.; Gundertofte,K.; Boeck,V.; Christensen,A.V.; Arnt,J.
参考来源:J Med Chem 1988,31(12),2247

Mosapride citrate, TAK-370, AS-4370, Gasmotin

莫沙必利枸橼酸莫沙必利Chemical Name: (?-4-Amino-5-chloro-2-ethoxy-N-[4-(4-fluorobenzyl)morpholin-2-ylmethyl]benzamide citrate dihydrate
CAS No. 144256-27-9 (anhydrous free base), 112885-41-3 (anhydrous free...
参考文献标题:Novel benzamides as selective and potent gastrokinetic agents.2.Synthesis and structure-activity relationships of 4-amino-5-chloro-2-ethoxy-N-[[4-(4-fluorobenzyl)-2-morpholinyl]methyl] benzamide citrate (AS-4370) and related compounds
文献作者:Kato,S.; Morie,T.; Kon,T.; Yoshida,N.; Karasawa,T.; Matsumoto,J.
参考来源:J Med Chem 1991,34(2),616-24

Moveltipril calcium, Altiopril calcium, MC-838, Lowpress

莫维普利钙莫维普利 Chemical Name: 1-[3-[[2(R)-[(Cyclohexylcarbonyl)amino]-1-oxopropyl]thio]-2(S)-methyl-1-oxopropyl]-L-proline calcium salt(2:1)
CAS No. 85921-53-5, 85856-54-8 (free base)
项目整合开发状态: Pr...
参考文献标题:Proline derivative
文献作者:Iwaoka,T.; Kuromaru,K.; Obatake,N.; Hata,S.I.; Matsunaga,I.; Fujimura,Y.; Aono,J.; Hinohara,Y.; Fukushima,M.; Nabata,H.; Sakai,K.; Tanaka,S.; Nakano,H.(Chugai Pharmaceutical Co.Ltd.)
参考来源:BE 0893553; JP 1982209270; JP 1988045252

Spirorenone, ZK-35973, Delta-1-MSp

螺利酮Chemical Name: 6beta,7beta:15beta,16beta-Dimethylen-1,4-androstadien[17(beta-1')-spiro-5']-perhydrofuran-2',3-dione; 17-Hydroxy-6beta,7beta:15beta,16beta-dimethylene-3-oxo-17alpha-pregna-1,4-diene...
参考文献标题:Novel spironolactones and process for their preparation
文献作者:Losert,W.; Bittler,D.; Vasals-Stenzel,J.; Wiechert,R.; Kerb,U.(Schering AG)
参考来源:DE 2652761; US 4129564

Spirohydantoin mustard(former USAN), Spiromustine, SHM, NSC-172112, Speratine

螺莫司汀Chemical Name: 3-[2-[Bis(2-chloroethyl)amino]ethyl]-1,3-diazaspiro[4,5]decane-2,4-dione; 3-[2-[Bis(2-chloroethyl)amino]ethyl]-5,5-pentamethylenehydantoin
CAS No. 56605-16-4
项目整合开发状态: Phase ...
参考文献标题:Spiromustine
文献作者:Prous,J.; Castar,J.
参考来源:Drugs Fut 1986,11(9),773

Epidoxorubicin, Pidorubicin(former Prop INN), 4'-epi-Doxorubicin, 4'-epi-Adriamycin, Epirubicin hydrochloride, 4'-epi-DX, IMI-28, E-ADM, Ellence, Farmorubicina, Pharmorubicin, Farmorubicin

表阿霉素Chemical Name: (1S,3S)-3-Glycoloyl-1,2,3,4,6,11-hexahydro-3,5,12-trihydroxy-10-methoxy-6,11-dioxo-1-naphthacenyl 3-amino-2,3,6-trideoxy-alpha-L-arabino-hexopyranoside hydrochloride; (8S,10S)-10-[...
参考文献标题:Epirubicin
文献作者:Serradell,M.N.; Castar,J.; Hopkins,S.J.; Blancafort,P.
参考来源:Drugs Fut 1983,8(5),402

Cimetidine, Tagamet

西咪替丁Chemical Name: N''-Cyano-N-methyl-N'-[2-(5-methyl-1H-imidazol-4-ylmethylsulfanyl)ethyl]guanidine
CAS No. 51481-61-9
项目整合开发状态: Launched-1977
项目研究机构: GlaxoSmithKline (Originator)
合成路线:1...
参考文献标题:Cimetidine
文献作者:Castar,J.
参考来源:Drugs Fut 1976,1(1),13

Sivelestat sodium hydrate, EI-546, Ono-5046.Na, Elaspol

西维来司他 Chemical Name: N-[2-[4-(tert-Butoxycarbonyloxy)phenylsulfonamido]benzoyl]glycine sodium salt tetrahydrate
CAS No. 201677-61-4, 127373-66-4 (anhydrous, free acid), 150374-95-1 (monoNa salt) 参考文献标题:Derivs.of p-substituted phenyl ester of pivalic acid
文献作者:Imaki,K.; Arai,Y.; Okegawa,T.(Ono Pharmaceutical Co.,Ltd.)
参考来源:EP 0347168; JP 1991020253; JP 1994179645; US 5017610; US 5336681; US 5403850