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

2614W94

3-[1-(三氟甲基)乙氧基]苯昔林-10,10-二氧化物Chemical Name: 3-[1-(Trifluoromethyl)ethoxy]phenoxathilin-10,10-dioxide
CAS No. 205187-35-5, 205187-51-5 ((R)-isomer), 205187-54-8 ((S)-isomer)
项目整合开发状态: Preclinical...
参考文献标题:Pharmacologically active cpds.and use
文献作者:Boros,E.; Harfenist,M.; Heyer,D.(Krenitsky Pharmaceuticals,Inc.)
参考来源:WO 9812190

KF-24345

3-[1-[6,7-二乙氧基-2-(4-吗啉基)喹唑啉-4-基]哌啶-4-基]-1,6-二甲基喹那唑仑-2,4(1H,3H)-二酮Chemical Name: 3-[1-[6,7-Diethoxy-2-(4-morpholinyl)quinazolin-4-yl]piperidin-4-yl]-1,6-dimethylquinazolin-2,4(1H,3H)-dione
CAS No. 1...
参考文献标题:Quinazoline deriv.
文献作者:Fujiwara,S.; Okamura,Y.; Takai,H.; Nonaka,H.; Moriyama,T.(Kyowa Hakko Kogyo Co.,Ltd.)
参考来源:EP 0726267; JP 1997165385; US 5948784; WO 9606841

IDN-1965

3-[2(S)-(1,3-二甲基-1H-吲哚-2-酰羧酰胺)-3-甲基丁胺]-5-氟-4-氧戊二醇酸Chemical Name: 3-[N-(1,3-dimethyl-1H-indol-2-ylcarbonyl)-L-valylamino]-5-fluoro-4-oxopentanoic acid; 3-[2(S)-(1,3-Dimethyl-1H-indol-2-ylcarboxamido)-3...
参考文献标题:C-Terminal modified (N-substd.)-2-indolyl dipeptides as inhibitors of the ICE/ced-3 family of cysteine proteases
文献作者:Bai,X.; Karanewsky,D.S.(Idun Pharmaceuticals,Inc.)
参考来源:US 5869519; US 5877197; WO 9811129

CNUA

3-[3-(2-氯乙基)-3-亚硝基脲基]-3-脱氧-D-阿洛糖Chemical Name: 3-[3-(2-Chloroethyl)-3-nitrosoureido]-3-deoxy-D-allose; 3-[[[(2-Chloroethyl)nitrosoamino]carbonyl]amino]-3-deoxy-D-allose
CAS No. 81428-46-8
项目整合开发...
参考文献标题:D-Allose derivative and preparation method thereof
文献作者:Yamada,M.; Edanami,K.; Kuroda,T.(Wakamoto Pharmaceutical Co.,Ltd.)
参考来源:DE 3111593; JP 81158797; US 4349546

Pelanserin hydrochloride, TR-2515

3-[3-(4-苯基-1-吡嗪基)丙基]奎那佐林-2,4(1H,3H)-二酮dro氯化物培兰色林Chemical Name: 3-[3-(4-Phenyl-1-piperazinyl)propyl]quinazoline-2,4(1H,3H)-dione hydrochloride
CAS No. 42877-18-9, 4052-11-3 (diHCl), 2208-51-7 (free ...
参考文献标题:TR-2515
文献作者:Schut,R.N.; Hong,E.
参考来源:Drugs Fut 1985,10(11),929

Dezinamide, AN-051, ADD-94057, AHR-11748

3-[3-(三氟甲基)苯氧基]-1-氮杂环丁烷甲酰胺Chemical Name: 3-[3-(Trifluoromethyl)phenoxy]-1-azetidinecarboxamide
CAS No. 91077-32-6
项目整合开发状态: Phase II
项目研究机构: Wyeth Pharmaceuticals (Originator)
合成路线:Reactio...
参考文献标题:3-Phenoxy-1-azetidine-carboxamides
文献作者:Teng,L.C.(A.H.Robins Co.Inc.)
参考来源:EP 0102194; US 4571393

PNU-96391, (S)-(-)-OSU-6162

3-[3-(甲基磺酰基)苯基]-1-丙基哌啶哌啶,3-[3-(甲基磺酰)苯基]-1-丙基-,(3R)- Chemical Name: (S)-(-)-3-[3-(Methanesulfonyl)phenyl]-1-propylpiperidine
CAS No. 146798-66-5, 160777-43-5 ((R)-isomer)
项目整合开发状态: Clinical
项...
参考文献标题:New centrally acting substd.phenylazacycloalkanes
文献作者:Svensson,K.A.I.; Wikstr鰉,H.V.; Carlsson,P.A.E.; Boije,A.M.P.; Waters,R.N.; Sonesson,C.A.; Stjerulof,N.P.; Andersson,B.R.(Pharmacia Corp.)
参考来源:EP 0641320; JP 1994509561; US 5462947; WO 9218475

Imidolol hydrochloride hydrate, Adimolol hydrochloride hydrate, MEN-935

3-[3-[(2-羟基-3-萘-1-基氧基丙基)氨基]-3-甲基丁基]-1H-苯并咪唑-2-酮水合物盐酸盐阿地洛尔 Chemical Name: 1-[3-[[3-(1-Naphthoxy)-2-hydroxypropyl]amino]-3,3-dimethylpropyl]-2-benzimidazolinone hydrochloride hydrate; 1-[3-[[2-Hydroxy...
参考文献标题:1-Aryloxy-2-hydroxy-3-[(benzimidazolin-one-substituted alkyl)-amino]-propanes and salts thereof
文献作者:Hoefke,W.; et al.(Boehringer Ingelheim GmbH)
参考来源:DE 2644833

GW-3965

3-[3-[[[2-氯-3-(三氟甲基)苯基]甲基](2,2-联苯基乙基)氨基]丙氧基]苯乙酸盐酸盐 GW3965盐酸盐 Chemical Name: 2-[3-[3-[N-[2-Chloro-3-(trifluoromethyl)benzyl]-N-(2,2-diphenylethyl)amino]propoxy]phenyl]acetic acid
CAS No. 405911-09-3...
参考文献标题:Chemical cpds.
文献作者:Willson,T.M.; Collins,J.L.; Maloney,P.R.; Fivush,A.M.; Stewart,E.L.(GlaxoSmithKline plc)
参考来源:WO 0224632

Zatebradine hydrochloride, UL-FS-49

3-[3-[[2-(3,4-二甲氧基苯基)乙基]甲基氨基]丙基]-1,3,4,5-四氢-7,8-二甲氧基-2H-3-苯并氮杂-2-酮盐酸盐扎替雷定Chemical Name: 1,3,4,5-Tetrahydro-7,8-dimethoxy-3-[3-[[2-(3,4-dimethoxyphenyl)ethyl]methylimino]propyl]-2H-3-benzazepin-2-one h...
参考文献标题:Benzazepines,process for their preparation and their application as pharmaceutical preparations
文献作者:Reiffen,M.; et al.(Dr.Karl Thomae GmbH)
参考来源:DE 3119874; EP 0065229; GB 2099425; JP 57193462