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

R-102444

Chemical Name: Dodecanoic acid 5(R)-[2-[2-[2-(3-methoxyphenyl)ethyl]phenoxy]ethyl]pyrrolidin-3(R)-yl ester hydrochloride
CAS No. 191090-74-1, 191155-65-4 (free base)
项目整合开发状态: Preclinical
项目研...
参考文献标题:Phenoxyalkylamines,-pyrrolidines and -piperidines for the treatment and prevention of circulatory diseases and psychosis
文献作者:Fujimoto,K.; Tanaka,N.; Asai,F.; Ito,T.; Koike,H.(Sankyo Co.,Ltd.)
参考来源:EP 0600717; JP 1994234736; JP 1994306025; US 5556864

NPS-1408.HCl((R)-isomer), NPS-1407.HCl

Chemical Name: (-)-4,4-Bis(3-fluorophenyl)butan-2(S)-amine hydrochloride
CAS No. 186495-93-2, 170018-83-4 (free base)
项目整合开发状态: Preclinical
项目研究机构: NPS Pharmaceuticals (Originator)
合成路线:Ho...
参考文献标题:Cpds.active at a novel site on receptor-operated calcium channels useful for treatment of neurological disorders and diseases
文献作者:Moe,S.T.; Mueller,A.L.(NPS Pharmaceuticals,Inc.)
参考来源:WO 9856752

Y-39677

Chemical Name: cis-2-[2-(Octahydro-2H-isoindol-2-yl)-2-oxoethyl]-3-[4-[2-(5-methyl-2-phenyloxazol-4-yl)ethoxy]phenyl]-2(E)-propenoic acid
CAS No. 312688-85-0
项目整合开发状态: Preclinical
项目研究机构: Mit...
参考文献标题:Hybridization of non-sulfonylurea insulin secretagogue and thiazolidinedione-derived insulin sensitizer
文献作者:Kitajima,H.; Nakamura,M.; Tamakawa,H.; Goto,N.
参考来源:Bioorg Med Chem Lett 2000,10(21),2453

AZB-002

Chemical Name: 1-Methyl-2-(2-phenylethynyl)-3-(3-phenyl-2-propynyl)-3H-benzimidazol-1-ium tetrafluoroborate
CAS No. 255716-41-7, 255716-40-6 (free base)
项目整合开发状态: Preclinical
项目研究机构: Universi...
参考文献标题:Novel DNA-cleaving antitumor agents
文献作者:Kerwin,S.M.; David,W.(Research Development Foundation ; University of Texas System)
参考来源:EP 1109552; US 6297284; WO 0003709; WO 0170217

AC-165024

Chemical Name: N-Cyclooctyl-N-[1-[3-(4-fluorophenoxy)propyl]piperidin-4-yl]propanamide
CAS No. 319428-14-3
项目整合开发状态: Biological Testing
项目研究机构: ACADIA (Originator)
合成路线:The reductive alkyl...
参考文献标题:Multistep solution-phase parallel synthesis of spiperone analogues
文献作者:Hansen,H.C.; Olsson,R.; Croston,G.E.; Andersson,C.M.
参考来源:Bioorg Med Chem Lett 2000,10(21),2435

PD-189659, CI-1044

Chemical Name: N-[9-Amino-4-oxo-1-phenyl-3,4,6,7-tetrahydropyrrolo[3,2,1-jk][1,4]benzodiazepin- 3(R)-yl]pyridine-3-carboxamide
CAS No. 197894-84-1
项目整合开发状态: Preclinical
项目研究机构: Pfizer (Origin...
参考文献标题:Diazepino-indoles as phosphodiesterase IV inhibitors
文献作者:Pascal,Y.; Jacobelli,H.; Calvet,A.; Payne,A.; Dahl,S.G.(Institut de Recherche Jouveinal)
参考来源:EP 0828742; US 5972927; WO 9736905

LAS-31180

Chemical Name: N-(1-Methyl-4-oxo-1,4-dihydroquinolin-3-yl)methanesulfonamide
CAS No. 137388-43-3
项目整合开发状态: Preclinical
项目研究机构: Almirall Prodesfarma (Originator)
合成路线:The title sulfonamide ...
参考文献标题:4(1H)Quinolone derivs.
文献作者:Puig Duran,C.; Pujol Noguera,F.; Prieto Soto,J.M.; Vega Noverola,A.; Gristwood,R.W.(Almirall Prodesfarma,SA)
参考来源:EP 0445062; JP 1992506813; WO 9113061

NSC-D699127

Chemical Name: 5,5'-Bis[2-[4-[3-(dimethylaminopropoxy]phenyl]-1H-benzimidazole]
CAS No. 234429-92-6
项目整合开发状态: Preclinical
项目研究机构: Institute of Cancer Research (Originator), Queen's University...
参考文献标题:Bis-benzazoles and their use as antineoplastic agents
文献作者:Mann,J.; Neidle,S.(Institute of Cancer Research; Queen's University of Belfast; University of Reading)
参考来源:WO 0063180

21-Hydroxyepothilone D, Desoxyepothilone F, dEpoF

Chemical Name: (4S,7R,8S,9S,13Z,16S)-4,8-Dihydroxy-5,5,7,9,13-pentamethyl-16-[(E)-1-methyl-2-[2-(hydroxymethyl)-4-thiazolyl]ethenyl]-1-oxacyclohexadec-13-ene-2,6-dione
CAS No. 252981-50-3
项目整合开发...
参考文献标题:New chemical synthesis of the promising cancer chemotherapeutic agent 12,13-desoxyepothilone B: Discovery of a surprising long-range effect on the diastereoselectivity of an aldol condensation
文献作者:Harris,C.R.; et al.
参考来源:J Am Chem Soc 1999,121(30),7050

FAUC-299

Chemical Name: 2-(4-Phenylpiperazin-1-ylmethyl)-1H-indole-5-carbonitrile
CAS No. 313972-96-2
项目整合开发状态: Biological Testing
项目研究机构: Friedrich-Alexander-Universit鋞 (Originator)
合成路线:Protectio...
参考文献标题:Cyanoindole derivatives as highly selective dopamine D4 receptor partial agonists: Solid-phase synthesis,binding assays,and functional experiments
文献作者:H黚ner,H.; Kraxner,J.; Gmeiner,P.
参考来源:J Med Chem 2000,43(23),4563