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

新产品编号:427649

Chemical Name: N,N'-[1,3-Propanediylbis[(methylimino)-2,1-ethanediyl]]bis[4-methyl-11-oxo-11H-indeno[1,2-b]quinoline-6-carboxamide]
CAS No. 214637-59-9
项目整合开发状态: Preclinical
项目研究机构: La Trobe ...
参考文献标题:Topoisomerase inhibitors
文献作者:Denny,W.A.; Deady,L.W.; Kaye,A.J.(La Trobe University)
参考来源:WO 9845272

新产品编号:475109

Chemical Name: 4-Chloro-N-[2-[3-[1-(4-pyridyl)-4-piperidinylmethyl]ureido]phenyl]benzamide
CAS No. 219491-38-0
项目整合开发状态: Preclinical
项目研究机构: Lilly (Originator)
合成路线:Treatment of 4-(dimethy...
参考文献标题:Antithrombotic agents
文献作者:Sawyer,J.S.; Tinsley,J.M.; Wiley,M.R.; Hall,S.E.; Milot,G.; Shuman,R.T.; Goodson,T.Jr.; Klimkowski,V.J.; Kyle,J.A.; Masters,J.J.; Weir,L.C.; Mendel,D.; Beight,D.W.; Tebbe,A.L.; Yee,Y.K.; et al.(Eli Lilly and Company)
参考来源:WO 9900121

FI-6828K

Chemical Name: 5-[4'-[2-Butyl-4-chloro-5-(1,3-dioxolan-2-yl)-1H-imidazol-1-ylmethyl]biphenyl-2-yl]-1H-tetrazole potassium salt
CAS No. 271593-77-2, 271593-76-1 (free acid)
项目整合开发状态: Preclinical<...
参考文献标题:2-Alkyl-5-halo-3-[2'-(tetrazol-5-yl)-biphenyl-4-ylmethyl]-3H-imidazole-4-carboxaldehyde acetal derivs.,their preparation and use
文献作者:Anglada,L.; Foguet,R.; Ortiz,J.A.; Sacrist醤,A.; Castell? J.M.(Ferrer Internacional SA)
参考来源:WO 0031071

Quinlukast, VUFB-19363

Chemical Name: 4-[4-(2-Quinolinylmethoxy)phenylsulfanyl]benzoic acid
CAS No. 252972-08-0
项目整合开发状态: Preclinical
项目研究机构: Res. Inst. Pharmacy Biochemistry (VUFB) (Originator)
合成路线:Ether cleav...
参考文献标题:Derivs.of hydroxyphenylsulfanylbenzoic and hydroxyphenylsulfanylarylacetic acids
文献作者:Bucharov? V.; Jr韈kov? H.; Brunov? B.; Kuchar,M.; Jandera,A.; Panajotov? V.; Kmon韈ek,V.(Research Institute of Pharmacy and Biochemistry (VUFB))
参考来源:WO 9967208

NCX-530

Chemical Name: 2-[1-(4-Chlorobenzoyl)-5-methoxy-2-methyl-1H-indol-3-yl]acetic acid 3-(nitrooxymethyl)phenyl ester
CAS No. 204268-63-3
项目整合开发状态: Preclinical
项目研究机构: NicOx (Originator), Kyoto P...
参考文献标题:Nitric ester derivs.and their use in urinary incontinence and other diseases
文献作者:Del Soldato,P.; Sannicolo',F.(NicOx SA)
参考来源:JP 2000517332; WO 9809948

SB-414240

Chemical Name: 2-Phenyl-3-[4-(1-piperidinyl)piperidin-1-ylmethyl]-N-[1(S),2,2-trimethylpropyl]quinoline-4-carboxamide
CAS No. 272104-60-6
项目整合开发状态: Biological Testing
项目研究机构: GlaxoSmithKline ...
参考文献标题:Quinoline derivs.as NK-2 and NK-3 receptor ligands
文献作者:Giardina,G.; Grugni,M.; Raveglia,L.F.; Nadler,G.M.M.G.; Farina,C.(SmithKline Beecham SpA)
参考来源:EP 1131294; WO 0031038

CDB-4124, Progenta

Chemical Name: 17alpha-Acetoxy-11beta-[4-(dimethylamino)phenyl]-21-methoxy-19-norpregna-4,9-diene- 3,20-dione
CAS No. 198414-31-2
项目整合开发状态: Phase II
项目研究机构: National Cancer Institute (Origina...
参考文献标题:21-Substd.progesterone derivs.as new antiprogestational agents
文献作者:Kim,H.K.; Blye,R.P.; Rao,P.N.; Cessac,J.W.; Acosta,C.K.(US Department of Health & Human Services)
参考来源:JP 2000509396; WO 9741145

BBL22

Chemical Name: 9-Chloro-7-(2-fluorophenyl)-5H-pyrimido[5,4-d][2]benzazepin-2-amine
CAS No. 76988-22-2, 76988-23-3 (diHCl)
项目整合开发状态: Preclinical
项目研究机构: Bessor and Bessor Laboratories (Origina...
参考文献标题:2-Benzazepines.5.Synthesis of pyrimido[5,4-d][2] benzazepines and their evaluation as anxiolytic agents
文献作者:Trybulski,E.J.; Benjamin,L.E.Sr.; Earley,J.V.; Fryer,R.I.; Gilman,N.W.; Reeder,E.; Walser,A.; Davidson,A.B.; Horst,W.D.; Sepinwall,J.; et al.
参考来源:J Med Chem 1983,26(11),1589

PNU-142796

Chemical Name: N-(4-Chlorobenzyl)-8-hydroxyquinoline-7-carboxamide
CAS No. 205037-64-5
项目整合开发状态: Biological Testing
项目研究机构: Pfizer (Originator)
合成路线:Treatment of 8-Hydroxyquinoline (I) wit...
参考文献标题:8-Hydroxy-7-substd.quinolines as anti-viral agents
文献作者:Vaillancourt,V.A.; Romines,K.R.; Romero,A.G.; Tucker,J.A.; Strohbach,J.W.; Bezencon,O.; Thaisrivongs,S.(Pharmacia & Upjohn AB)
参考来源:EP 0927164; WO 9811073

新产品编号:316909

Chemical Name: (?-trans-7-Benzyl-3-[2-methoxy-5-[5-(trifluoromethyl)-1H-tetrazol-1-yl]phenyl]-1-oxa-7-azaspiro[4.5]decane
CAS No. 202389-71-7, 202390-24-7 (cis-isomer, monoHCl salt), 202390-00-9 (m...
参考文献标题:Spiro-piperidine derivs.and their use as therapeutic agents
文献作者:Curtis,N.R.; Huscroft,I.T.; Kulagowski,J.J.; Swain,C.J.(Merck Sharp & Dohme Ltd.)
参考来源:EP 0912579; US 6071928; WO 9801450