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:329565

Chemical Name: 5-Phenyl-2-[4-(pyridin-4-ylcarbonyl)phenylsulfonylmethyl]pentanohydroxamic acid hydrochloride
CAS No. 203248-89-9
项目整合开发状态: Preclinical
项目研究机构: Celltech (Originator)
合成路线:Al...
参考文献标题:Hydroxamic and carboxylic acid derivs.having MMP and TNF inhibitory activity
文献作者:Owen,D.A.; Montana,J.G.; Keily,J.F.; Watson,R.J.; Baxter,A.D.(Celltech Group plc)
参考来源:EP 0968182; JP 2000517297; WO 9805635

Tel-01

Chemical Name: 2,9-Bis[3-(4-morpholinyl)propyl]anthra[2,1,9-def:6,5,10-d'e'f']diisoquinoline-1,3,8,10(2H,9H)-tetrone
CAS No. 154355-15-4
项目整合开发状态: Biological Testing
项目研究机构: University of Tex...
参考文献标题:Inhibition of human telomerase by a G-quadruplex-interaction cpd.
文献作者:Salazar,M.; Kerwin,S.M.; Hurley,L.H.; Fedoroff,O.Y.(University of Texas System)
参考来源:US 6156763; WO 9940087

SU-058(uncomplexed), RP-698

Chemical Name: [N-[2-[4,7,10-Tris(carboxylatomethyl)-1,4,7,10-tetraazacyclododecan-1-yl]acetyl]-L-glutamyl-N1-[3-[7-[N-(1H-benzimidazol-2-ylmethyl)-N-methylcarbamoyl]-2(S)-(carboxymethyl)-3-oxo-2,3,4,...
参考文献标题:Vitronectin receptor antagonist pharmaceuticals
文献作者:Sworin,M.; Cheesman,E.H.; Rajopadhyem,M.(DuPont Pharmaceuticals Co.)
参考来源:EP 1140864; WO 0035887

TA-103(ligand), RP-728

Chemical Name: [N-[2-[4,7,10-Tris(carboxylatomethyl)-1,4,7,10-tetraazacyclododecan-1-yl]acetyl]-L-glutamyl-N1-[2-[4-[N-[4-[1(S)-carboxy-2-[1-[3-(1H-imidazol-2-ylamino)propyl]-1H-indazol-5-ylcarboxamid...
参考文献标题:Vitronectin receptor antagonist pharmaceuticals
文献作者:Rajopadhye,M.; Harris,T.D.; Cheesman,E.H.(DuPont Pharmaceuticals Co.)
参考来源:WO 0035488

新产品编号:582685

Chemical Name: 2-[4-(3'-Ethoxy-2-methylbiphenyl-4-yl)-1,2,3,6-tetrahydropyridin-1-ylsulfonyl]acetohydroxamic acid; 2-[4-(3'-Ethoxy-2-methylbiphenyl-4-yl)-1,2,3,6-tetrahydropyridin-1-ylsulfonyl]-N-hydr...
参考文献标题:Hydroxamic acid derivs.as matrix metalloprotease (MMP) inhibitors
文献作者:Whitlock,G.A.; Dack,K.N.(Pfizer Inc.)
参考来源:EP 1036062; JP 2001525396; WO 9929667

新产品编号:593759

Chemical Name: N-(3-tert-Butyl-1-methyl-1H-pyrazol-5-yl)-N'-[4-(pyridin-4-ylmethyl)phenyl]urea
CAS No. 229002-15-7
项目整合开发状态: Preclinical
项目研究机构: Bayer (Originator)
合成路线:In a related proced...
参考文献标题:Inhibition of p38 kinase activity using substd.heterocyclic ureas
文献作者:Riedl,B.; Lee,W.; Lowinger,T.B.; Redman,A.; Smith,R.A.; Khire,U.; Dumas,J.; Scott,W.J.; Wood,J.E.; Johnson,J.; Paulsen,H.; Hatoum-Mokdad,H.(Bayer Corp.)
参考来源:WO 9932111

Ro-09-4609

Chemical Name: 3-Methyl-4-[3-(pyridin-3-ylmethylamino)propoxy]-1-benzofuran-2-carboxylic acid ethyl ester
CAS No. 279230-20-5
项目整合开发状态: Preclinical
项目研究机构: Roche (Originator)
合成路线:Lithiati...
参考文献标题:Novel bicyclic cpds.
文献作者:Fujii,T.; Tsujii,S.; Liu,P.; Ohtsuka,T.; Ebiike,H.; Masubuchi,M.; Aoki,Y.; Kawasaki,K.(F.Hoffmann-La Roche AG)
参考来源:US 6376491; WO 0037464

新产品编号:789927

Chemical Name: trans-3-[4-[6-Methoxy-1,2,3,4-tetrahydroisoquinolin-2-yl]cyclohexyl]-1H-indole- 5-carbonitrile
CAS No. 302916-78-5
项目整合开发状态: Biological Testing
项目研究机构: Wyeth Pharmaceuticals (O...
参考文献标题:Tetrahydroisoquinolinyl-indole derivs.for the treatment of depression
文献作者:Meagher,K.L.; Mewshaw,R.E.(American Home Products Corp.)
参考来源:WO 0064886

SP-500263

Chemical Name: 7-Hydroxy-3-phenyl-4-[4-[2-(1-piperidinyl)ethoxy]benzyl]-2H-1-benzopyran-2-one hydrochloride
CAS No. 280137-80-6 (free base)
项目整合开发状态: Preclinical
项目研究机构: Signal (Originator) 参考文献标题:Cpds.and methods for modulation of estrogen receptors
文献作者:Bhagwat,S.S.; McKie,J.A.; Khammungkhune,S.(Signal Pharmaceuticals,Inc.)
参考来源:WO 0149673

新产品编号:570029

Chemical Name: 2-[3-(4-Chlorophenyl)-2-propenyl]-5,6-bis(4-methoxyphenyl)pyridazin-3(2H)-one
CAS No. 225666-41-1
项目整合开发状态: Preclinical
项目研究机构: Kowa (Originator)
合成路线:Glyoxylic acid (II),ge...
参考文献标题:Novel pyridazine derivs.and drugs containing the same as the active ingredient
文献作者:Yoshizaki,H.; Habata,Y.; Kumai,N.; Kotaki,K.; Ohkuchi,M.; Ohgiya,T.; Yamazaki,Y.; Matsuda,T.; Kitamura,T.; Koshi,T.; Kyotani,Y.; Shigyo,H.(Kowa Co.,Ltd.)
参考来源:EP 1043317; JP 1999152274; JP 2000198776; US 6348468; WO 9925697