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

TER-117

Chemical Name: L-Glutamyl-S-(benzyl)-L-cysteinyl-D-phenylglycine
CAS No. 152684-53-2
项目整合开发状态: Preclinical
项目研究机构: Telik (Originator)
合成路线:D-Phenylglycine (I) was converted to ethyl ester ...
参考文献标题:Glutathione analogs and paralog panels comprising glutathione mimics
文献作者:Kauvar,L.M.; Lyttle,M.H.(Telik,Inc.)
参考来源:EP 0720620; US 5599903; WO 9508563

新产品编号:527315

Chemical Name: 1-[5-[2-[N-[4-(Acetamidosulfonyl)phenyl]carbamoyl]phenylsulfanyl]-5-oxopentyl]pyridinium bromide
CAS No. 221120-25-8
项目整合开发状态: Biological Testing
项目研究机构: Achillion (Originator)...
参考文献标题:Novel thiolesters and uses thereof
文献作者:Song,Y.; Turpin,J.A.; Huang,M.; Inman,J.K.; Walqvist,A.; Appella,E.; Maynard,A.; Rice,W.G.; Covell,D.G.(US Department of Health & Human Services)
参考来源:WO 9965871

新产品编号:147635

Chemical Name: N-(4,6-Dimethyl-1-octyl-2,3-dihydro-1H-indol-7-yl)-2,2-dimethylpropionamide hydrochloride
CAS No. 178469-58-4
项目整合开发状态: Preclinical
项目研究机构: Kyoto Pharmaceutical (Originator) 参考文献标题:Novel heterocyclic derivs.,process for producing the same,and medicinal use thereof
文献作者:Matsui,H.; Kamiya,S.; Shirahase,H.; Nakamura,S.; Wada,K.(Kyoto Pharmaceutical Industries,Ltd.)
参考来源:EP 0782986; JP 1996092210; US 5990150; WO 9609287

NNC-26-1167

Chemical Name: 1-[N-[5-Amino-5-methyl-2(E)-hexenoyl]-N-methyl-3-(2-naphthyl)-D-alanyl-N-methyl-3-(2-thienyl)-D-alanyl]-1,2,2-trimethylhydrazine
CAS No. 232614-78-7
项目整合开发状态: Preclinical
项目研究机...
参考文献标题:Growth hormone secretagogues derived from NN703 with hydrazides as c-terminal
文献作者:Ankersen,M.; Nielsen,K.K.; Hansen,T.K.; Raun,K.; Hansen,B.S.
参考来源:Eur J Med Chem 2000,35(5),487

新产品编号:761451

Chemical Name: 5,5'-[(2,6-Dichlorophenyl)methylene]bis[4-hydroxy-2-(4-morpholinyl)-6-oxo-1,6-dihydropyridine-3-carboxylic acid] diethyl ester]
CAS No. 289896-25-9
项目整合开发状态: Preclinical
项目研究机构...
参考文献标题:Synthesis and antitumor activity of 4-hydroxy-2-pyridone derivatives
文献作者:Cocco,M.T.; Congiu,C.; Onnis,V.
参考来源:Eur J Med Chem 2000,35(5),545

Y-39041

Chemical Name: N-[1-[4-[4-(2-Pyrimidinyl)-1-piperazinylmethyl]phenyl]cyclopropyl]acetamide
CAS No. 223511-88-4
项目整合开发状态: Preclinical
项目研究机构: Mitsubishi Pharma (Originator)
合成路线:Curtius rea...
参考文献标题:Piperazine cpds.and medicinal use thereof
文献作者:Adachi,K.; Moimoto,H.; Aoki,Y.; Hisadome,M.; Hanano,T.(Welfide Corporation)
参考来源:EP 1029851; WO 9919301

NVP-LAF-389, LAF-389

Chemical Name: Cyclohexanecarboxylic acid 7-oxo-6(S)-[(2R,3R,4S,5R,6E)-3,4,5-trihydroxy-2-methoxy-8,8-dimethyl-6-nonenamido]perhydroazepin-3(R)-yl ester
CAS No. 270902-51-7, 374602-77-4 (undefined ...
参考文献标题:Certain substd.caprolactams,pharmaceutical compsns.containing them and their use in treating tumors
文献作者:Bair,K.W.; Kinder,F.R.Jr.; Jagoe,C.T.(Novartis AG)
参考来源:EP 1131297; WO 0029382

新产品编号:763033

Chemical Name: 4-[4-(4-Fluorophenyl)-5-(4-pyridyl)oxazol-2-yl]-1-methylpiperidin-4-ol
CAS No. 290357-24-3
项目整合开发状态: Preclinical
项目研究机构: Novartis (Originator)
合成路线:1-(4-Fluorophenyl)-2-(4-p...
参考文献标题:SAR of 4-hydroxypiperidine and hydroxyalkyl substituted heterocycles as novel p38 MAP kinase inhibitors
文献作者:Revesz,L.; Di Padova,F.E.; Buhl,T.; Feifel,R.; Gram,H.; Hiestand,P.; Manning,U.; Zimmerlin,A.G.
参考来源:Bioorg Med Chem Lett 2000,10(11),1261

新产品编号:753541

Chemical Name: L-Tyrosyl-L-cysteinyl-1-(2-aminoethyl)cyclopentanecarbonyl-L-cysteine cyclic (2-4)-disulfide
CAS No. 288619-37-4
项目整合开发状态: Biological Testing
项目研究机构: Roche (Originator)
合成路线...
参考文献标题:The design and synthesis of potent cyclic peptide VCAM-VLA-4 antagonists incorporating an achiral Asp-Pro mimetic
文献作者:Fotouhi,N.; Joshi,P.; Fry,D.; Cook,C.; Tilley,J.W.; Kaplan,G.; Hanglow,A.; Rowan,K.; Schwinge,V.; Wolitzky,B.
参考来源:Bioorg Med Chem Lett 2000,10(11),1171

新产品编号:139725

Chemical Name: 9-Benzyl-2-chloro-6-(2-furyl)-9H-purine
CAS No. 176515-43-8
项目整合开发状态: Preclinical
项目研究机构: Universitetet i Oslo (Originator)
合成路线:2,6-Dichloropurine (I) was N-alkylated with ...
参考文献标题:9-Benzylpurines with inhibitory activity against Mycobacterium tuberculosis
文献作者:Bakkestuen,A.K.; Gundersen,L.-L.; Langli,F.; Nolsoe,J.M.J.
参考来源:Bioorg Med Chem Lett 2000,10(11),1207