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

VIPGC-NO

Chemical Name: Histidyl-seryl-aspartyl-alanyl-valyl-phenylalanyl-threonyl-aspartyl-asparaginyl-tyrosyl-threonyl-arginyl-leucyl-arginyl-lysyl-glutaminyl-methionyl-alanyl-valyl-lysyl-lysyl-tyrosyl-leucy...
参考文献标题:Nitrosylated neuropeptides
文献作者:Stamler,J.; Saenz De Tejada,I.(Boston University; Brigham & Women's Hospital)
参考来源:EP 0822826; JP 1999504008; WO 9632954

CGS-31398

Chemical Name: N-(Butylsulfonyl)-1-[3-[4-(1-pyrrolyl)phenyl]-2(R)-(N,3,5-trimethylbenzamido)propionamido]cyclopropane-1-carboxamide; N1-[1-[N-(Butylsulfonyl)carbamoyl]cyclopropyl]-N2-(3,5-dimethylbenz...
参考文献标题:N-aroylamino acid amides as endothelin inhibitors
文献作者:Ksander,G.M.; Kukkola,P.J.; Robinson,L.A.(Novartis AG)
参考来源:EP 0821670; JP 1999505522; WO 9633170

新产品编号:152381

Chemical Name: N-[2(S)-[2-[1-(4-Cyanobenzyl)-1H-imidazol-5-yl]acetamido]-3(S)-methylpentyl]-N-(1-naphthylmethyl)glycyl-L-methionine
CAS No. 179025-19-5, 179025-20-8 (trifluoroacetate)
项目整合开发状态: ...
参考文献标题:Thio-free inhibitors of farnesyl-protein transferase
文献作者:Anthony,N.J.; Desolms,S.J.; Gomez,R.P.; Graham,S.L.; Hutchinson,J.H.; Stokker,G.E.(Merck & Co.,Inc.)
参考来源:JP 1998508005; US 5652257; WO 9610034

新产品编号:153963

Chemical Name: N-[2(S)-[2-[1-(4-Cyanobenzyl)-1H-imidazol-5-yl]acetamido]-3(S)-methylpentyl]-N-(1-naphthylmethyl)glycyl-L-methionine methyl ester
CAS No. 179026-12-1, 179026-13-2 (trifluoroacetate)<...
参考文献标题:Thio-free inhibitors of farnesyl-protein transferase
文献作者:Anthony,N.J.; Desolms,S.J.; Gomez,R.P.; Graham,S.L.; Hutchinson,J.H.; Stokker,G.E.(Merck & Co.,Inc.)
参考来源:JP 1998508005; US 5652257; WO 9610034

Sparoxomycin A1

Chemical Name: N-[1(S)-(Hydroxymethyl)-2-[(RS)-[[(SS)-methylsulfinyl]methyl]sulfinyl]ethyl]-3-(6-methyl-2,4-dioxo-1,2,3,4-tetrahydropyrimidin-5-yl)-2(E)-propenamide
CAS No. 174390-01-3
项目整合开发状态:...
参考文献标题:Synthesis and morphological reversion activity on src(ts)NRK cells of pyrimidinylpropanamide antibiotics,sparsomycin,sparoxomycin A1,A2,and their analogues
文献作者:Nakajima,N.; Enomoto,T.; Matsuura,N.; Ubukata,M.
参考来源:Bioorg Med Chem Lett 1998,8(23),3331

Sparoxomycin A2

Chemical Name: N-[1(S)-(Hydroxymethyl)-2-[(RS)-[[(RS)-methylsulfinyl]methyl]sulfinyl]ethyl]-3-(6-methyl-2,4-dioxo-1,2,3,4-tetrahydropyrimidin-5-yl)-2(E)-propenamide
CAS No. 174390-02-4
项目整合开发状态:...
参考文献标题:Synthesis and morphological reversion activity on src(ts)NRK cells of pyrimidinylpropanamide antibiotics,sparsomycin,sparoxomycin A1,A2,and their analogues
文献作者:Nakajima,N.; Enomoto,T.; Matsuura,N.; Ubukata,M.
参考来源:Bioorg Med Chem Lett 1998,8(23),3331

R-102557

Chemical Name: (2R,3R)-2-(2,4-Difluorophenyl)-3-[trans-2-[4-[4-(2,2,3,3-tetrafluoropropoxy)phenyl]buta-1(E),3(E)-dienyl]-1,3-dioxan-5-ylsulfanyl]-1-(1,2,4-triazol-1-yl)-2-butanol
CAS No. 183800-35-...
参考文献标题:Triazole antifungal agent
文献作者:Oida,S.; Tanaka,T.; Tajima,Y.; Konosu,T.; Somada,A.; Miyaoka,T.; Yasuda,H.(Sankyo Co.,Ltd.)
参考来源:EP 0841327; JP 1996333350; US 5977152; WO 9631491

WS-9885B, FR-182877

Chemical Name: (3R,4S,6R,6aS,7aS,9aS,10S,11S,12R,12aS,12bS,12cR)-10,12-Dihydroxy-4,6,8,11-tetramethyl-4,6,6a,7,7a,9a,10,11,12,12a,12b,12c-dodecahydro-1H,3H-3,6-etheno-as-indaceno[1,2-d]pyrano[4,3-b]py...
参考文献标题:A cascade cycloaddition strategy leading to the total synthesis of (-)-FR182877
文献作者:Evans,D.A.; Starr,J.T.
参考来源:Angew Chem.Int Ed Engl 2002,41(10),1787

RS-100329

Chemical Name: 5-Methyl-3-[3-[4-[2-(2,2,2-trifluoroethoxy)phenyl]piperazin-1-yl]propyl]pyrimidine-2,4(1H,3H)-dione hydrochloride
CAS No. 186386-15-2 (as dihydrochloride)
项目整合开发状态: Preclinical 参考文献标题:Pyrimidinedione,pyrimidinetrione,triazinedione,tetrahydroquinazolinedione derivs.as alpha1-adrenergic receptor antagonists
文献作者:Bantle,G.W.; Elworthy,T.R.; Guzman,A.; Jaime-Figueroa,S.; Lopez-Tapia,F.J.; Morgans,D.J.Jr.; Perez-Medrano,A.; Pfister,J.R.; Sjogren,E.B.; Talamas,F.X.(F.Hoffmann-La Roche AG)
参考来源:EP 0748800; JP 1997100269

FK-355

Chemical Name: 2-[4-[3,5-Bis(trifluoromethyl)benzoyl]-3(R)-(1H-indol-3-ylmethyl)piperazin-1-yl]-N-(4-methylpiperazin-1-yl)acetamide fumarate
CAS No. 185749-87-5, 185749-84-2 (free base)
项目整合开发状态...
参考文献标题:1-Benzoyl-2-(indolyl-3-alkyl)-piperazine derivs.as neurokinin receptor antagonists
文献作者:Matsuo,M.; Hagiwara,D.; Manabe,T.; Konishi,N.; Shigenaga,S.; Murano,K.; Matsuda,H.; Miyake,H.(Fujisawa Pharmaceutical Co.,Ltd.)
参考来源:EP 0846116; JP 1999505830; WO 9637489