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

FYK-1388

Chemical Name: N1-[2-(4-Guanidinophenyl)-1(S)-(N-methylcarbamoyl)ethyl]-N4-hydroxy-2(R)-isobutyl-3(S)-(3-phenylpropyl)succinamide acetate
CAS No. 184947-94-2, 184947-92-0 (diastereomer), 184947-93-...
参考文献标题:Highly water-soluble metalloproteinase inhibitor
文献作者:Fujisawa,T.; Odake,S.; Morita,Y.; Hongo,T.; Ito,H.; Yasuda,J.; Suda,E.; Igeta,K.; Morikawa,T.(Fuji Yakuhin Kogyo Co.,Ltd.)
参考来源:EP 0832875; WO 9633968

J-104870

Chemical Name: N-[3-[6-(5-Ethylthiazol-2-ylsulfanylmethyl)-4-(4-morpholinyl)pyridin-2-ylaminomethyl]-5-methoxyphenyl]carbamic acid allyl ester
CAS No. 196498-48-3
项目整合开发状态: Preclinical
项目研究机构...
参考文献标题:Aminopyridine derivs.
文献作者:Fukami,T.; Mase,T.; Tsuchiya,Y.; Kanatani,A.; Fukuroda,T.(Banyu Pharmaceutical Co.,Ltd.)
参考来源:EP 0889034; US 6011039; WO 9734873

RO-09-4746, RO-0094746

Chemical Name: N-[3-[2-(2,4-Difluorophenoxymethyl)-3-methyl-1-benzofuran-4-yloxy]propyl]-N-(pyridin-3-ylmethyl)amine
CAS No. 279229-35-5
项目整合开发状态: Preclinical
项目研究机构: Chugai (Originator)
合...
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

RO-09-4879, RO-0094879

Chemical Name: N-[3-[3-Methyl-2-(2,3,4-trifluorophenoxymethyl)-1-benzofuran-4-yloxy]propyl]-N-(pyridin-3-ylmethyl)amine
CAS No. 279229-44-6
项目整合开发状态: Preclinical
项目研究机构: Chugai (Originator) 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:589013

Chemical Name: 6-Amino-2-butyl-9-(4-fluorobenzyl)-9H-purin-8-ol
CAS No. 228107-55-9
项目整合开发状态: Preclinical
项目研究机构: Japan Energy (Originator), Sumitomo Pharmaceuticals (Originator)
合成路线:Cond...
参考文献标题:Type 2 helper T cell-selective immune response suppressors
文献作者:Matsui,H.; Takaku,H.; Isobe,Y.; Ogita,H.; Tobe,M.; Tomizawa,H.(Japan Energy Corp.)
参考来源:EP 1043021; US 6376501; WO 9932122

S-37435

Chemical Name: N-[1(R)-[N-(3-Amino-2-hydroxypropyl)carbamoyl]-2-naphthylethyl]-4-(4-oxo-2,3,4,5-tetrahydro-1,5-benzothiazepin-5-yl)butyramide hydrochloride
CAS No. 220977-91-3, 220979-20-4 ((R)-iso...
参考文献标题:Bicycle amine derivs.
文献作者:Salmon,R.; Sunley,R.L.; Godfrey,C.R.A.; Urch,C.J.; Lewis,T.; Bishop,N.D.(AstraZeneca plc)
参考来源:US 5912254; US 6066646

LY-349950

Chemical Name: N-[3-[2-(Dimethylamino)ethyl]-2-methyl-1H-indol-5-yl]-4-fluorobenzamide hydrochloride
CAS No. 189805-93-4, 189806-34-6 (free base)
项目整合开发状态: Preclinical
项目研究机构: Lilly (Originat...
参考文献标题:N-[2-Substd.-3-(2-aminoethyl)-1H-indol-5-yl]-amides: New 5-HT1F agonists
文献作者:Fritz,J.E.; Hahn,P.J.; Kaldor,S.W.; Siegel,M.G.; Xu,Y.-C.(Eli Lilly and Company)
参考来源:EP 0768301; JP 1999513666; WO 9713512

新产品编号:212497

Chemical Name: N-[4-[2(R)-[1(R)-[3,5-Bis(trifluoromethyl)phenyl]ethoxy]-3(S)-(4-fluorophenyl)morpholin-4-ylmethyl]-1H-1,2,3-triazol-5-ylmethyl]-N,N-dimethylamine hydrochloride
CAS No. 188923-01-5, ...
参考文献标题:Substd.morpholine derivs.and their use as therapeutic agents
文献作者:Baker,R.; Harrison,T.; Mcleod,A.M.; Owens,A.P.; Seward,E.M.; Swain,C.J.; Teall,M.R.(Merck Sharp & Dohme Ltd.)
参考来源:EP 0737192; EP 1099702; JP 1997507484; JP 2000219629; US 5612337; WO 9518124

AR-R25859

Chemical Name: N-[1-Azabicyclo[2.2.2]oct-3(R)-yl]-3-(2-thienyl)-2-propenamide; N-[Quinuclidin-3(R)-yl]-3-(2-thienyl)-2-propenamide
CAS No. 340682-16-8 (E-isomer)
项目整合开发状态: Biological Testing
...
参考文献标题:Identification of a series of PPARgamma/delta dual agonists via solid-phase parallel synthesis
文献作者:Liu,K.G.; Lambert,M.H.; Leesnitzer,L.M.; Oliver,W.Jr.; Ott,R.J.; Plunket,K.D.; Stuart,L.W.; Brown,P.J.; Willson,T.M.; Sternbach,D.D.
参考来源:Bioorg Med Chem Lett 2001,11(22),2959

AR-C85095MX

Chemical Name: 5-(5H-Dibenzo[a,d]cyclohepten-5-yl)-5'-O-[[(1,1-dichloro-1-phosphonomethyl)(hydroxy)phosphoryloxy](hydroxy)phosphoryl]-4-thiouridine tetrasodium salt
CAS No. 214480-01-0, 214480-70-3...
参考文献标题:Novel phosphate cpds.and their use as medicaments
文献作者:Meghani,P.; Kindon,N.; Thom,S.(AstraZeneca AB; AstraZeneca plc)
参考来源:WO 9845309