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

SRI-7055

Chemical Name: 1-(3-Methoxybenzyloxy)adenosine perchlorate
CAS No. 141776-54-7, 123404-14-8 (free base)
项目整合开发状态: Preclinical
项目研究机构: Southern Research Institute (Originator), US Army Med. Re...
参考文献标题:Adenosine cpds.useful in the prevention and treatment of vaccinia virus infections
文献作者:Montgomery,J.A.; Secrist,J.A.III; Krauth,C.A.(Southern Research Institute)
参考来源:US 5102873

Perzinfotel, WAY-126090, EAA-090

Chemical Name: 2-[8,9-Dioxo-2,6-diazabicyclo[5.2.0]non-1(7)-en-2-yl]ethylphosphonic acid
CAS No. 144912-63-0
项目整合开发状态: Phase II
项目研究机构: Wyeth Pharmaceuticals (Originator)
合成路线:Combining (3...
参考文献标题:[[(2-Amino-3,4-dioxo-1-cyclo-buten-1-yl)amino]alkyl]-acid derivs.
文献作者:Kinney,W.A.; Garrison,D.C.(Wyeth)
参考来源:EP 0496561; JP 1992321654; US 5168103

L-692429

Chemical Name: 3-Amino-3-methyl-N-[2-oxo-1-[2'-(1H-tetrazol-5-yl)biphenyl-4-ylmethyl]-2,3,4,5-tetrahydro-1H-1-benzazepin-3(R)-yl]butyramide
CAS No. 145455-23-8, 145457-42-7 (HCl), 145455-80-7 (mono...
参考文献标题:Benzo-fused lactams promote release of growth hormone
文献作者:Fisher,M.H.; Wyvratt,M.J.; Schoen,W.R.; DeVita,R.J.(Merck & Co.,Inc.)
参考来源:EP 0513974; JP 1994172316; US 5206235; WO 9216524

S-9788

Chemical Name: 6-[4-[2,2-Bis(4-fluorophenyl)ethylamino]piperidin-1-yl]-N,N'-diallyl-1,3,5-triazine-2,4-diamine bismethanesulfonate
CAS No. 140945-01-3 (free base)
项目整合开发状态: Phase II
项目研究机构: S...
参考文献标题:New triazine derivatives as potent modulators of multidrug resistance
文献作者:Dhainaut,A.; R間nier,G.; Atassi,G.; Pierr? A.; L閛nce,S.; Kraus-Berthier,L.; Prost,J.F.
参考来源:J Med Chem 1992,35(13),2481-96

SW-33377, SR-233377, Win-33377

Chemical Name: N-[1-[2-(Diethylamino)ethylamino]-9-oxothioxanthen-4-ylmethyl]methanesulfonamide; 1-[2-(Diethylamino)ethylamino]-4-(methanesulfonamidomethyl)thioxanthen-9-one
CAS No. 146537-07-7
...
参考文献标题:Anti-solid tumor efficacy and preparation of N-[[1-[[2-(diethylamino)ethyl]amino]-9-oxo-9H-thioxanthen-4-yl]methyl]methanesulfonamide (WIN 33377) and related derivatives
文献作者:Wentland,M.P.; et al.
参考来源:Bioorg Med Chem Lett 1994,4(4),609

E-5531

Chemical Name: 2-Deoxy-6-O-[2-deoxy-3-O-[3(R)-[5(Z)-dodecenoyloxy]decyl]-6-O-methyl-2-(3-oxotetradecanamido)-4-O-phosphono-beta-D-glucopyranosyl]-3-O-[3(R)-hydroxydecyl]-2-(3-oxotetradecanamido)-alpha...
参考文献标题:Anti-endotoxin cpds.
文献作者:Christ,W.J.; Kawata,T.; Hawkins,L.D.; Kobayashi,S.; Asano,O.; Rossignol,D.P.(Eisai Co.,Ltd.)
参考来源:EP 0536969; JP 1993194470; US 5530113

PD-137966

Chemical Name: (Z)-5-[2-(2,6-Dichloro-3-methylphenylamino)benzylidene]-2-thiooxathiazolidin-4-one
CAS No. 144987-93-9, 149703-32-2 (undefined isomer)
项目整合开发状态: Biological Testing
项目研究机构: Pfiz...
参考文献标题:2-Substd.thiazolidinone,oxazolidinone,and imidazolidinone derivs.of fenamates as antiinflammatory agents
文献作者:Belliotti,T.R.; Boschelli,D.H.; Connor,D.T.; Kostlan,C.R.(Pfizer Inc.)
参考来源:US 5143929

SC-52491

Chemical Name: 4-Amino-N-[1-azatricyclo[3.3.1.0(3,7)]nonan-4(R)-yl]-5-chloro-2-methoxybenzamide
CAS No. 139228-16-3 (stereoisomer), 139344-03-9 (stereoisomer, monoHCl)
项目整合开发状态: Preclinical
项...
参考文献标题:Enantioselective synthesis of dual 5-HT4/5-HT3 serotonergic azanoradamantane SC-52491
文献作者:Becker,D.P.; et al.
参考来源:Tetrahedron 1999,55(40),11787

A-5021

Chemical Name: (-)-9-[1(S),2(R)-Bis(hydroxymethyl)cyclopropan-1-ylmethyl]guanine
CAS No. 145512-85-2, 144985-39-7 (cis-isomer, racemic), 144985-37-5 (trans-isomer, racemic)
项目整合开发状态: Phase I
...
参考文献标题:Cyclopropane deriv.
文献作者:Hatsuya,S.; Sekiyama,T.; Tsuji,T.; Iwayama,S.; Okunishi,M.(Ajinomoto Co.,Inc.)
参考来源:EP 0502690; JP 1993194421; US 5342840; US 5449840

LY-191704

Chemical Name: trans-(?-8-Chloro-4-methyl-1,2,3,4,4a,5,6,10b-octahydrobenzo[f]quinolin-3-one
CAS No. 146117-78-4
项目整合开发状态: Preclinical
项目研究机构: Lilly (Originator)
合成路线:6-Chloro-2-tetralone ...
参考文献标题:Nonsteroidal inhibitors of human type I steroid 5alpha-reductase
文献作者:Jones,C.D.; Audia,J.E.; Lawhorn,D.E.; McQuaid,L.A.; Neubauer,B.L.; Pike,A.J.; Pennington,P.A.; Stamm,N.B.; Toomey,R.E.; Hirsch,K.S.
参考来源:J Med Chem 1993,36(3),421-3