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

Argyrin B, A-21459-B

Chemical Name: (4S,7S,13R,22R)-13-Ethyl-4-(1H-indol-3-ylmethyl)-7-(4-methoxy-1H-indol-3-ylmethyl)-18,22-dimethyl-16-methylene-24-thia-3,6,9,12,15,18,21,26-octaazabicyclo[21.2.1]hexacosa-1(25),23(26)-d...
参考文献标题:Total synthesis of the cyclic heptapeptide argyrin B: A new potent inhibitor of T-cell independent antibody formation
文献作者:Ley,S.V.; Priour,A.; Heusser,C.
参考来源:Org Lett 2002,4(5),711

YM-47813

Chemical Name: 4-Amino-5-chloro-N-[2-[1-(dimethylamino)cyclohexyl]ethyl]-2-methoxybenzamide
CAS No. 178241-68-4
项目整合开发状态: Preclinical
项目研究机构: Yamanouchi (Originator)
合成路线:The intermediate ...
参考文献标题:Novel 5-hydroxytryptamine 4 (5-HT4) receptor agonists.Synthesis and gastroprokinetic activity of 4-amino-N-[2-(1-aminocycloalkan-1-yl)ethyl]-5-chloro-2-methoxybenzamides
文献作者:Suzuki,T.; Imanishi,N.; Itahana,H.; Watanuki,S.; Miyata,K.; Ohta,M.; Nakahara,H.; Yamagiwa,Y.; Mase,T.
参考来源:Chem Pharm Bull 1998,46(7),1116

SNAP-5399

Chemical Name: 2-(2-Aminoethoxymethyl)-N3-[3-(4,4-diphenylpiperidin-1-yl)propyl]-6-ethyl-4-(4-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxamide
CAS No. 166807-77-8, 166810-98-6 ((-)-enantiomer), 1...
参考文献标题:Design and synthesis of novel dihydropyridine alpha-1A antagonists
文献作者:Hong,X.; Marzbadi,M.R.; Nagarathnam,D.; Miao,S.W.; Chiu,G.; Wong,W.C.; Wetzel,J.M.; Fang,J.; Forray,C.; Chen,T.B.; O'Malley,S.S.; Chang,R.S.; Gluchowski,C.
参考来源:Bioorg Med Chem Lett 1999,9(19),2843

NU-3076

Chemical Name: 2,2',2'',2'''-[4,8-Bis(4-methoxybenzylamino)pyrimido[5,4-d]pyrimidine-2,6-diyl]bis(nitrilo)tetrakis(ethanol); 2,6-Bis[N,N-bis(2-hydroxyethyl)amino]-4,8-bis(4-methoxybenzylamino)pyrimido...
参考文献标题:Pyrimidopyrimidine cpds.
文献作者:Calvert,A.H.; Griffin,R.J.; Curtin,N.J.; Golding,B.T.; Newell,D.R.(University of Newcastle upon Tyne)
参考来源:WO 9843974

TS-951

Chemical Name: endo-N-[8-(3-Hydroxypropyl)-8-azabicyclo[3.2.1]oct-3-yl]-1-isopropyl-2-oxo-1,2-dihydroquinoline-3-carboxamide
CAS No. 174486-39-6
项目整合开发状态: Preclinical
项目研究机构: Taisho (Originat...
参考文献标题:Quinolinecarboxylic acid deriv.
文献作者:Ohuchi,Y.; Suzuki,M.; Asanuma,H.; Yokomori,S.; Hatayama,K.(Taisho Pharmaceutical Co.,Ltd.)
参考来源:EP 0710662; JP 1996034784; US 5753673; WO 9531455

YM-49244

Chemical Name: 1'-[2-[3-(3,4-Dichlorophenyl)-1-[2-[3-(isopropoxy)phenyl]acetyl]piperidin-3-yl]ethyl]-1'-methyl-3-oxospiro[1,2,3,4-tetrahydroisoquinoline-1,4'-piperidinium] iodide
CAS No. 173941-19-...
参考文献标题:Synthesis and NK1 receptor antagonistic activity of (?-1-acyl-3-(3,4-dichlorophenyl)-3-[2-(spiro-substituted piperidin-1'-yl)ethyl]piperidines
文献作者:Kubota,H.; Okamoto,Y.; Fujii,M.; Ikeda,K.; Takeuchi,M.; Shibanuma,T.; Isomura,Y.
参考来源:Bioorg Med Chem Lett 1998,8(12),1541

GS-2888

Chemical Name: Nomega-(tert-Butoxycarbonyl)-L-arginyl-glycine ditetradecylamide dihydrochloride
CAS No. 175969-22-9
项目整合开发状态: Biological Testing
项目研究机构: Gilead (Originator), GlaxoSmithKline (...
参考文献标题:Cationic lipids for delivery of nucleic acids to cells
文献作者:Deprince,R.B.; Facchine,K.L.; Lewis,G.S.; Lewis,J.G.; Lin,K.-Y.; Matteucci,M.D.; Mook,R.A.Jr.; Wagner,R.W.(Gilead Sciences Inc.; Glaxo Wellcome plc)
参考来源:WO 9601841

TBC-11241

Chemical Name: 3-[N-(4-Chloro-3-methylisoxazol-5-yl)sulfamoyl]-N-(6-cyano-1,3-benzodioxol-5-yl)thiophene-2-carboxamide
CAS No. 184036-18-8
项目整合开发状态: Preclinical
项目研究机构: Encysive Pharmaceutica...
参考文献标题:Thienyl-,furyl-,pyrrolyl- and biphenylsulfonamides and derivs.thereof that modulate the activity of endothelin
文献作者:Chan,M.F.; Raju,B.G.; Kois,A.; Verner,E.J.; Wu,C.; Castillo,R.S.; Yalamoori,V.; Balaji,V.N.(Texas Biotechnology Corp.)
参考来源:EP 0819125; JP 1999507015; WO 9631492

Timcodar dimesilate, VX-853

Chemical Name: N1-Benzyl-4-chloro-N2-methyl-N2-[2-oxo-2-(3,4,5-trimethoxyphenyl)acetyl]-N1-[3-(4-pyridyl)-1-[2-(4-pyridyl)ethyl]propyl]-L-phenylalaninamide dimethanesulfonate
CAS No. 183313-30-6, 1...
参考文献标题:Novel amino acid derivs.with improved multi-drug resistance activity
文献作者:Zelle,R.E.; Harding,M.W.(Vertex Pharmaceuticals Inc.)
参考来源:EP 0797567; JP 1998509151; US 5543423; WO 9615101

SC-078

Chemical Name: 2-(2-Chlorophenyl)-4-(4-fluorophenyl)-5-[4-(methylsulfonyl)phenyl]thiazole
CAS No. 177560-23-5
项目整合开发状态: Preclinical
项目研究机构: Pfizer (Originator)
合成路线:The condensation of 4-(...
参考文献标题:Substd.thiazoles for the treatment of inflammation
文献作者:Talley,J.J.; Carter,J.S.; Collins,P.W.; Kramer,S.W.; Penning,T.D.; Rogier,D.J.Jr.; Rogers,R.S.(Pharmacia Corp.)
参考来源:EP 0772606; JP 1998504542; US 5668161; WO 9603392