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

A-304121

Chemical Name: 2(R)-Amino-1-[4-[3-[4-(cyclopropylcarbonyl)phenoxy]propyl]piperazin-1-yl]propan-1-one ; 1-[4-[3-[4-(D-Alanyl)piperazin-1-yl]propoxy]phenyl]-1-cyclopropylmethanone
CAS No. 360551-71-9...
参考文献标题:Cyclic and bicyclic diamino histamine-3 receptor antagonists
文献作者:Black,L.A.; Faghih,R.; Bennani,Y.L.; Liu,H.; Zhang,H.Q.; Dwight,W.J.; Gentles,R.G.; Phelan,K.M.; Vasudevan,A.(Abbott Laboratories Inc.)
参考来源:WO 0166534

NS-417

Chemical Name: 5-(4-Chlorophenyl)-8-methyl-2,3,6,7,8,9-hexahydro-1H-pyrrolo[3,2-h]isoquinoline-2,3-dione 3-oxime hydrochloride
CAS No. 352204-06-9, 160753-58-2 (free base)
项目整合开发状态: Biological T...
参考文献标题:AMPA antagonists and a method of treatment therewith
文献作者:W鋞jen,F.; Drejer,J.(NeuroSearch A/S)
参考来源:EP 0698025; JP 1996510221; US 5780493; US 5843945; WO 9426747

NS-1231

Chemical Name: 5-(4-Chlorophenyl)-2,3,6,7,8,9-hexahydro-1H-benzo[g]indole-2,3-dione 3-oxime
CAS No. 309711-72-6 (free base), 352204-07-0 (mono HCl salt)
项目整合开发状态: Preclinical
项目研究机构: NeuroSea...
参考文献标题:Isatine derivs.with neurotrophic activity
文献作者:Moeller,A.; Peters,D.; Groenborg,M.(NeuroSearch A/S)
参考来源:EP 1255734; US 2003040518; WO 0155110

NDBT

Chemical Name: 3-[4-(Dimethylamino)phenyltellanyl]propane-1-sulfonic acid sodium salt
CAS No. 252051-99-3
项目整合开发状态: Preclinical
项目研究机构: University of Kentucky (Originator), Uppsala University...
参考文献标题:Novel water-soluble diorganyl tellurides with thiol peroxidase and antioxidant activity
文献作者:Kanda,T.; Engman,L.; Cotgreave,I.A.; Powis,G.
参考来源:J Org Chem 2001,64(22),8161

新产品编号:607997

Chemical Name: 3-[6-Amino-8-(3-fluorophenyl)-2-[2-(1-hydroxycyclohexyl)ethynyl]-9H-purin-9-yl]benzamide hydrochloride
CAS No. 232252-56-1, 232252-55-0 (free base)
项目整合开发状态: Biological Testing 参考文献标题:Purine derivs.and adenosine A2 receptor antagonists serving as preventives/remedies for diabetes
文献作者:Asano,O.; Hoshino,Y.; Kobayashi,S.; Nagata,K.; Harada,H.; Yoshikawa,S.; Nagaoka,J.; Inoue,T.; Horizoe,T.; Yasuda,N.; Murakami,M.(Eisai Co.,Ltd.)
参考来源:EP 1054012; JP 1999263789; WO 9935147

新产品编号:245719

Chemical Name: (2R*,2'S*)-3,3'-(Ethanediyl)bis[2-(3,4-dichlorophenyl)thiazolidin-4-one]
CAS No. 192629-34-8, 162556-04-9 (deleted CAS), 192629-18-8 (diastereomer), 162556-03-8 (undefined stereochem...
参考文献标题:Synthesis and antiinflammatory,analgesic activity of 3,-3'-(1,2-ethanediyl)-bis[2-aryl-4-thiazolidinone] chiral compounds,Part 10
文献作者:Vigorita,M.G.; Ottana,R.; Monforte,F.; Maccari,R.; Trovato,A.; Monforte,M.T.; Taviano,M.F.
参考来源:Bioorg Med Chem Lett 2001,11(21),2791

新产品编号:410247

Chemical Name: N-(2,2-Dimethylcyclopentylmethyl)-4-[5-(3,3,3-trifluoropropyl)-1,2,4-oxadiazol-3-yl]benzamide isomer A
CAS No. 212380-87-5 ((-)-enantiomer), 212380-88-6 ((+)-enantiomer)
项目整合开发状态:...
参考文献标题:Benzoic acid derivs.and related cpds.as antiarrhythmic agents
文献作者:Poss,M.A.; Lloyd,J.; Rovnyak,G.C.; Caulfield,T.J.; Atwal,K.S.; Stein,P.D.; Ahmad,S.(Bristol-Myers Squibb Co.)
参考来源:WO 9837068

新产品编号:737721

Chemical Name: 6-Chloro-2-(2-hydroxybiphenyl-3-yl)-1H-indole-5-carboxamidine
CAS No. 277312-21-7
项目整合开发状态: Preclinical
项目研究机构: Celera (Originator)
合成路线:The ammonolysis of the cyano group o...
参考文献标题:Exploiting subsite S1 of trypsin-like serine proteases for selectivity: Potent and selective inhibitors of urokinase-type plasminogen activator
文献作者:Mackman,R.L.; Katz,B.A.; Breitenbucher,J.G.; Hui,H.C.; Verner,E.; Luong,C.; Liu,L.; Sprengeler,P.A.
参考来源:J Med Chem 2001,44(23),3856

CRX-395

Chemical Name: 6-[5-(7-Amino-1H-indol-2-ylcarboxamido)-1-benzofuran-2-ylcarbonyl]-8(S)-(chloromethyl)-2-methyl-4-(4-methylpiperazin-1-ylcarbonyloxy)-3,6,7,8-tetrahydrobenzo[1,2-b:4,3-b']dipyrrole-1-ca...
参考文献标题:Cytotoxic agents
文献作者:McGee,D.P.C.; Saunders,O.L.; Martichonok,V.; Wu,G.; Ng,H.P.; Li,Z.; Yarranton,G.T.(Medarex,Inc.)
参考来源:US 2003050331; WO 0296910

A-306552

Chemical Name: 1-(N,N-Dibutylcarbamoylmethyl)-4(S)-(2,3-dihydrobenzofuran-5-yl)-2(R)-(3-fluoro-4-methylphenyl)pyrrolidine-3(R)-carboxylic acid
CAS No. 380180-51-8
项目整合开发状态: Preclinical
项目研究机构...
参考文献标题:Pyrrolidine-3-carboxylic acids as endothelin antagonists.5.Highly selective potent,and orally active ETA antagonists
文献作者:Jae,H.-S.; Winn,M.; von Geldern,T.W.; Sorensen,B.K.; Chiou,W.J.; Nguyen,B.; Marsh,K.C.; Opgenorth,T.J.
参考来源:J Med Chem 2001,44(23),3978