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

TC-2557(sesquifumarate), TC-2559

3-丁烯-1-胺,4-(5-乙氧基-3-吡啶基)-N-甲基-, (3E)- Chemical Name: 4-(5-Ethoxypyridin-3-yl)-N-methyl-3(E)-buten-1-amine D-galactarate (2:1)
CAS No. 326924-19-0, 189274-78-0 (free base), 212332-35-9 (sesquifumar...
参考文献标题:[3-(5-Ethoxypyridin)yl]-alkenyl 1 amine cpds.
文献作者:Caldwell,W.S.; Dull,G.M.; Miller,C.H.
参考来源:US 5616716

DB-289

4,4'-(2,5-呋喃基)双[N-甲氧基苯甲脒]Chemical Name: 4,4'-(Furan-2,5-diyl)bis(N-methoxybenzamidine)
CAS No. 186953-56-0
项目整合开发状态: Phase II
项目研究机构: MediChem (Supplier), Georgia State University (Originato...
参考文献标题:Furan derivs.for inhibiting Pneumocystis carinii pneumonia,Giardia lamblia and Cryptosporidium parvum
文献作者:Tidwell,R.R.; Hall,J.E.; Kumar,A.; Dykstra,C.C.; Boykin,D.W.; Wilson,W.D.; Blagburn,B.L.(Auburn University; Georgia State University; University of North Carolina)
参考来源:WO 9615126

873140, GW-873140, ONO-4128, AK-602

4-[4-[[(3R)-1-丁基-3-[(R)-环己基羟基甲基]-2,5-二氧代-1,4,9-三氮杂螺[5.5]十一烷-9-基]甲基]苯氧基]苯甲酸 Chemical Name: 4-[4-[1-Butyl-3(R)-[1(R)-cyclohexyl-1-hydroxymethyl]-2,5-dioxo-1,4,9-triazaspiro[5.5]undec-9-ylmethyl]phenoxy...
参考文献标题:Triazaspiro[5.5]undecane derivs.and drugs containing the same as the active ingredient
文献作者:Shibayama,S.; Hamano,S.; Takaoka,Y.; Habashita,H.(Ono Pharmaceutical Co.,Ltd.)
参考来源:EP 1378510; WO 0274770

SM-10661(racemate), SM-12502

4-噻唑烷酮,3,5-二甲基-2-(3-吡啶基)-,盐酸盐(1:1),(2R,5S)-rel- Chemical Name: (+)-cis-(2R,5S)-3,5-Dimethyl-2-(3-pyridyl)thiazolidin-4-one hydrochloride
CAS No. 119383-00-5, 130841-70-2 (racemate)
项目整合开发状态: Ph...
参考文献标题:SM-12502
文献作者:Koike,H.; Natsume,Y.; Tojo,S.; Morooka,S.
参考来源:Drugs Fut 1995,20(2),153

ICA-17043

4-氟-A-(4-氟苯基)-A-苯基-苯甲酰胺Chemical Name: 2,2-Bis(4-fluorophenyl)-2-phenylacetamide
CAS No. 289656-45-7
项目整合开发状态: Phase II
项目研究机构: ICAgen (Orphan Drug), ICAgen (Originator), McNeil Consumer Prod...
参考文献标题:Gardos channel antagonists
文献作者:Rigdon,G.C.; McNaughton-Smith,G.A.; Stocker,J.W.(ICAgen,Inc.)
参考来源:EP 1158971; US 6288122; WO 0050026

LY-334370

4-氟-N-(3-(1-甲基哌啶-4-基)-1H-吲哚-5-基)苯甲酰胺盐酸盐 4-氟-N-[3-(1-甲基-4-哌啶基)-1H-吲哚-5-基]苯甲酰胺盐酸盐Chemical Name: 4-Fluoro-N-[3-(1-methylpiperidin-4-yl)-1H-indol-5-yl]benzamide fumarate
CAS No. 182563-09-3, 182563-08...
参考文献标题:5-Substd.-3-(1,2,3,6-tetrahydropyridin-4-yl)- and 3-(piperidin-4-yl)-1H-indoles: New 5-HT1F agonists
文献作者:Audia,J.E.; Dressman,B.A.; Droste,J.J.; Fritz,J.E.; Kaldor,S.W.; Koch,D.J.; Krushinski,J.H.Jr.; Nissen,J.S.; Rocco,V.P.; Schaus,J.M.; Thompson,D.C.(Eli Lilly and Company)
参考来源:EP 0733628; JP 1999502816; US 5708008; WO 9629075

Ameltolide, ADD-75073, LY-201116

4-氨基-N-(2,6-二甲基苯基)苯甲酰胺Chemical Name: 4-Amino-N-(2,6-dimethylphenyl)benzamide
CAS No. 787-93-9, 107293-98-1 (monoHCl)
项目整合开发状态: Phase I
项目研究机构: Lilly (Originator)
合成路线:4-Nitrobenzoylchlori...
参考文献标题:Anticonvulsant activity of some 4-aminobenzanilides
文献作者:Clark,C.R.; Sansom,R.T.; Lin,C.-M.; Norris,G.N.
参考来源:J Med Chem 1985,28(9),1259

4-ADMPP, ADD-213063

4-氨基-n-(2,6-二甲基苯基)邻苯二甲酰亚胺Chemical Name: 4-Amino-N-(2,6-dimethylphenyl)phthalimide
CAS No. 158276-70-1
项目整合开发状态: Preclinical
项目研究机构: INSERM (Originator), National Institutes of Health (Origin...
参考文献标题:Anticonvulsant activity and interactions with neuronal voltage-dependent sodium channel of analogues of ameltolide
文献作者:Vamecq,J.; Lambert,D.; Poupaert,J.H.; Masereel,B.; Stables,J.P.
参考来源:J Med Chem 1998,41(18),3307

Imidazoacridinone, Imidacrine, XLS-002, C-1311, Symadex

5-((2-(二乙基氨基)乙基)氨基)-8-羟基-6H-咪唑并[4,5,1-de]吖啶-6-酮 Chemical Name: 5-[2-(Diethylamino)ethylamino]-8-hydroxy-6H-imidazo[4,5,1-de]acridin-6-one dihydrochloride hydrate
CAS No. 138154-55-9 (anhydrous), 1...
参考文献标题:Chromophore-modified antineoplastic imidazoacridinones.Synthesis and activity against murine leukemias
文献作者:Cholody,W.M.; Martelli,S.; Konopa,J.
参考来源:J Med Chem 1992,35(2),378-82

DAMP-ES

5-(1-金刚烷基)-6-甲基嘧啶-2,4-二胺 Chemical Name: 5-(1-Adamantyl)-2,4-diamino-6-methylpyrimidine ethanesulfonate salt; 6-Methyl-5-tricyclo[3.3.1(3,7)]dec-1-yl-2,4-pyrimidinediamine ethanesulfonate (salt)
CA...
参考文献标题:DAMP-ES
文献作者:Blancafort,P.; Serradell,M.N.; Hopkins,S.J.; Castar,J.
参考来源:Drugs Fut 1983,8(4),310