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

Adaphostin, NSC-680410

金刚烷-1-基4-[(2,5-二羟基苄基)氨基]苯甲酸酯Chemical Name: 4-(2,5-Dihydroxybenzylamino)benzoic acid 1-adamantyl ester
CAS No. 241127-58-2
项目整合开发状态: Preclinical
项目研究机构: Mayo Clinic (Originator), National Canc...
参考文献标题:Disubstd.lavendustin A analogs and pharmaceutical compsns.comprising the analogs
文献作者:Narayanan,V.L.; Sausville,E.A.; Kaur,G.; Varma,R.K.(US Department of Health & Human Services)
参考来源:EP 1060160; WO 9943636

Auranofin, SK&F-39162, Ridauran, Ridaura

金诺芬Chemical Name: (2,3,4,6-Tetra-O-acetyl-1-thio-beta-D-glucopyranosato-S)(triethylphosphine)gold; (1-Thio-beta-D-glucopyranosato-S)(triethylphosphine)gold 2,3,4,6-tetraacetate
CAS No. 34031-32-8 参考文献标题:Oral gold.Antiarthritic properties of alkylphosphine gold coordinatin complexes
文献作者:Sutton,B.M.; McGusty,E.; Walz,D.T.; DiMartino ,M.J.
参考来源:J Med Chem 1972,15(11),1095-98

Motexafin gadolinium, Gadolinium texaphyrin, PCI-0120, GdT2B2, Gd-Tex, Xcytrin

钆,双(乙酰-kO)[9,10-二乙基-20,21-双[2-[2-(2-甲氧基乙氧基)乙氧基]乙氧基]-4,15-二甲基-8,11-亚胺基-3,6:16,13-二硝基-1,18-苯二氮卓二氮环固烯-5,14-二丙醇-kN1,kN18,kN23,kN24,kN25]-,水合物(1:),(PB-7-11-233'2'4)-Chemical Name: (PB-7-11-233'2'4)-Bis(ace...
参考文献标题:Texaphyrin metal complex mediated ester hydrolysis
文献作者:Sessler,J.L.; Hemmi,G.W.; Magda,D.; Miller,R.A.; Ross,K.L.; Wright,M.; Dow,W.C.; Smith,D.A.; Kr醠,V.A.; Iverson,B.; Mody,T.(University of Texas System)
参考来源:WO 9429316

Gadoversetamide, Gd-DTPA-bismethoxyethylamide, MP-1177-10, OptiMARK

钆8,11-二(羧酸甲基)-14-{2-[(2-甲氧基乙基)氨基]-2-氧代乙基}-6-氧代-2-氧杂-5,8,11,14-四氮杂十六烷-16-酸酯维塞胺 Chemical Name: [N,N-Bis[2-[(carboxymethyl)[N-(2-methoxyethyl)carbamoylmethyl]amino]ethyl]glycinato(3-)]gadolinium; [8,11-...
参考文献标题:Novel magnetic resonance imaging agents
文献作者:Periasamy,M.P.; Weber,R.W.(Mallinckrodt Medical Inc.)
参考来源:WO 9001024

Gadoxetic acid disodium salt, Gadoxate disodium, Gd-EOB-DTPA(undefined isomer), Primovist, Eovist

钆塞酸Chemical Name: Disodium [3,6,9-tris(carboxymethyl)-4(S)-(4-ethoxybenzyl)-3,6,9-triazaundecane-1,11-dioate(5-)]gadolinate(2-)
CAS No. 135326-11-3 (free acid)
项目整合开发状态: Launched-2004
项目研究机构:...
参考文献标题:Substd.complex-builders,complexes and complex salts,process for their preparation and pharmaceutical compsns.containing them
文献作者:Deutsch,J.; Gries,H.; Klieger,E.; Niedballa,U.; Renneke,F.J.; Conrad,J.; Mzel,W.(Schering AG)
参考来源:DE 3710730; WO 8807521

Gadobutrol, SH-L-562, Gadovist

钆布醇Chemical Name: [10-[(1RS,2SR)-2,3-Dihydroxy-1-(hydroxymethyl)propyl]-1,4,7,10-tetraazacyclodecane-1,4,7-triacetato(3-)]gadolinium
CAS No. 138071-82-6
项目整合开发状态: Launched-1998
项目研究机构: Scheri...
参考文献标题:1,4,7,10-Tetraazacyclododecane-butyl-triols,process for their preparation,and pharmaceutical agents containing these cpds.
文献作者:Platzek,J.; Gries,H.; Weinmann,H.-J.; Schuhmann-Giampieri,G.; Press,W.-R.(Schering AG)
参考来源:DE 4009119; EP 0448191; US 2002176823; US 6399043

Gadoteridol, Gd(HP-DO3A), Gd-HP-DO3A, SQ-32692, ProHance

钆特醇Chemical Name: (?-[10-(2-Hydroxypropyl)-1,4,7,10-tetraazacyclodecane-1,4,7-triacetato(3-)-N1,N4,N7,N10,O1,O4,O7,O10]gadolinium; (?-[10-(2-Hydroxypropyl)-1,4,7,10-tetraazacyclododecane-1,4,7-triacet...
参考文献标题:Synthesis of nonionic gadolinium chelates useful as contrast agents for magnetic resonance imaging: 1,4,7 Tris(carboxymethyl)-10-substituted-1,4,7,10-tetraazacyclodecanes and their corresponding gadolinium chelates
文献作者:Emswiler,J.E.; Gaughan,G.T.; Delaney,E.J.; Prasad,J.S.; Tweedle,M.F.; Dischino,D.D.; Srivastava,S.K.
参考来源:Inorg Chem 1991,30(6),1265-9

Gadofosveset sodium, MS-32520, MS-325, AngioMARK

钆膦维司三钠Chemical Name: Trisodium [2(R)-[(4,4-diphenylcyclohexyloxy)(hydroxy)phosphoryloxymethyl]diethylenetriaminopentaacetato(6-)]gadolinate(3-); Trisodium (SA-8-11252634)-[[4(R)-[bis[(carboxy-kappaO)m...
参考文献标题:Diagnostic imaging contrast agents with extended blood retention
文献作者:Scott,D.M.; Sajiki,H.; McMurray,T.J.; Lauffer,R.B.(Epix Medical,Inc.)
参考来源:WO 9623526

SJA-6017

钙蛋白酶抑制剂VIChemical Name: 4-Fluorophenylsulfonyl-L-valyl-L-leucinal
CAS No. 190274-53-4
项目整合开发状态: Preclinical
项目研究机构: Pfizer (Originator), Senju (Originator)
合成路线:The condensation of L-valin...
参考文献标题:Angiogenesis inhibitor
文献作者:Fukiage,C.; Azuma,M.; Inoue,J.; Nakamura,M.; Yoshida,Y.(Senju Pharmaceuticals Co.,Ltd.)
参考来源:EP 0771565; EP 0927716; EP 0928786; JP 1998147564; JP 1998147566; JP 2001233847; US 6057290; US 6214800

新产品编号:204587

铂(2+)7-氧杂二环[2.2.1]庚烷-2,3-二羧酸酯-环己烷-1,2-二胺(1:1)Chemical Name: (trans-Cyclohexane-1,2-diamine-kappaN,kappaN')(7-oxabicyclo[2.2.1]heptane-2,3-dicarboxylato(2-)-kappaO2,kappaO3)platinum
CAS No. 187819-7...
参考文献标题:Synthesis of platinum complexes and uses thereof
文献作者:Ho,Y.P.; Au-Yeung,S.C.F.; Jiang,T.; Han,X.; Wang,X.; Lin,G.; Lu,S.(Chinese University of Hong Kong)
参考来源:WO 9849174