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

Epoxomicin, BU-4061T

环氧酶素Chemical Name: 2-[Acetyl-(N-methyl)isoleucyl-isoleucyl-threonyl-leucyl]-2(R)-methyloxyrane
CAS No. 134381-21-8
项目整合开发状态: Preclinical
项目研究机构: Bristol-Myers Squibb (Originator), Yale Univer...
参考文献标题:Total synthesis of the potent proteasome inhibitor epoxomicin: A useful tool for understanding proteasome biology
文献作者:Sin,N.; Kim,K.B.; Elofsson,M.; Meng,L.; Auth,H.; Kwok,B.H.; Crews,C.M.
参考来源:Bioorg Med Chem Lett 1999,9(15),2283

Ciclotizolam, WE-973

环氯唑仑Chemical Name: 2-Bromo-4-(2-chlorophenyl)-9-cyclohexyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepine
CAS No. 58765-21-2
项目整合开发状态: Biological Testing
项目研究机构:
合成路线:The reaction o...
参考文献标题:Substd.6-aryl-4H-s-triazolo-[3,4c]-thieno-[2,3e]-1,4-diazepines and acid addition salts thereof
文献作者:Weber,K.-H.; Kuhn,F.J.; Bauer,A.; Danneberg,P.(Boehringer Ingelheim Pharma GmbH & Co.KG)
参考来源:DE 2410030; GB 1490269

Ciclesonide, BTR-15, B-9207-015, BY-9010, Alvesco

环索奈德环索奈德 Chemical Name: (R)-11beta,16alpha,17,21-Tetrahydroxypregna-1,4-diene-3,20-dione cyclic 16,17-acetal with cyclohexanecarboxaldehyde, 21-isobutyrate; 16alpha,17alpha-[(R)-Cyclohexylmethylenedi...
参考文献标题:Acetals and esters of 16alpha-hydroxyprednisolone and fluocinolone
文献作者:Calatayud,J.; Conde,J.R.; Luna,M.(Byk Elmu SA)
参考来源:BE 1005876; CH 683343; DE 4129535; ES 2034893; FR 2666585; GB 2247680; JP 1992257599; US 5482934

Butoctamide hemisuccinate, Listomin

琥珀酸氢布酰胺Chemical Name: N-(2-Ethylhexyl)-3-hydroxybutyramide hydrogen succinate; N-2-Ethylhexyl-beta-hydroxybutyramide hydrogen succinate; N-(2-Ethylhexyl)-3-hydroxybutanamide hydrogen succinate
CAS ...
参考文献标题:N-Substd.-beta-oxybutyramide semisuccinate and its salt having effects of increasing paradoxical sleep and tranquillizing
文献作者:Yamagisawa,I.; Torii,S.; Sakuma,A.(Lion Corp.)
参考来源:DE 1768445; US 3639457

Vatalanib succinate, PTK/ZK, CGP-79787D, CGP-79787(free base), ZK-222584, PTK-787

琥珀酸瓦他拉尼瓦他拉尼伐拉尼布Chemical Name: N-(4-Chlorophenyl)-4-(pyridin-4-ylmethyl)phthalazin-1-amine succinate
CAS No. 212142-18-2, 212141-51-0 (diHCl), 212141-54-3 (free base), 212141-89-4 (fumarate), 2121...
参考文献标题:Phthalazines with angiogenesis inhibiting activity
文献作者:Altmann,K.-H.; Mett,H.; Wood,J.; Stover,D.R.; Frei,J.; Bold,G.; Traxler,P.(Novartis AG)
参考来源:EP 0970070; WO 9835958

Solifenacin succinate, YM-53705(monoHCl), YM-905, Vesicare

琥珀酸索利那新 2(1H)-异喹啉羧酸,3,4-二氢-1-苯基,(3R)-1-氮环[2.2.2],酸盐-3-基酯,盐酸盐(1:1),(1R)- Chemical Name: 1(S)-Phenyl-1,2,3,4-tetrahydroisoquinoline-2-carboxylic acid 3(R)-quinuclidinyl ester monosuccinate
CAS No. 24...
参考文献标题:Novel quinuclidine derivs.and medicinal compsn.thereof
文献作者:Takeuchi,M.; Naito,R.; Hayakawa,M.; Okamoto,Y.; Yonetoku,Y.; Ikeda,K.; Isomura,Y.(Yamanouchi Pharmaceutical Co.,Ltd.)
参考来源:EP 0801067; US 6017927; WO 9620194

Cifenline succinate, Cibenzoline succinate, UP-33901(free base), Ro-227796(free base), Exacor, Cibenol, Cipralan

琥珀酸西苯唑啉琥珀酸西苯唑啉西苯唑啉Chemical Name: 2-(2,2-Diphenylcyclopropyl)-4,5-dihydro-1H-imidazole succinate
CAS No. 100678-32-8, 57625-97-5 (butanedioate (2:1)), 53267-01-9 (free base)
项目整合开发状态: Launched...
参考文献标题:Cibenzoline
文献作者:Neuman,M.; Blancafort,P.; Castar,J.; Serradell,M.N.
参考来源:Drugs Fut 1982,7(4),239

Regadenoson, CVT-3146

瑞加德松Chemical Name: 2-[4-(N-Methylcarbamoyl)-1H-pyrazol-4-yl)adenosine; 6-Amino-2-[4-(methylcarbamoyl)-1H-pyrazol-1-yl]purine-9-yl-beta-D-ribofuranoside
CAS No. 313348-27-5
项目整合开发状态: Phase III 参考文献标题:N-Pyrazole A2A receptor agonists
文献作者:Zablocki,J.A.; Palle,V.P.; Elzein,E.O.(CV Therapeutics,Inc.)
参考来源:EP 1189916; US 6403567; WO 0078779

Recainam, Wy-42362

瑞卡南尿素,N-(2,6-二甲基苯基)-N'-[3-[(1-甲基)氨基]丙基]-,盐酸盐(1:1) Chemical Name: N-(2,6-Dimethylphenyl)-N'-[3-(1-methylethylamino)propyl]urea; N-(2,6-Dimethylphenyl)-N'-[3-(isopropylamino)propyl]urea
CAS No. 7473...
参考文献标题:Urea derivatives,processes for preparing them and compositions containing them
文献作者:Sulkowski,T.S.; Bergey,J.L.; Mascitti,A.A.(American Home Products Corp.)
参考来源:EP 0007184; GB 2025406; JP 80500480; US 4224242

Repirinast, MY-5116, Romet

瑞吡司特Chemical Name: 7,8-Dimethyl-4,5-dioxo-5,6-dihydro-4H-pyrano[3,2-c]quinoline-2-carboxylic acid 3-methylbutyl ester
CAS No. 73080-51-0
项目整合开发状态: Launched-1987
项目研究机构: Mitsubishi Chemical (O...
参考文献标题:Repirinast
文献作者:Castar,J.; Prous,J.
参考来源:Drugs Fut 1987,12(1),37