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

Edotecarin, ED-749, J-107088

12-(β-D-葡萄吡喃基)-2,10-二羟基-6-[2-羟基-1-(羟甲基)乙基氨基]-6,7,12,13-四氢-5H-吲哚[2,3-a]吡咯罗[3,4-c]卡巴唑-5,7-二酮Chemical Name: 12-(beta-D-Glucopyranosyl)-2,10-dihydroxy-6-[2-hydroxy-1-(hydroxymethyl)ethylamino]-6,7,12,13-t...
参考文献标题:Synthesis and biological activities of NB-506 analogues: Effects of the positions of two hydroxyl groups at the indole rings
文献作者:Ohkubo,M.; Nishimura,T.; Honma,T.; Nishimura,I.; Ito,S.; Yoshinari,T.; Suda,H.; Morishima,H.; Nishimura,S.
参考来源:Bioorg Med Chem Lett 1999,9(23),3307

NSC-262244, TPA

12-O-十四烷酰佛波醋酸酯-13 4α-佛波醇12-十四酸酯13-乙酸酯 Chemical Name: (1aR,1bS,4aR,7aS,7bS,8R,9R,9aS)-9a-Acetoxy-4a,7b-dihydroxy-3-(hydroxymethyl)-1,1,6,8-tetramethyl-9-(tetradecanoyloxy)-1a,1b,4,4a,5,7a,7b,8,9,9a-dec...
参考文献标题:Active components of croton oil.IX.Partial synthesis of the active components of croton oil
文献作者:Bresch,H.; et al.
参考来源:Z Naturforsch B - J Chem Sci 1968,23(4),539

Arbaprostil, CU-83, U-42842, Arbastyl, Arbacet

15(R)-15-甲基前列腺素E2Chemical Name: (E,Z)-(1R,2R,3R)-7-[3-Hydroxy-2-[(3R)-(3-hydroxy-3-methyl-1-octenyl)]-5-oxocyclopentyl]-5-heptenoic acid; (15R)-15-Methylprostaglandin E2
CAS No. 55028-70-1
项目整合开...
参考文献标题:15-Methyl Prostaglandins E2
文献作者:Hillier,K.
参考来源:Drugs Fut 1976,1(9),442

EpiBr, HE-2000, Immunitin, Inactivin

16-溴表雄酮Chemical Name: 16alpha-Bromoepiandrosterone; 16alpha-Bromo-3beta-hydroxyandrostan-17-one
CAS No. 28507-02-0
项目整合开发状态: Phase II
项目研究机构: Colthurst (Originator), Hollis-Eden (Originator),...
参考文献标题:Inhibition of HIV replication: Synthesis of [4-14C]-5alpha-androstan-16alpha-bromo-3 beta-ol-17-one
文献作者:Han,M.C.; Hayes,B.A.; Prendergast,P.T.; Gupta,S.
参考来源:J Label Compd Radiopharm 2000,43(12),1149

Osaterone acetate, TZP-4238, Hipros

17-alpha-乙酰氧基-6-氯-2-氧杂-4,6-孕甾二烯-3,20-二酮Chemical Name: 17alpha-Acetoxy-6-chloro-2-oxapregna-4,6-diene-3,20-dione; 6-Chloro-17-hydroxy-2-oxapregna-4,6-diene-3,20-dione 17-acetate; 2-Oxachlormadinone ace...
参考文献标题:2-Oxa- or aza-pregnane derivs
文献作者:Shibata,K.; Yamakoshi,N.; Koizumi,N.; Takegawa,S.; Shimazawa,E.; Mieda,M.(Teikoku Hormone Manufacturing Co.,Ltd.)
参考来源:AU 8654245; EP 0193871; ES 8801510; ES 8801669; ES 8801670; ES 8801928; JP 1986204198; JP 1986204199; US 4735103; US 4914106

WAY-141839, GMA-839, Co-2-6749

19-去甲堙嘀-20-1,3,21-二羟基-3-(三氟甲基)-,(3α,5β)-Chemical Name: 3alpha,21-Dihydroxy-3beta-(trifluoromethyl)-19-nor-5beta-pregnan-20-one
CAS No. 162882-76-0
项目整合开发状态: Preclinical
项目研究机构: CoCensys (Orig...
参考文献标题:Methods and compsns.for inducing sleep
文献作者:Lan,N.T.-Y.; Gee,K.W.(CoCensys,Inc.)
参考来源:CA 2163748; WO 9427608

ara-CDP-D,L-PBA

1-beta-D-阿拉伯糖呋喃基胞嘧啶 5'-二磷酸酯-1-O-十八烷基-2-O-棕榈酰-甘油Chemical Name: 1-[5-O-(1-Octadecyl-2-palmitoyl-rac-glycero-diphospho)-beta-D-arabinofuranosyl]cytosine disodium salt; 1-beta-D-Arabinofuranosylcytosine-5...
参考文献标题:Thiophospholipid conjugates of antitumor agents
文献作者:(Health Research,Inc.)
参考来源:EP 0183843; US 4622392; WO 8600309

SDZ-89-485

1H-1,2,4-三唑-1-乙醇,a-(4-氯苯)-a-(1-环丙基-1-甲基乙基)-,(aR)-Chemical Name: (-)-(R)-alpha-(4-Chlorophenyl)-alpha-(1-cyclopropyl-1-methylethyl)-1H-1,2,4-triazol-1-ethanol; (-)-(R)-2-(4-Chlorophenyl)-3-cyclopropyl-...
参考文献标题:Synthesis and structure-activity relationships of SDZ 89-485 and analogues
文献作者:Meingassner,J.G.; Grassberger,M.A.; Schaub,F.
参考来源:Xth Cong Int Soc Human Animal Mycol (Barcelona) 1988,Abst P-153

DBO-83

1H-2-苯并吡喃-5,6-二醇,1-(氨基甲基)-3,4-二氢-3-(羟甲基)-,(1R,3S)-Chemical Name: 3-Chloro-6-(3,8-diazabicyclo[3.2.1]oct-3-yl)pyridazine dihydrochloride
CAS No. 195211-53-1
项目整合开发状态: Preclinical
项目研究机构: Unive...
参考文献标题:Mono- and disubstituted-3,8-diazabicyclo[3.2.1]octane derivatives as analgesics structurally related to epibatidine: Synthesis,activity,and modeling
文献作者:Barlocco,D.; Cignarella,G.; Tondi,D.; Vianello,P.; Villa,S.; Bartolini,A.; Ghelardini,C.; Galeotti,N.; Anderson,D.J.; Kuntzweiler,T.A.; Colombo,D.; Toma,L.
参考来源:J Med Chem 1998,41(5),674

Indisetron hydrochloride, N-3389, Indisetron HCl Nisshin, Sinseron

1H-吆佐-3-羔酰胺,N-[(7-endo)-3,9-二甲基-3,9-二氮双环[3.3.1]非7-基]-,二盐酸盐(9CI)Chemical Name: N-(endo-3,9-Dimethyl-3,9-diazabicyclo[3.3.1]non-7-yl)-1H-indazole-3-carboxamide dihydrochloride
CAS No. 160472-97-9, 14...
参考文献标题:Azabicyclo derivs.and their use as antiemetics
文献作者:Kikuchi,H.; Satoh,H.; Yahata,N.; Hagihara,K.; Hayakawa,T.; Mino,S.; Yanai,M.(Nisshin Flour Milling Co.,Ltd.)
参考来源:EP 0469449; JP 1993310749; US 5187166