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

BMS-212122

9-[4-[2,5-二甲基-4-[[2-[4-(三氟甲基)苯基]苯甲酰基]氨基]苯并咪唑-1-基]丁基]-N-(2,2,2-三氟乙基)芴-9-甲酰胺Chemical Name: 9-[4-[2,5-Dimethyl-4-[4'-(trifluoromethyl)biphenyl-2-ylcarboxamido]-1H-benzimidazol-1-yl]butyl]-N-(2,2,2-triflu...
参考文献标题:Conformationally restricted aromatic inhibitors of microsomal triglyceride transfer protein and method
文献作者:Biller,S.A.; Dickson,J.K.; Lawrence,R.M.; Magnin,D.R.; Poss,M.A.; Robl,J.A.; Slusarchyk,W.A.; Sulsky,R.B.; Tino,J.A.(Bristol-Myers Squibb Co.)
参考来源:EP 0904262; JP 2000502355; WO 9726240

YM-53601

9H-咔唑,2-[(2E)-2-(1-氮杂双环[2.2.2]辛-3-亚基)-2-氟乙氧基]-,一盐酸盐Chemical Name: (E)-2-[2-Fluoro-2-(quinuclidin-3-ylidene)ethoxy]-9H-carbazole hydrochloride
CAS No. 182959-33-7, 182959-28-0 (undefined isomer), 18...
参考文献标题:Novel quinuclidine derivs.having tricyclic fused hetero ring
文献作者:Isaka,M.; Ishihara,T.; Matsuda,K.; Kakuta,H.; Moritani,H.(Yamanouchi Pharmaceutical Co.,Ltd.)
参考来源:EP 0812840; WO 9626938

NSC-619003, KRN-8602(diHCl), MX2, R-20X2(as de-morpholino analog)

9-乙基-4,6,9,10,11-五羟基-7-(5-羟基-6-甲基-4-吗啉-4-基四氢吡喃-2-基)氧基-8,10-二氢-7H-并四苯-5,12-二酮Chemical Name: 3'-Deamino-3'-morpholino-13-deoxo-10-hydroxycarminomycin; 3'-Deamino-3'-morpholinooxaunomycin
CAS No. 1050...
参考文献标题:Anthracycline cpds
文献作者:Kawai,H.; Komeshima,N.; Mizobuchi,S.; Nakajima,S.; Odagawa,A.; Otake,N.; Tatsuta,K.(Microbial Chemistry Research Foundation)
参考来源:EP 0188293; JP 1986167696; JP 1987016495; US 4710564

Amrubicin hydrochloride, SM-5887, Calsed

9-乙酰-9-氨基-7-(4,5-二羟基-2-基)氧-6,11-二羟基-8,10-二氢-7H-四烯-5,12-二酮盐酸盐氨柔比星 Chemical Name: (+)-(7S,9S)-9-Acetyl-9-amino-7-[(2-deoxy-beta-D-erythro-pentopyranosyl)oxy]-7,8,9,10-tetrahydro-6,11-dihydroxy-5,12-nap...
参考文献标题:Aminonaphthacene derivs.
文献作者:Ishizumi,K.; Ohashi,N.; Tanno,N.; Sato,H.; Fukui,M.; Morisada,S.(Sumitomo Pharmaceuticals Co.,Ltd.)
参考来源:EP 0107486; US 4673668

OROS(R)-tacrine, Tacrine hydrochloride, CI-970, THA.HCl, Cognex

9-氨基-1,2,3,4-四氢吖啶盐酸盐水合物他克林 Chemical Name: 1,2,3,4-Tetrahydroacridin-9-amine hydrochloride
CAS No. 1684-40-8, 321-64-2 (free base)
项目整合开发状态: Launched-1993
项目研究机构: Pfizer (Originator)
合成路线:...
参考文献标题:7,8,9,10-Tetrahalo-6H-cyclohepta[b]quinolines
文献作者:Sigal,M.V.Jr.; Brent,B.J.; Marchini,P.
参考来源:US 3232945

SM-10888

9-氨基-8-氟-1,2,3,4-四氢-2,4-甲基丙啶Chemical Name: 9-Amino-8-fluoro-2,4-methano-1,2,3,4-tetrahydroacridine citrate; 8-Fluoro-1,2,3,4-tetrahydro-2,4-methanoacridin-9-amine citrate
CAS No. 129297-21-8, 11620...
参考文献标题:Quinoline derivs
文献作者:Kawakami,H.; Ohuchi,R.; Kitano,M.; Ono,K.(Sumitomo Pharmaceuticals Co.,Ltd.)
参考来源:EP 0268871; JP 1988225358; JP 1988239271; JP 1989000073

SK&F-86466

9-氯-3-甲基-1,2,4,5-四氢-3-苯并氮杂卓Chemical Name: 6-Chloro-2,3,4,5-tetrahydro-3-methyl-1H-3-benzazepine
CAS No. 73943-10-9
项目整合开发状态: Phase II
项目研究机构: GlaxoSmithKline (Originator)
合成路线:The reaction...
参考文献标题:2,3,4,5-Tetrahydro-1H-3-Benzazepines,process for their production and pharmaceutical compositions having dopamine receptor blocking activity
文献作者:Holden,K.G.; Kaiser,C.(SmithKline Beecham Corp.)
参考来源:EP 0007070; EP 0080012; ES 482276; ES 482281; JP 8011584; US 4265890

OMPT, LXR-1035

9-辛地丙烯酸(9Z)-, 3-[(羟基甲基唲冲基)氧]-2-甲氧丙基酯Chemical Name: 9(Z)-Octadecenoic acid 2-methoxy-3-(thiophosphonooxy)propyl ester
CAS No. 213738-69-3
项目整合开发状态: Preclinical
项目研究机构: LXR Biotechnology (Origi...
参考文献标题:Compsns.containing lysophosphatidic acids which inhibit apoptosis and uses thereof
文献作者:Boyd,E.A.; Umansky,S.R.; Baxter,A.D.; Price,S.; Goddard,J.G.; Picker,D.H.; Wijkmans,J.C.H.M.(Evotec Biosystems AG; LXR Biotechnology Inc.)
参考来源:WO 9947101

Technetim (99mTc) tiatide, Technetium (99mTc) mertiatide, MAG3-[99mTc], [99mTc]-MAG3, MAGscinti, Technescan MAG3

a-D-吡喃葡萄糖苷,甲基3-O-b-D-吡喃葡萄糖基-4,6-O-(苯基亚甲基)-Chemical Name: 99mTc-Mercaptoacetylglycylglycylglycine disodium salt; 99mTc-Mercaptoacetyltriglycine disodium salt; (SP-5-25)-[N-[N-[N-(Mercaptoacetyl)glycyl]...
参考文献标题:Radiolabeled technetium chelates for use in renal function determinations
文献作者:Fritzburg,A.(University of Utah)
参考来源:EP 0173424

Eritoran tetrasodium, B-1287, E-5564

a-D-葡萄糖吡喃糖,3-O-癸基-2-脱氧-6-O-[2-脱氧-3-O-[(3R)-3-甲氧基脱氧]-6-O-甲基-2-[[(11Z)-1-氧基-1-辛克-1-基]氨基]-4-O-磷酸-b-D-葡萄糖吡喃基]-2-[(1,3-二氧乙-手环)氨基]-,1-(二氢磷酸盐),钠盐(1:4)间氯苯基哌嗪盐酸盐Chemical Name: 3-O-Decyl-2-deoxy-6-O-[2-deoxy-3-...
参考文献标题:Substd.liposaccharides useful in the treatment and prevention of endotoxemia
文献作者:Kobayashi,S.; Kawata,T.; Christ,W.J.; Rossignol,D.P.(Eisai Co.,Ltd.)
参考来源:US 5750664; WO 9639411