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

S-21552-1

Chemical Name: (+)-(R)--8-[4-[5-Methoxyspiro[3,4-dihydro-2H-1-benzopyran-3,2'-pyrrolidin]-1'-yl]butyl]-8-azaspiro[4.5]decane-7,9-dione hydrochloride
CAS No. 153167-20-5 ((-)-enantiomer, free base),...
参考文献标题:3-Aminochromane spiro derivs.,processes for their preparation and pharmaceutical compsns.containing them
文献作者:Guillaumet,G.; Podona,T.; Adam,G.; Guardiola,B.; Renard,P.(ADIR et Cie.)
参考来源:EP 0564358; FR 2689509; JP 1994287190; JP 1995084471; US 5376661; US 5397783

L-742728

Chemical Name: (1S,5R,6S)-2-[7-[4-(Carbamoylmethyl)-1,4-diazabicyclo[2.2.2]octane-1,4-diylium-1-ylmethyl]-9-oxofluoren-3-yl]-6-[1(R)-hydroxyethyl]-1-methyl-1-carba-2-penem-3-carboxylate chloride
CA...
参考文献标题:1-beta-Methyl-carbapenem,compsns.containing same and methods of use
文献作者:Greenlee,M.L.; Dininno,F.P.; Hammond,M.L.(Merck & Co.,Inc.)
参考来源:US 5451579; WO 9521841

新产品编号:123905

Chemical Name: (3beta,5alpha,25R)-3-[4-O-[4,6-O-Bis[N-(2-fluorophenyl)carbamoyl]-beta-D-glucopyranosyl]-beta-D-glucopyranosyloxy]spirostan-12-one; 4'',6''-Bis[N-(2-fluorophenyl)carbamoyl]hecogenyl bet...
参考文献标题:Process research and large-scale synthesis of 4'',6''-bis((2-fluorophenyl)carbomoyl)hecogenyl beta-O-cellobioside: A potent cholesterol absorption inhibitor
文献作者:Urban,F.J.; et al.
参考来源:Org Process Res Dev 1998,2(2),66

AG-2033((6R)-isomer), AG-2034

Chemical Name: N-[5-[2-[2-Amino-4-oxo-4,6,7,8-tetrahydro-3H-pyrimido[5,4-b][1,4]thiazin-6(S)-yl]ethyl]thien-2-ylcarbonyl]-L-glutamic acid
CAS No. 177575-17-6
项目整合开发状态: Phase I
项目研究机构: Agouron...
参考文献标题:Syntheses of optically pure cpds.useful as GARFT inhibitors and their intermediates
文献作者:Varney,M.D.; Palmer,C.L.; Romines,W.H.(Agouron Pharmaceuticals,Inc.)
参考来源:WO 9640674

PD-146626

Chemical Name: 9-Methoxy-2,3,4,5-tetrahydro[1]benzothieno[2,3-f]-1,4-thiazepin-5-one
CAS No. 172832-10-9
项目整合开发状态: Preclinical
项目研究机构: Pfizer (Originator)
合成路线:Methyl 3-chloro-5-methoxyben...
参考文献标题:Benzothiophene,benzofuran and indolethiazepinones,oxazepinones and diazepinones as inhibitors of cell adhesion and as inhibitors of HIV
文献作者:Boschelli,D.H.; Connor,D.T.; Kramer,J.B.; Unangst,P.C.(Pfizer Inc.)
参考来源:EP 0749434; JP 1997509961; US 5489586; WO 9524408

Sibrafiban, G-7333, Ro-48-3657/000, Ro-48-3657, Xubix

Chemical Name: (Z)-2-[1-[N-(4-Hydroxyamidinobenzoyl)-L-alanyl]piperidin-4-yloxy]acetic acid ethyl ester
CAS No. 172927-65-0
项目整合开发状态: Phase III
项目研究机构: Chugai (Originator), Roche (Originator)...
参考文献标题:Acetic acid derivs.as medicaments
文献作者:Alig,L.; Hadvary,P.; H黵zeler M黮ler,M.; M黮ler,M.; Steiner,B.; Weller,T.(F.Hoffmann-La Roche AG)
参考来源:EP 0656348; JP 1995196592; US 5726185

GW-320659, 1555U88, BW-1555U88

Chemical Name: (2S,3S,5R)-2-(3,5-Difluorophenyl)-3,5-dimethylmorpholin-2-ol hydrochloride
CAS No. 135306-42-2, 135414-64-1 (racemic, (2alpha,3alpha, 5alpha)-isomer)
项目整合开发状态: Phase II
项目研究机构:...
参考文献标题:Novel morpholinol cpds.,their preparation and use
文献作者:Kelley,J.L.; Musso,D.L.; Boswell,G.E.; Cooper,B.R.(GlaxoSmithKline plc)
参考来源:AU 9165639; EP 0426416; JP 1991206084; US 5104870

UR-1827

Chemical Name: 2-(1-Benzylpiperidin-4-yl)-1-[4-(5-methylpyrimidin-4-ylamino)phenyl]-1-ethanone
CAS No. 158973-91-2
项目整合开发状态: Preclinical
项目研究机构: Ube (Originator)
合成路线:The condensation of 1...
参考文献标题:Pyrimidine cpd.
文献作者:Kimura,T.; Kuroki,Y.; Fujiwara,H.; Anpeiji,S.(Ube Industries,Ltd.)
参考来源:EP 0664291; WO 9407890

BCH-2687, LEF-553

Chemical Name: L-Tyrosyl-D-arginyl-L-phenylalanyl-L-phenylalaninamide
CAS No. 171807-58-2
项目整合开发状态: Phase II
项目研究机构: AstraZeneca (Originator)
合成路线:Fmoc-protected phenylalanine (I) is attac...
参考文献标题:Novel opioid peptides for the treatment of pain and use thereof
文献作者:Brown,W.; DiMaio,J.; Schiller,P.; Martel,R.(AstraZeneca plc)
参考来源:JP 1997509168; WO 9522557

CEP-1612

Chemical Name: Nalpha-(2-Cyclopentyl-10-phthalimidodecanoyl)-Nomega-nitro-L-arginyl-L-leucinal
CAS No. 179538-06-8, 167416-10-6 (deleted CAS)
项目整合开发状态: Preclinical
项目研究机构: Cephalon (Originato...
参考文献标题:Multicatalytic protease inhibitors
文献作者:Iqbal,M.; Diebold,J.; Siman,R.; Chatterjee,S.; Kauer,J.C.(Cephalon,Inc.)
参考来源:JP 1998507465; JP 2000290197; WO 9614857