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

LFM-A12

Chemical Name: (Z)-2-Cyano-3-hydroxy-N-[4-(trifluoromethoxy)phenyl]-2-butenamide
CAS No. 153736-40-4, 139442-47-0 (undefined isomer)
项目整合开发状态: Preclinical
项目研究机构: Parker Hughes Institute (Ori...
参考文献标题:Inhibitors of the EGF-receptor tyrosine kinase and their use
文献作者:Ghosh,S.; Uckun,F.M.; Zheng,Y.(Parker Hughes Institute)
参考来源:WO 0056703

XJ-304

Chemical Name: N-[2-(4-Cyanophenyl)-1-methyl-4,4-bis(trifluoromethyl)-4,5-dihydro-1H-imidazol-5-yl]-N-methyl-4-propylcyclohexanecarboxamide
CAS No. 195812-62-5 ((-)-trans-isomer), 195812-63-6 ((+)-...
参考文献标题:Design,synthesis and structure-activity relationship studies of novel 4,4-bis(trifluoromethyl)imidazolines as acyl-CoA:cholesterol acyltransferase (ACAT) inhibitors and antihypercholesterolemic agents
文献作者:Li,H.-Y.; DeLucca,I.; Boswell,G.A.; Billheimer,J.T.; Drummond,S.; Gillies,P.J.; Robinson,C.
参考来源:Bioorg Med Chem 1997,5(7),1345

XQ-786

Chemical Name: 2,2-Difluoro-2-(4-isobutylphenyl)-N-[6-methyl-2,4-bis(methylsulfanyl)-3-pyridinyl]acetamide
CAS No. 186024-90-8
项目整合开发状态: Biological Testing
项目研究机构: Bristol-Myers Squibb (Origi...
参考文献标题:Amides for the treatment of atherosclerosis
文献作者:Ko,S.S.; Wilde,R.G.; DeLucca,I.; Li,H.-Y.; Kezar,H.S.III; Boswell,G.A.; Srivastava,A.S.(DuPont Pharmaceuticals Co.)
参考来源:US 5583147

PGE-2946979

Chemical Name: 4-(Benzyloxycarbonyl)-1-(4-methoxyphenylsulfonyl)piperazine-2(R)-carbohydroxamic acid
CAS No. 204139-85-5 (undefined isomer)
项目整合开发状态: Preclinical
项目研究机构: Procter & Gamble (Ori...
参考文献标题:1,4-Heterocyclic metalloprotease inhibitors
文献作者:De,B.; Natchus,M.G.; Pikul,S.; Almstead,N.G.; Matthews,R.S.; Taiwo,Y.O.; Cheng,M.(The Procter & Gamble Co.)
参考来源:EP 0923563; EP 0925287; WO 9808825; WO 9808827

PGE-5747401

Chemical Name: N1-Benzyl-N3-hydroxy-4-(4-methoxyphenylsulfonyl)-N1-methylpiperazine-1,3(R)-dicarboxamide; 4-(N-Benzyl-N-methylcarbamoyl)-1-(4-methoxyphenylsulfonyl)piperazine-2(R)-carbohydroxamic acid...
参考文献标题:1,4-Heterocyclic metalloprotease inhibitors
文献作者:De,B.; Natchus,M.G.; Pikul,S.; Almstead,N.G.; Matthews,R.S.; Taiwo,Y.O.; Cheng,M.(The Procter & Gamble Co.)
参考来源:EP 0923563; EP 0925287; WO 9808825; WO 9808827

CP-265298

Chemical Name: (3S-cis)-N-[3-[6-(5,6-Difluoro-2-benzothiazolylmethoxy)-4-hydroxy-2,2-dimethyl-3,4-dihydro-2H-1-benzopyran-3-ylmethyl]-4-methoxyphenyl]trifluoromethanesulfonamide
CAS No. 158103-79-8...
参考文献标题:Sulfonamide derivs.of benzenefused hydroxy substd.cycloalkyl and heterocyclic ring cpds.
文献作者:Marfat,A.(Pfizer Inc.)
参考来源:EP 0665842; JP 1995508534; US 5641789; WO 9408996

新产品编号:312163

Chemical Name: 5-Chloro-4-isopropoxy-2-methoxy-N-(2-methyl-1,2,3,4-tetrahydro-5-isoquinolinyl)benzamide
CAS No. 201150-38-1 (monoHCl)
项目整合开发状态: Preclinical
项目研究机构: GlaxoSmithKline (Originator...
参考文献标题:Substd.benzamide derivs.and their use as anticon
文献作者:Harling,J.D.; Orlek,B.S.; Thompson,M.(SmithKline Beecham plc)
参考来源:EP 0906283; US 6110934; WO 9748683

Fiduxosin hydrochloride, A-185980.1, ABT-980

Chemical Name: (3aR,9bR)-cis-3-[4-(9-Methoxy-1,2,3,3a,4,9b-hexahydro-[1]benzopyrano[3,4-c]pyrrol-2-yl)butyl]-8-phenylpyrazino[2',3':4,5]thieno[3,2-d]pyrimidine-2,4(1H,3H)-dione hydrochloride
CAS No...
参考文献标题:Benzopyranopyrrole and benzopyranopyridine alpha-1 adrenergic cpds.
文献作者:Meyer,M.D.; Altenbach,R.J.; Basha,F.; Carroll,W.A.; Drizin,I.; Kerwin,J.F.; Wendt,M.D.; Haight,A.R.; Zhang,W.(Abbott Laboratories Inc.)
参考来源:EP 0942911; US 5891882; US 6046207; WO 9824791

L-818571

Chemical Name: 2-(Cyclopropylmethyl)-4-(4-fluorophenyl)-5-[4-(methylsulfonyl)phenyl]pyridazin-3(2H)-one
CAS No. 213763-92-9
项目整合开发状态: Preclinical
项目研究机构: Merck Frosst (Originator)
合成路线:Cyc...
参考文献标题:Pyridazinones as inhibitors of cyclooxygenase-2
文献作者:Therien,M.; Li,C.S.; Lau,C.K.; Prasit,P.; Gauthier,J.Y.(Merck Frosst Canada Inc.)
参考来源:EP 0975604; US 6004960; WO 9841511

L-804600

Chemical Name: 2-Benzyl-4-isopropoxy-5-[4-(methylsulfonyl)phenyl]pyridazin-3(2H)-one
CAS No. 213763-99-6
项目整合开发状态: Preclinical
项目研究机构: Merck Frosst (Originator)
合成路线:Reaction of benzyloxya...
参考文献标题:Anti-tumor cpds.,pharmaceutical compsns.,methods for preparation thereof and for treatment
文献作者:Ojima,I.; Bombardelli,E.(Affymax Technologies,NV; State University of New York,Albany)
参考来源:US 5705508