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

Cinpropazide

桂丙齐特Chemical Name: N-(3,4,5-Trimethoxycinnamoyl)-N'-(isopropylaminocarbonylmethyl)-piperazine; N-Isopropyl-[4-(3,4,5-trimethoxycynnamoyl)-1-piperazino]acetamide
CAS No. 23887-47-0
项目整合开发状态: Biol...
参考文献标题:Derivatives of 1-(3,4,5-trimethoxycinnamoyl)piperazineand process for their preparation
文献作者:Fauren,C.; et al.(Laboratoires Delalande)
参考来源:BE 0730345; FR 2007372; GB 1218591; US 3634411

Cinnarizine clofibrate, LM-16

桂利嗪氯贝特Chemical Name: 1-(Diphenylmethyl)-4-(3-phenyl-2-propenyl)piperazine 2-(4-chlorophenoxy)-2-methylpropanoate
CAS No. 60763-49-7
项目整合开发状态: Not Determined
项目研究机构:
合成路线:By heating a mixt...
参考文献标题:
文献作者:
参考来源:BE 837117

Sunifiram, DM-235

桑尼非拉姆Chemical Name: 1-(4-Benzoylpiperazin-1-yl)propan-1-one; 1-Benzoyl-4-(1-oxopropyl)piperazine
CAS No. 314728-85-3
项目整合开发状态: Preclinical
项目研究机构: Universit?degli Studi di Firenze (Originator...
参考文献标题:1,4-Diazabicyclo[4.3.0]nonan-9-ones and 1,4-diamidopiperazines as new classes of highly potent nootropic drugs
文献作者:Bellucci,C.; Ghelardini,C.; Dei,S.; Bartolini,A.; Galeotti,N.; Romanelli,M.N.; Gualtiere,F.; Manetti,D.; Scapecchi,S.; Teodori,E.
参考来源:16th Int Symp Med Chem (Sept 18 2000,Bologna) 2000,Abst PB-119

Tolciclate, K-9147

桥萘酯Chemical Name: N-Methyl-N-(3-methylphenyl)carbamothioic acid O-(1,2,3,4-tetrahydro-1,4-methanonaphthalen-6-yl) ester
CAS No. 50838-36-3
项目整合开发状态: Not Determined
项目研究机构:
合成路线:Compound c...
参考文献标题:Tolciclate
文献作者:Castar,J.; de Angelis,L.
参考来源:Drugs Fut 1976,1(11),543

Gossypol

棉酚Chemical Name: 1,1',6,6',7,7'-Hexahydroxy-3,3'-dimethyl-5,5'-diisopropyl-(2,2'-binaphthalene)-8,8'-dicarboxaldehyde; 2,2'-Bis(1,6,7-trihydroxy-3-methyl-5-isopropyl-8-formylnaphthalene)
CAS No. 30...
参考文献标题:Gossypol
文献作者:Leeson,P.
参考来源:Drugs Fut 1979,4(5),338

beta-Elemene, Elemene

榄香烯Chemical Name: (1alpha,2beta,4beta)-2,4-Diisopropenyl-1-methyl-1-vinylcyclohexane; (1alpha,2beta,4beta)-1-Ethenyl-1-methyl-2,4-bis(1-methylethenyl)cyclohexane
CAS No. 33880-83-0, 192460-89-2 ((-...
参考文献标题:Stereoselective synthesis of (?-beta-elemene by a doubly diastereodifferentiating internal alkylation: A remarkable difference in the rate of enolization between syn and anti esters
文献作者:Lee,J.; Kim,S.; Kim,D.; Chang,J.
参考来源:Tetrahedron 2001,57(7),1247

Olivomycin A

橄榄霉素Chemical Name: (2S,3S)-6-[4-O-Acetyl-2,6-dideoxy-3-O-(2,6-dideoxy-4-O-methyl-alpha-D-galactopyranosyl)-beta-D-galactopyranosyloxy]-2-[2,6-dideoxy-3-O-[2,6-dideoxy-3-O-(2,6-dideoxy-4-O-isobutyryl-3...
参考文献标题:Total synthesis of olivomycin A
文献作者:Roush,W.R.; et al.
参考来源:J Am Chem Soc 1999,121(9),1990

Olamufloxacin mesilate, HSR-903

欧拉沙星Chemical Name: (-)-5-Amino-7-[7(S)-amino-5-azaspiro[2.4]hept-5-yl]-1-cyclopropyl-6-fluoro-8-methyl-4-oxo-1,4-dihydroquinoline-3-carboxylic acid methanesulfonate
CAS No. 167887-97-0 (free base)<...
参考文献标题:5-Amino-8-methyl-7-pyrrolidinylquinoline-3-carboxylic acid deriv.
文献作者:Ito,Y.; Kato,H.; Yasuda,S.; Kado,N.; Yoshida,T.; Yamamoto,Y.(Hokuriku Seiyaku Co.,Ltd.)
参考来源:CA 2126118; EP 0641793; JP 1995309864; US 5547962

Bicalutamide, ICI-176334, Raffolutil, Casodex

比卡鲁胺Chemical Name: (?-4-[3-(4-Fluorophenylsulfonyl)-2-hydroxy-2-methylpropionamido]-2-(trifluoromethyl)benzonitrile
CAS No. 90357-06-5
项目整合开发状态: Launched-1995
项目研究机构: AstraZeneca (Originator)...
参考文献标题:Amide derivs.
文献作者:Tucker,H.(AstraZeneca plc)
参考来源:EP 0100172; JP 1990131462; US 4636505

Bidisomide, SC-40230

比地索胺 1-哌啶丁丁酰胺,a-[2-[乙酰(1-甲基)氨基]乙基]-a-(2-氯苯基)- Chemical Name: (?-alpha-[2-[Acetyl(1-methylethyl)amino]ethyl]-alpha-(2-chlorophenyl)-1-piperidinebutanamide; (?-alpha-(o-Chlorophenyl)-alpha-[2-(N-isoprop...
参考文献标题:Synthesis and structure-activity relationships of new series of antiarrhythmic agents: Monobasic derivatives of disobutamide
文献作者:Chorvat,R.J.; Rorig,K.J.; Fowler,K.W.; Frederick,L.G.; Desai,B.N.; Garthwaite,S.M.; Hatley,F.R.
参考来源:J Med Chem 1988,312158