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

ST-1455(free base)

Chemical Name: (?-7-Chloro-9-(4-methylpiperazin-1-yl)-9,10-dihydropyrrolo[2,1-b][1,3]benzothiazepine dihydrochloride
CAS No. 214270-71-0 (free base)
项目整合开发状态: Preclinical
项目研究机构: Sigma-Tau (O...
参考文献标题:New antipsychotic agents with serotonin and dopamine antagonist properties based on a pyrrolo[2,1-b][1,3]benzothiazepine structure
文献作者:Campiani,G.; Nacci,V.; Bechelli,S.; Ciani,S.M.; Garofalo,A.; Fiorini,I.; Wikstrom,H.; de Boer,P.; Liao,Y.; Tepper,P.G.; Cagnotto,A.; Mennini,T.
参考来源:J Med Chem 1998,41(20),3763

新产品编号:185603

Chemical Name: 4-(4-Amino-6-chloropyrimidin-2-ylsulfanyl)-N,N-diethyl-2(E)-butenamide
CAS No. 185219-02-7
项目整合开发状态: Biological Testing
项目研究机构: Pfizer (Originator)
合成路线:Alkylation of 4,6-di...
参考文献标题:Alpha-substituted pyrimidine-thioalkyl and alkylester compounds as inhibitors of viral reverse transcriptase
文献作者:Nugent,R.A.; et al.(Pharmacia & Upjohn AB)
参考来源:EP 0824524; WO 9635678

Stampidine, Sampidine, STAMP, d4T-pBPMAP, HI-113

Chemical Name: 5'-O-[(4-Bromophenoxy)(O-methyl-L-alanino)phosphoryl]-3'-deoxy-2',3'-didehydrothymidine
CAS No. 217178-62-6
项目整合开发状态: Preclinical
项目研究机构: Parker Hughes Institute (Originator) 参考文献标题:Aryl phosphate derivatives of d4T having anti-HIV activity
文献作者:Uckun,F.M.(Parker Hughes Institute)
参考来源:WO 0000501

新产品编号:449797

Chemical Name: N-Methyl-2(R)-(1-methyl-1H-tetrazol-5-ylsulfanylmethyl)-N-(4-nitrobenzyl)-4-oxoazetidine-1-carboxamide
CAS No. 216960-81-5
项目整合开发状态: Biological Testing
项目研究机构: Bio-Mega (Origin...
参考文献标题:Potent beta-lactam inhibitors of human cytomegalovirus protease
文献作者:Yoakim,C.; Ogilvie,W.W.; Cameron,D.R.; Chabot,C.; Grand-Maitre,C.; Guse,I.; Hache,B.; Kawai,S.; Naud,J.; O'Meara,J.A.; Plante,R.; Deziel,R.
参考来源:Antivir Chem Chemother 1998,9(5),379

LY-339624

Chemical Name: (2S)-2-Amino-4-cyclopentylideneglutaric acid; 4-Cyclopentylidene-L-glutamic acid
CAS No. 213778-21-3
项目整合开发状态: Biological Testing
项目研究机构: Lilly (Originator), NPS Allelix (Origi...
参考文献标题:Glutamic acid derivs.and pharmaceutical compsns.for the treatment of central nervous system disorders
文献作者:Rubio Esteban,A.; Pedregal Tercero,C.(Lilly SA)
参考来源:EP 0867430; ES 2133095; JP 1998279542

H10

Chemical Name: 3-(3-Pyridinyl)-1,5a,6,7,8,9-hexahydropyrano[4,3-b][1]benzopyran-1-one
CAS No. 194796-92-4
项目整合开发状态: Biological Testing
项目研究机构: Kansas State University (Originator)
合成路线:Cla...
参考文献标题:Tricyclic and tetracyclic pyrones
文献作者:Perchellet,J.-P.; Hua,D.H.(Kansas State University)
参考来源:US 5958970

新产品编号:269449

Chemical Name: (5aS,7S)-7-Isopropenyl-3-(3-pyridinyl)-1,5a,6,7,8,9-tetrahydropyrano[4,3-b]chromen-1-one
CAS No. 194937-76-3
项目整合开发状态: Biological Testing
项目研究机构: Kansas State University (Origi...
参考文献标题:A one-pot condensation of pyrones and enals.Synth
文献作者:Hua,D.H.; et al.
参考来源:J Org Chem 1997,62(20),6888

PD-164800

Chemical Name: 2-(1,3-Benzodioxol-5-ylmethyl)-4-(1,3-benzodioxol-5-ylsulfanyl)-7,8-dimethoxy-2H-1,2-benzothiazine-3-carboxylic acid 1,1-dioxide
CAS No. 215648-26-3
项目整合开发状态: Preclinical
项目研究机...
参考文献标题:Endothelin receptor antagonists: Synthesis and structure-activity relationships of substituted benzothiazine-1,1-dioxides
文献作者:Berryman,K.A.; Edmunds,J.J.; Bunker,A.M.; Haleen,S.; Bryant,J.; Welch,K.M.; Doherty,A.M.
参考来源:Bioorg Med Chem 1998,6(9),1447

Trybizine hydrochloride, SIPI-1029, T-46

Chemical Name: 1',1''-(Hexane-1,6-diyl)bis(oxy)bis(spiro[cyclopentane-1,2'(1'H)-1',3',5'-triazine]-4',6'-diamine) dihydrochloride
CAS No. 172280-69-2, 219325-24-3 (free base)
项目整合开发状态: Preclinic...
参考文献标题:Synthesis and antiprotozoal activities of some new triazine derivatives including a new antitrypanosomal agent: SIPI-1029
文献作者:Zhang,X.P.; Shen,J.; Xin,Z.M.; Qiu,Q.P.; Zhou,W.C.
参考来源:Acta Pharm Sin 1996,31(11),823

HZ2

Chemical Name: (1R,2S,4R,5S)-3,7-Dimethyl-9-oxo-2,4-di(2-pyridinyl)-3,7-diazabicyclo[3.3.1]nonane-1,5-dicarboxylic acid dimethyl ester
CAS No. 42165-92-4
项目整合开发状态: Preclinical
项目研究机构: Gr黱enth...
参考文献标题:HZ2,a selective kappa-opioid agonist
文献作者:K鰃el,B.; et al.
参考来源:CNS Drug Rev 1998,4(1),54