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

(+)-ROD-188

Chemical Name: (+)-5(R)-[2-(4-Methylphenylsulfonyl)-1,2,3,4-tetrahydroisoquinolin-1(R)-yl]tetrahydrofuran-2-one
CAS No. 309267-40-1
项目整合开发状态: Preclinical
项目研究机构: CNRS (Originator), Universit鋞...
参考文献标题:5-[1'-(2'-N-arylsulfonyl-1',2',3',4'-tetrahydroisoquinoly)]-4,5-dihydro-2(3H)-furanones: Positive allosteric modulators of the GABAA receptor with a new mode of action
文献作者:Razet,R.; Thomet,U.; Furtmuller,R.; Chiaroni,A.; Sigel,E.; Sieghart,W.; Dodd,R.H.
参考来源:J Med Chem 2000,43(23),4363

CWJ-a-5

Chemical Name: 1-(4-Methylpiperazin-1-yl)-3-phenylisoquinoline hydrochloride
CAS No. 194292-31-4, 203628-27-7 (free base)
项目整合开发状态: Preclinical
项目研究机构: Chonnam National University (Originator...
参考文献标题:Synthesis and antitumor activity of 3-arylisoquinoline derivatives
文献作者:Park,M.-J.; Chung,B.-H.; Cho,W.-J.; Lee,C.-O.; Yo,S.-J.
参考来源:Arch Pharmacal Res 1997,20(3),264

Thioplatin

Chemical Name: (SP-4-1)-Bis(O-ethyl carbonodithioato-kappaS,kappaS')platinum
CAS No. 19965-15-2, 3444-55-1 (deleted CAS)
项目整合开发状态: Preclinical
项目研究机构: Heraeus (Supplier), Deutsches Krebsforsc...
参考文献标题:Medicament containing platinum complex cpds.and the use thereof
文献作者:Amtmann,E.; Schilling,G.(Deutsches Krebsforschungszentrum; Ruprecht-Karls-Universit鋞 Heidelberg)
参考来源:WO 0010543

MHP-34a

Chemical Name: 4-[(1S,6R,9S,12R)-12-Methoxy-10,11,13-trioxatricyclo[7.2.2.0(1,6)]tridec-9-yl]benzoic acid; 4-[(3R,5aS,9aR,10S)-10-Methoxyhexahydro-3,9a-(epoxymethano)-9aH-1,2-benzodioxepin-3(4H)-yl]be...
参考文献标题:Water-soluble trioxanes as potent and safe antimalarial agents
文献作者:Posner,G.H.; Shapiro,T.A.; Parker,M.H.; Krasavin,M.(Johns Hopkins University)
参考来源:US 6136847; WO 0059501

MF-10058

Chemical Name: 5-[2-[4-[4-(Diethylamino)butyl]piperidin-1-yl]acetyl]-5H-dibenzo[b,f]azepine
CAS No. 315719-45-0
项目整合开发状态: Preclinical
项目研究机构: Mediolanum (Originator)
合成路线:Horner-Emmons rea...
参考文献标题:Selective M2 muscarinic receptor antagonists having 5H-dibenz[b,f]azepine structure
文献作者:Imbimbo,B.P.; Mandelli,G.R.; Terni,P.M.L.; Maiorana,S.(Mediolanum Farmaceutici)
参考来源:WO 0102386

R-123942

Chemical Name: N-[1-[6-(1,2,4-Thiadiazol-5-yl)pyridazin-3-yl]piperidin-4-yl]-N-[3-(trifluoromethyl)phenyl]amine
CAS No. 193957-04-9
项目整合开发状态: Preclinical
项目研究机构: Janssen (Originator)
合成路线:...
参考文献标题:Angiogenesis inhibiting pyridazinamines
文献作者:Stokbroekx,R.A.; Van der Aa,M.J.M.; Willems,M.; Meerpoel,L.; Luyckx,M.G.M.; Tuman,R.W.(Janssen Pharmaceutica NV)
参考来源:EP 0876366; JP 2000503014; US 5985878; WO 9726258

ORG-41841

Chemical Name: 5-Amino-N-tert-butyl-4-(3-methoxyphenyl)-2-(methylsulfanyl)thieno[2,3-d]pyrimidine-6-carboxamide trifluoroacetate
CAS No. 301847-37-0 (free base)
项目整合开发状态: Preclinical
项目研究机构: ...
参考文献标题:Bicyclic heteroaromatic cpds.useful as LH agonists
文献作者:Adang,A.E.P.; Gerritsma,G.G.; Van Straten,N.C.R.(Akzo Nobel N.V.)
参考来源:EP 1171443; JP 2002541259; US 6569863; WO 0061586

Ro-0094889, Ro-09-4889

Chemical Name: 2',3'-Di-O-acetyl-5'-deoxy-5-vinylcytidine
CAS No. 216449-60-4
项目整合开发状态: Phase I
项目研究机构: Chugai (Originator)
合成路线:Silylation of 5-iodocytosine (I) with hexamethyldisilazane,...
参考文献标题:5'-Deoxy-cytidine derivs.
文献作者:Hattori,K.; Suda,H.; Ishikawa,T.; Shimma,N.; Kohchi,Y.; Oikawa,N.; Ishitsuka,H.(F.Hoffmann-La Roche AG)
参考来源:DE 19823484; EP 0882734; ES 2142763; FR 2763953; GB 2325931; JP 1998330395

新产品编号:592177

Chemical Name: N-(5-tert-Butylisoxazol-3-yl)-N'-[4-(4-pyridyloxy)phenyl]urea
CAS No. 228999-48-2
项目整合开发状态: Preclinical
项目研究机构: Bayer (Originator), Onyx (Codevelopment)
合成路线:In a related pr...
参考文献标题:Inhibition of p38 kinase activity using substd.heterocyclic ureas
文献作者:Riedl,B.; Lee,W.; Lowinger,T.B.; Redman,A.; Smith,R.A.; Khire,U.; Dumas,J.; Scott,W.J.; Wood,J.E.; Johnson,J.; Paulsen,H.; Hatoum-Mokdad,H.(Bayer Corp.)
参考来源:WO 9932111

GSQ-83698, GBB-83698, BB-83698

Chemical Name: N-[1(S)-Acetyl-2,2-dimethylpropyl]-2(R)-(N-formyl-N-hydroxyaminomethyl)hexanamide
CAS No. 301684-93-5, 428862-38-8
项目整合开发状态: Phase I
项目研究机构: Vernalis (Originator), Oscient Phar...
参考文献标题:Antimicrobial agents
文献作者:Todd,R.S.; Beckett,R.P.; Brookings,D.C.; Smith,H.K.; Thompson,A.J.(British Biotech Pharmaceuticals Ltd.)
参考来源:EP 1169031; JP 2002541197; WO 0061134