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

新产品编号:106503

Chemical Name: 1-Deoxy-1-[2-[2-(1H-imidazol-4-yl)ethylamino]-6-(2,2-diphenylethylamino)-9H-purin-9-yl]-N-ethyl-beta-D-ribofuranuronamide trifluoroacetate
CAS No. 167465-88-5 (as hydrochloride), 167...
参考文献标题:2,6-Diaminopurine derivs.
文献作者:Gregson,M.; Ayres,B.E.; Ewan,G.B.; Ellis,F.; Knight,J.(Glaxo Wellcome plc)
参考来源:EP 0680488; JP 1996505864; US 5925624; WO 9417090

新产品编号:718737

Chemical Name: 1-(2,2-Dimethyl-6-nitro-2,3-dihydro-4H-1,4-benzothiazin-4-yl)-2-propanone
CAS No. 265994-74-9
项目整合开发状态: Biological Testing
项目研究机构: Yamanouchi (Originator)
合成路线:Alkylation of...
参考文献标题:Novel potassium channel openers.Part 4: Transformation of the 1,4-benzoxazine skeleton into 1,4-benzothiazine,1,2,3,4-tetrahydroquinoline,1,2,3,4-tetrahydroquinoxaline,indoline,and 1,5-benzoxazepine
文献作者:Matsumoto,Y.; Tsuzuki,R.; Matsuhisa,A.; Yamagiwa,Y.; Yanagisawa,I.; Shibanuma,T.; Nohira,H.
参考来源:Bioorg Med Chem 2000,8(2),393

新产品编号:707663

Chemical Name: 2(R,S)-[(1R*,3S*,4S*)-4-(6-Amino-9H-purin-9-yl)spiro[2.2]pent-1-ylmethoxy](phenoxy)phosphorylamino]propionic acid methyl ester; N-[[(1R*,3S*,4S*)-4-(Adenin-9-yl)spiro[2.2]pent-1-ylmetho...
参考文献标题:Spiropentane mimics of nucleosides: Analogues of 2'-deoxyadenosine and 2'-deoxyguanosine.Synthesis of all stereoisomers,isomeric assignment,and biological activity
文献作者:Guan,H.P.; Ksebati,M.B.; Cheng,Y.C.; Drach,J.C.; Kern,E.R.; Zemlicka,J.
参考来源:J Org Chem 2000,65(5),1280

SB-227122

Chemical Name: 4-Hydroxy-3-methoxy-4',17-dimethyl-6,7-didehydropyrrolo[2',3':6,7]morphinan-5'-carboxylic acid diisopropylamide
CAS No. 177284-71-8
项目整合开发状态: Preclinical
项目研究机构: GlaxoSmithKlin...
参考文献标题:Heterocycle-condensed morphinoid derivs.
文献作者:Dondio,G.; Ronzoni,S.(SmithKline Beecham plc)
参考来源:EP 0770081; JP 1998502657; US 5981540; WO 9602545

新产品编号:720319

Chemical Name: N-[4-Oxo-4-(4-pyridinylamino)butyl]carbamic acid tert-butyl ester
CAS No. 266353-29-1
项目整合开发状态: Preclinical
项目研究机构: Chiesi (Originator)
合成路线:4-(tert-Butoxycarbonylamino)buty...
参考文献标题:4-Aminopyridine derivatives with antiamnesic activity
文献作者:Andreani,A.; Leoni,A.; Locatelli,A.; Morigi,R.; Rambaldi,M.; Pietra,C.; Villetti,G.
参考来源:Eur J Med Chem 2000,35(1),77

新产品编号:672859

Chemical Name: 3-Isopropyl-4-methylpentanoic acid [2-(hydroxymethyl)-4-[(Z)-3-isopropyl-4-methylpentylidene]-5-oxotetrahydrofuran-2-yl]methyl ester
CAS No. 253603-03-1
项目整合开发状态: Biological Testi...
参考文献标题:Conformationally constrained analogues of diacylglycerol (DAG).16.How much structural complexity is necessary for recognition and high binding affinity to protein kinase C?
文献作者:Nacro,K.; Bienfait,B.; Lee,J.; Han,K.C.; Kang,J.-H.; Benzaria,S.; Lewin,N.E.; Bhattacharyya,D.K.; Blumberg,P.M.; Marquez,V.E.
参考来源:J Med Chem 2000,43(5),921

新产品编号:473527

Chemical Name: N-[2-[4-(Dimethylamino)benzamido]-4-hydroxyphenyl]-4-methoxybenzamide
CAS No. 219491-20-0
项目整合开发状态: Biological Testing
项目研究机构: Lilly (Originator)
合成路线:Treatment of 4-(dimeth...
参考文献标题:Antithrombotic agents
文献作者:Sawyer,J.S.; Tinsley,J.M.; Wiley,M.R.; Hall,S.E.; Milot,G.; Shuman,R.T.; Goodson,T.Jr.; Klimkowski,V.J.; Kyle,J.A.; Masters,J.J.; Weir,L.C.; Mendel,D.; Beight,D.W.; Tebbe,A.L.; Yee,Y.K.; et al.(Eli Lilly and Company)
参考来源:WO 9900121

A-204176

Chemical Name: N-[5-(1H-Imidazol-4-yl)-5,6,7,8-tetrahydronaphthalen-1-yl]methanesulfonamide
CAS No. 258527-44-5, 258526-38-4 (HCl), 258818-73-4 (R-isomer), 258526-39-5 (R-isomer, HCl salt), 258818-...
参考文献标题:Imidazoles and related cpds.as alpha1A agonists
文献作者:Altenbach,R.J.; Holladay,M.W.; Carroll,W.A.; Meyer,M.D.; Kerwin,J.F.Jr.; Kolasa,T.; Rohde,J.; Khilevich,A.(Abbott Laboratories Inc.)
参考来源:WO 0007997

AWD-33-159

Chemical Name: 4-Amino-1-(2-chlorophenyl)pyridin-2(1H)-one
CAS No. 256653-53-9
项目整合开发状态: Preclinical
项目研究机构: AWD.pharma (Originator)
合成路线:The title N-phenylpyrimidinone was prepared from t...
参考文献标题:New 4-amino-1-aryl-pyridine-2-ones with anticonvulsive action and method for producing same
文献作者:Bartsch,R.; Rostock,A.; Lankau,H.-J.; Unverferth,K.; Arnold,T.; Granik,V.; Grizik,S.(AWD.pharma GmbH & Co.KG)
参考来源:DE 19835918; EP 1102748; JP 2002522420; WO 0007988

SJ-755

Chemical Name: 3-[(5S,8S)-8-(1H-Benzimidazol-2-ylaminomethyl)-7-(butoxycarbonyl)-1-oxa-2,7-diazaspiro[4.4]non-2-en-3-ylcarboxamido]-2(S)-(2,4,6-trimethylphenylsulfonamido)propionic acid trifluoroaceta...
参考文献标题:Spirocycle integrin inhibitors
文献作者:Jadhav,P.K.; Smallheer,J.M.(DuPont Pharmaceuticals Co.)
参考来源:EP 0888344; US 5760029; WO 9733887