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:878519

Chemical Name: 2(S)-[1,1-Bis(4-cyanophenylsulfanyl)methyl]tetrahydropyran-3(R),4(R),5(R)-triol
CAS No. 354150-40-6, 354150-53-1 (diastereomer)
项目整合开发状态: Preclinical
项目研究机构: Gedeon Richter (Or...
参考文献标题:Orally active antithrombotic thioglycosides,Part XIII - Conversion of 2,6-anhydro-D-altrose and -mannose derivatives with 4-substituted phenyl thiols to prepare compounds with potential antithrombotic activity
文献作者:Bozo,E.; Boros,S.; Kuszmann,J.
参考来源:Carbohydr Res 2001,332(3),325

SCH-350634

Chemical Name: 4-[1-(2,4-Dimethyl-1-oxidopyridin-3-ylcarbonyl)-4-methylpiperidin-4-yl]-2(S)-methyl-1-[1(S)-[4-(trifluoromethyl)phenyl]ethyl]piperazine hydrochloride; 2,4-Dimethyl-3-[4-methyl-4-[3(S)-m...
参考文献标题:Piperazine derivs.useful as CCR5 antagonists
文献作者:Labroli,M.A.; Smith,E.M.; Baroudy,B.M.; Gilbert,E.; Tagat,J.R.; Josien,H.B.; Steensma,R.; Laughlin,M.A.; Miller,M.W.; Clader,J.W.; McKittrick,B.A.; Neustadt,B.R.; Palani,A.; McCombie,S.W.; Vice,S.F.(Schering Corp.)
参考来源:EP 1175401; WO 0066558

GR-377

Chemical Name: N,N'-Bis(4-ethoxyphenyl)-9,10-dioxo-9,10-dihydroanthracene-2,6-disulfonamide
CAS No. 187034-59-9
项目整合开发状态: Biological Testing
项目研究机构: Gentili (Originator)
合成路线:The title bis...
参考文献标题:Mono- and disulfo-substd.anthraquinones and their use for the treatment of bone matrix disorders
文献作者:Benetti,D.; Aloisi,R.; Guainai,G.; Rosini,S.(Istituto Gentili SpA)
参考来源:WO 9700675

AP-23317

Chemical Name: [4-[2-(4-Aminocyclohexylamino)-9-ethyl-9H-purin-6-ylamino]phenyl](hydroxy)phosphorylmethyl]phosphonic acid
CAS No. 344585-41-7 (trans-isomer)
项目整合开发状态: Preclinical
项目研究机构: Aria...
参考文献标题:Purine derivs.
文献作者:Weigele,M.; Sawyer,T.K.; Wang,Y.; Shakespeare,W.C.; Bohacek,R.; Sundaramoorthi,R.; Metcalf,C.A.III; Dalgarno,D.C.(Ariad Pharmaceuticals Inc.)
参考来源:US 2002068721

新产品编号:801001

Chemical Name: 2(R)-(Methylamino)-3-(4-phenoxyphenylsulfonyl)propionohydroxamic acid
CAS No. 310464-35-8 (enantiomer)
项目整合开发状态: Preclinical
项目研究机构: Pfizer (Originator)
合成路线:The reaction of...
参考文献标题:alpha-Amino-beta-sulphone hydroxamates as potent MMP-13 inhibitors that spare MMP-1
文献作者:Becker,D.P.; Barta,T.E.; Bedell,L.; DeCrescenzo,G..; Freskos,J.N.; Getman,D.P.; Hockerman,S.L.; Li,M.; Mehta,P.; Mischke,B.V.; Munie,G.E.; Swearingen,C.; Villamil,C.I.
参考来源:Bioorg Med Chem Lett 2001,11(20),2719

SR-149415, SSR-149415

Chemical Name: (-)-1-[5-Chloro-1-(2,4-dimethoxyphenylsulfonyl)-3-(2-methoxyphenyl)-2-oxo-2,3-dihydro-1H-indol-3-yl]-4(R)-hydroxy-L-proline N,N-dimethylamide
CAS No. 352276-92-7, 352277-03-3 (diaste...
参考文献标题:Novel 1,3-dihydro-2H-indol-2-one derivs.,preparation method and pharmaceutical compsns.containing them
文献作者:Wagnon,J.; Tonnerre,B.; Roux,R.; Serradeil-Le Gal,C.(Sanofi-Synthabo)
参考来源:EP 1255751; FR 2804114; WO 0155130

M-55113

Chemical Name: 4-(6-Chloronaphthalen-2-ylsulfonyl)-1-[1-(4-pyridyl)piperidin-4-ylmethyl]piperazin-2-one
CAS No. 229646-37-1, 239071-44-4 (monohydrochloride), 229646-85-9 (monomethanesufonate salt)<...
参考文献标题:Aromatic cpds.having cyclic amino or salts thereof
文献作者:Miyazaki,Y.; Mukaihira,T.; Nishida,H.; Hosaka,Y.; Matsusue,T.(Mochida Pharmaceutical Co.,Ltd.)
参考来源:EP 1048652; WO 9933805

WMC-79

Chemical Name: 5-Nitro-2-[3-[4-[3-(6-oxo-6H-imidazo[4,5,1-de]acridin-5-ylamino)propyl]piperazin-1-yl]propyl]benzo[de]isoquinoline-1,3(2H)-dione
CAS No. 359630-61-8
项目整合开发状态: Preclinical
项目研究机...
参考文献标题:1,8-Naphthalimide imidazo[4,5,1-de]acridones with anti-tumor activity
文献作者:Cholody,W.M.; Michejda,C.J.; Kosakowska-Cholody,T.(US Department of Health & Human Services)
参考来源:WO 0166545

A-320436

Chemical Name: N-[2-[4-[3-(4'-Cyanobiphenyl-4-yloxy)propyl]perhydro-1,4-diazepin-1-yl]-2-oxo-1(R)-(thiazol-4-ylmethyl)ethyl]furan-2-carboxamide
CAS No. 378233-39-7
项目整合开发状态: Preclinical
项目研究机...
参考文献标题:Cyclic and bicyclic diamino histamine-3 receptor antagonists
文献作者:Black,L.A.; Faghih,R.; Bennani,Y.L.; Liu,H.; Zhang,H.Q.; Dwight,W.J.; Gentles,R.G.; Phelan,K.M.; Vasudevan,A.(Abbott Laboratories Inc.)
参考来源:WO 0166534

A-317920

Chemical Name: N-[2-[4-[3-[4-(Cyclopropylcarbonyl)phenoxy]propyl]piperazin-1-yl]-1(R)-methyl-2-oxoethyl]furan-2-carboxamide
CAS No. 360551-59-3
项目整合开发状态: Preclinical
项目研究机构: Abbott (Originato...
参考文献标题:Cyclic and bicyclic diamino histamine-3 receptor antagonists
文献作者:Black,L.A.; Faghih,R.; Bennani,Y.L.; Liu,H.; Zhang,H.Q.; Dwight,W.J.; Gentles,R.G.; Phelan,K.M.; Vasudevan,A.(Abbott Laboratories Inc.)
参考来源:WO 0166534