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

PNU-177553

Chemical Name: N-[3-[3-Fluoro-4-(1-oxidothiomorpholin-4-yl)phenyl]-2-oxooxazolidin-5(S)-ylmethyl]thioacetamide
CAS No. 216868-86-9
项目整合开发状态: Biological Testing
项目研究机构: Pfizer (Originator)
...
参考文献标题:Oxazolidinone antibacterial agents having a thiocarbonyl functionality
文献作者:Hester,J.B.Jr.; Perricone,S.C.; Nidy,E.G.; Poel,T.-J.(Pharmacia Corp.)
参考来源:EP 0984947; JP 2002501530; US 6218413; WO 9854161

CP-642959

Chemical Name: 11-Amino-11-deoxy-3-des(hexopyranosyloxy)-9-deoxo-9-(methoxyimino)-6-O-methyl-3-oxo-11-[3(R)-[4-(3-pyridyl)imidazol-1-yl]butylhydrazino]erythromycin A 11- N1,12-O-cyclic carbamate
CA...
参考文献标题:Carbamate and carbazate ketolide antibiotics
文献作者:Kaneko,T.; Su,W.-G.; Wu,Y.-J.(Pfizer Inc.)
参考来源:EP 1115732; WO 0017218

RWJ-415663

Chemical Name: 11-Amino-13-deethyl-11-deoxy-3-des(hexopyranosyloxy)-2-fluoro-3-oxo-13-propyl-6-O-[3-(3-quinolyl)-2(E)-propenyl]erythromycin A 11-N,12-O-cyclic carbamate
CAS No. 301320-09-2, 300841-...
参考文献标题:Structure-antibacterial activty relationships of ketolides derived from 15-methylerythromycin A
文献作者:Macielag,M.; et al.
参考来源:41st Intersci Conf Antimicrob Agents Chemother (Dec 16 2001,Chicago) 2001,Abst F-1174

新产品编号:845297

Chemical Name: N-Methyl-N-(2-methyl-1H-indol-3-ylmethyl)-3-(7-oxo-5,6,7,8-tetrahydro-1,8-naphthyridin-3-yl)-2(E)-propenamide
CAS No. 335029-51-1
项目整合开发状态: Preclinical
项目研究机构: GlaxoSmithKline ...
参考文献标题:Fab I inhibitors
文献作者:Uzinskas,I.N.; Miller,W.H.; Newlander,K.A.; Jakas,D.R.; Seefeld,M.A.; DeWolf,W.E.Jr.(GlaxoSmithKline Inc.)
参考来源:EP 1226138; WO 0127103

新产品编号:701335

Chemical Name: (2R*,3R*,3aS*,5aR*,10S*,10aR*)-N-(3,4-Dichlorophenyl)-10-hydroxy-4-oxo-2-phenyl-2,3,3a,4,5a,10-hexahydrofuro[2,3-c]indeno[1,2-b]furan-3-carboxamide
CAS No. 261157-64-6 (undefined ste...
参考文献标题:Tetracyclic heterocycles as antimicrobial agents
文献作者:Wang,Z.; Hill,J.; Finn,J.; Yu,X.Y.; Keith,D.; Gallant,P.; Wendler,P.(Cubist Pharmaceuticals,Inc.)
参考来源:US 6153645; WO 0017206

新产品编号:702917

Chemical Name: (2R*,3R*,3aS*,5aR*,10R*,10aR*)-N-(3,4-Dichlorophenyl)-10-hydroxy-4-oxo-2-phenyl-2,3,3a,4,5a,10-hexahydrofuro[2,3-c]indeno[1,2-b]furan-3-carboxamide
CAS No. 261157-64-6 (undefined ste...
参考文献标题:Tetracyclic heterocycles as antimicrobial agents
文献作者:Wang,Z.; Hill,J.; Finn,J.; Yu,X.Y.; Keith,D.; Gallant,P.; Wendler,P.(Cubist Pharmaceuticals,Inc.)
参考来源:US 6153645; WO 0017206

新产品编号:533643

Chemical Name: 7-[3(S)-Amino-4(R)-ethylpiperidin-1-yl]-1-cyclopropyl-8-methoxy-4-oxo-1,4-dihydroquinoline-3-carboxylic acid
CAS No. 221240-75-1 (undefined stereochem.)
项目整合开发状态: Biological Testi...
参考文献标题:Antimicrobial quinolones,their compsns.and uses
文献作者:Hu,X.E.; Gray,J.L.; Almstead,J.-I.K.; Ledoussal,B.(The Procter & Gamble Co.)
参考来源:EP 1015445; WO 9914214

GW-532

Chemical Name: 4-Chloro-N-[4-[N-[4-[4-(2-ethoxy-4-ethylphenyl)piperidin-1-yl]butyl]carbamoyl]phenyl]benzamide
CAS No. 320589-95-5
项目整合开发状态: Preclinical
项目研究机构: GlaxoSmithKline (Originator) 参考文献标题:Binding competition of SREBP-cleavage activating protein (SCAP) antagonists
文献作者:Grand-Perret,T.A.R.; Issandou,M.(GlaxoSmithKline plc)
参考来源:WO 0106261

YM-91746

Chemical Name: N-[6-Methoxy-5-(2-methoxyphenoxy)-2,2'-bipyrimidin-4-yl]-1-phenyl-1(E)-butene-2-sulfonamide potassium salt
CAS No. 192645-50-4 (undefined isomer)
项目整合开发状态: Preclinical
项目研究机构: ...
参考文献标题:Arylethenesulfonamide derivs.and drug compsn.containing the same
文献作者:Harada,H.; Kazami,J.; Watanuki,S.; Tsuzuki,R.; Sudou,K.; Tanaka,A.(Yamanouchi Pharmaceutical Co.,Ltd.)
参考来源:EP 0882719; US 6083955; WO 9722595

JB-99157

Chemical Name: 3-[5-(Adamant-1-yloxymethyl)-2-cyclohexyl-1H-imidazol-4-ylcarboxamido]benzoic acid
CAS No. 269069-71-8, 372489-10-6 (Na salt)
项目整合开发状态: Preclinical
项目研究机构: James Black Foundati...
参考文献标题:Pharmaceutical compsns.comprising proton pump inhibitors and gastrin/cholecystokinin receptor ligands
文献作者:Kalindjian,S.B.; Mesens,J.L.; Black,J.W.; Hull,R.A.D.; Shankley,N.P.; Andries,L.J.(James Black Foundation Ltd.; Janssen Pharmaceutica NV)
参考来源:WO 0185167