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

T-91825

Chemical Name: (6R,7R)-7-[(Z)-2-(5-Amino-1,2,4-thiadiazol-3-yl)-2-(ethoxyimino)acetamido]-3-[4-(1-methylpyridinium-4-yl)thiazol-2-ylsulfanyl]-3-cephem-4-carboxylate
CAS No. 189345-04-8
项目整合开发状态:...
参考文献标题:TAK-599,a novel N-phosphono type prodrug of anti-MRSA cephalosporin T-91825: Synthesis,physicochemical and pharmacological properties
文献作者:Ishikawa,T.; Matsunaga,N.; Tawada,H.; et al.
参考来源:42nd Intersci Conf Antimicrob Agents Chemother (Sept 27 2002,San Diego) 2002,Abst F-332

新产品编号:921233

Chemical Name: 4(R)-(1-Benzothien-2-ylmethyl)-D-glutamic acid
CAS No. 400625-61-8
项目整合开发状态: Preclinical
项目研究机构: Lilly (Originator)
合成路线:D-Glutamic acid (I) is treated with SOCl2 in EtOH to...
参考文献标题:Chemical cpds.
文献作者:Martin,J.A.; Ezquerra-Carrera,J.; Tebbe,M.J.; De Dios,A.; Prieto,L.; McGee,J.E.; Rubio-Esteban,A.; Smith,M.C.(Eli Lilly and Company)
参考来源:WO 0214261

Epidoxoform

Chemical Name: 10,10'-[(1S,3R,4aS,7aR,8S,10R,11aS,14aR)-1,8-Dimethylperhydro-5,12-methanodipyrano[4,3-d:4',3'-i][1,6,3,8]dioxadiazecin-3,10-diyl]bis(oxy)bis[(6aS,11S)-8-glycoloyl-6,8,11-trihydroxy-1-m...
参考文献标题:Anti-cancer drug aldehyde conjugate drugs with enhanced cytotoxicity: Cpds.,compsns.and methods
文献作者:Taatjes,D.J.; Fenick,D.J.; Koch,T.H.(University Technology Corp.)
参考来源:JP 2002514213; US 6677309; WO 9846598

新产品编号:774107

Chemical Name: 1(R)-[4-[4-(4,6-Dimethyl-1,3,5-triazin-2-yl)-2(R),6(S)-dimethylpiperazin-1-yl]pyrimidin-2-yl]ethanol
CAS No. 300551-49-9
项目整合开发状态: Preclinical
项目研究机构: Pfizer (Originator)
合成...
参考文献标题:Aminopyrimidines as sorbitol dehydrogenase inhibitors
文献作者:Mylari,B.L.; Zembrowski,W.J.; Murry,J.A.; Chu-Moyer,M.Y.(Pfizer Products Inc.)
参考来源:EP 1185275; US 6414149; WO 0059510

新产品编号:918069

Chemical Name: N-[4-[Bis(2-chloroethyl)amino]phenyl]-N'-[2-(4-hydroxyphenyl)ethyl]urea
CAS No. 393511-88-1
项目整合开发状态: Biological Testing
项目研究机构: Imperial Coll. of Sci., Technol. & Med. (Origin...
参考文献标题:Phenylethylamine derivs.and their use in the treatment of melanoma
文献作者:Riley,P.A.; Photiou,A.; Khan,T.H.; Osborn,H.M.I.; Malkin,H.
参考来源:EP 1303481; WO 0208174

BMS-292655

Chemical Name: 3-(Phosphonooxymethyl)benzoic acid [2(R)-[4-(4-cyanophenyl)thiazol-2-yl]-1(R)-(2,4-difluorophenyl)-1-(1H-1,2,4-triazol-1-ylmethyl)propoxy]methyl ester sodium salt
CAS No. 271250-73-8...
参考文献标题:Water soluble prodrugs of azole cpds.
文献作者:Hudyma,T.W.; Kim,O.K.; Zheng,X.(Bristol-Myers Squibb Co.)
参考来源:WO 0030655

AC98-6446

Chemical Name: (3S,6R,9S,12R,15S)-12-[4-[4-[4,6-O-(2-Adamantylidene)-alpha-D-mannopyranosyloxy]-alpha-D-mannopyranosyloxy]benzyl]-15-cyclohexylmethyl-9-[1(S)-hydroxy-1-[2-iminoimidazolidin-4(S)-yl]met...
参考文献标题:Synthesis of AC98-6446,a semisynthetic mannopeptimycin derivative
文献作者:Dushin,R.G.; Wang,T.; Fortier,G.; Iera,S.; Papamichelakis,M.; Richard,L.; Sellstedt,J.; Shah,S.
参考来源:42nd Intersci Conf Antimicrob Agents Chemother (Sept 27 2002,San Diego) 2002,Abst F-352

ANA-380, PMCDG dipivoxil, LB-80380

Chemical Name: Bis(2,2-dimethylpropionic acid) 1-(2-amino-9H-purin-9-ylmethyl)cyclopropoxymethylphosphorylbis(oxymethylene) diester; 1-(2-Amino-9H-purin-9-ylmethyl)cyclopropoxymethylphosphonic acid bi...
参考文献标题:Novel acyclic nucleoside phosphonate derivs.,salts thereof and process for the preparation of the same
文献作者:Lee,C.-H.; Kim,Y.-Z.; Kim,J.-H.; Choi,T.-S.; Kim,C.-M.; Kim,J.-M.; Choi,J.-R.; Roh,K.-Y.; Cho,D.-G.; Hwang,J.-T.; Cho,W.-Y.; Jang,H.-S.; Kim,T.-K.; Cho,S.-J.; Kim,G.-W.(LG Chem Ltd.)
参考来源:WO 0257288

LY-329332

Chemical Name: (3S,6R,7R,22R,23S,26S,36R,38aR)-22-(3-Amino-2,3,6-trideoxy-3-C-methyl-alpha-L-mannopyranosyloxy)-3-(carbamoylmethyl)-10,19-dichloro-44-[2-O-[3-(4'-fluorobiphenyl-4-ylmethylamino)-2,3,6-...
参考文献标题:Novel glycopeptide antibiotics: N-alkylated derivatives active against vancomycin-resistant enterococci
文献作者:Rodriguez,M.J.; Snyder,N.J.; Zweifel,M.J.; Wilkie,S.C.; Stack,D.R.; Cooper,R.D.G.; Nicas,T.I.; Mullen,D.L.; Butler,T.F.; Thompson,R.C.
参考来源:J Antibiot 1998,51(6),560

EP-935

Chemical Name: Acetic acid (4R,5S,6S,7R,9R,10S,14R)-6-[3,6-dideoxy-4-O-[2,6-dideoxy-3-C-methyl-4-O-(3-methylbutyryl)-alpha-L-ribo-hexopyranosyl]-3-(dimethylamino)-beta-D-glucopyranosyl]-10-(dimethylam...
参考文献标题:9-Amino-14-membered macrolides derived from leucomycins
文献作者:Or,Y.S.; Wang,J.; Phan,L.T.; Vo,N.(Enanta Pharmaceuticals,Inc.)
参考来源:US 6436906; WO 0281493