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:209333

Chemical Name: 2-(2-Amidino-1,2,3,4-tetrahydroisoquinolin-7-yloxy)-2-[4-(1-amidino-4-piperidinyloxy)phenyl]acetic acid dihydrochloride
CAS No. 188576-47-8
项目整合开发状态: Biological Testing
项目研究机构:...
参考文献标题:New cyclic guanidines,process for preparing the same and medicaments
文献作者:Kucznierz,R.; Von der Saal,W.; Leinert,H.; Grams,F.; Stegmeier,K.(Roche Diagnostics GmbH)
参考来源:DE 19530996; EP 0846115; JP 1999511445; WO 9708165

KML-010

Chemical Name: 8-[4-(4-Fluorophenyl)-4-oxobutyl]-1-methyl-1,3,8-triazaspiro[4.5]decan-4-one dihydrochloride
CAS No. 1045-22-3, 217635-62-6 (free base), 217635-65-9 (labeled)
项目整合开发状态: Biological...
参考文献标题:2,4,8-Triaza-spiro(4,5)dec-2-enes
文献作者:Janssen,P.A.J.(Janssen Pharmaceutica NV)
参考来源:US 3155669

GPI-6150

Chemical Name: 1,11b-Dihydro-1-benzopyrano[4,3,2-de]isoquinolin-3(2H)-one
CAS No. 220938-17-0
项目整合开发状态: Preclinical
项目研究机构: Guilford Pharmaceuticals (Originator)
合成路线:Reduction of 9-xanthe...
参考文献标题:Poly(ADP-ribose) polymerase ("PARP") inhibitors,methods and pharmaceutical compsns.for treating neural or cardiovascular tissue damage
文献作者:Maclin,K.M.; Li,J.-H.; Zhang,J.; Jackson,P.F.(Guilford Pharmaceuticals Inc.)
参考来源:EP 1019409; WO 9911645

新产品编号:171365

Chemical Name: (1alpha,3beta,5Z,7E,23R)-24,24-Difluoro-9,10-secocholesta-5,7,10(19)-triene-1,3,23,25-tetraol; 24,24-Difluoro-1alpha,23(R),25-trihydroxyvitamin D3
CAS No. 183274-07-9
项目整合开发状态: Bi...
参考文献标题:Synthesis and biological evaluation of (23R)- and (23S)-24,24-difluoro-1alpha,23,25-trihydroxyvitamin D3
文献作者:Iwasaki,H.; Miyamoto,Y.; Hosotani,R.; Nakano,Y.; Konno,K.; Takayama,H.
参考来源:Chem Pharm Bull 1998,46(12),1932

新产品编号:172947

Chemical Name: (1alpha,3beta,5Z,7E,23S)-24,24-Difluoro-9,10-secocholesta-5,7,10(19)-triene-1,3,23,25-tetraol; 24,24-Difluoro-1alpha,23(S),25-trihydroxyvitamin D3
CAS No. 183274-08-0
项目整合开发状态: Bi...
参考文献标题:Synthesis and biological evaluation of (23R)- and (23S)-24,24-difluoro-1alpha,23,25-trihydroxyvitamin D3
文献作者:Iwasaki,H.; Miyamoto,Y.; Hosotani,R.; Nakano,Y.; Konno,K.; Takayama,H.
参考来源:Chem Pharm Bull 1998,46(12),1932

AT-61

Chemical Name: (E)-N-[2-Chloro-2-phenyl-1-(piperidin-1-ylcarbonyl)vinyl]benzamide
CAS No. 211363-59-6
项目整合开发状态: Biological Testing
项目研究机构: Gilead (Originator)
合成路线:Condensation of benzalde...
参考文献标题:2-Benzoylamino-3-phenylpropenamide derivs.and methods of using the same
文献作者:Conway,S.C.; Perni,R.B.(Avid Corp.)
参考来源:WO 9833501

SRI-8202

Chemical Name: 6-(5-Methoxy-2-methylphenylaminomethyl)-5-methylpyrido[2,3-d]pyrimidine-2,4-diamine
CAS No. 159210-78-3
项目整合开发状态: Preclinical
项目研究机构: Southern Research Institute (Originator) 参考文献标题:Lipophilic antifolates as agents against opportunistic infections.1.Agents superior to trimetrexate and piritrexim against Toxoplasma gondii and Pneumocystis carinii in in vitro evaluations
文献作者:Piper,J.R.; Johnson,C.A.; Krauth,C.A.; Carter,R.L.; Hosmer,C.A.; Queener,S.F.; Borotz,S.E.; Pfefferkorn,E.R.
参考来源:J Med Chem 1996,39(6),1271

新产品编号:142889

Chemical Name: 4-[4-(Methylsulfonyl)phenyl]-5-phenyl-2-(trifluoromethyl)-1H-imidazole
CAS No. 177754-60-8
项目整合开发状态: Preclinical
项目研究机构: Pfizer (Originator)
合成路线:Reaction of benzaldehyde (I...
参考文献标题:4,5-Substd.imidazolyl cpds.for the treatment of inflammation
文献作者:Weier,R.M.; Collins,P.W.; Stealey,M.A.; Barta,T.E.; Huff,R.M.(Pharmacia Corp.)
参考来源:EP 0772601; US 5620999; WO 9603387

新产品编号:305835

Chemical Name: N-[2-(4-Aminophenyl)-1(S)-[4-(2-fluoroethyl)piperidin-1-ylcarbonyl]ethyl]-4-[1(S)-benzyl-2-(4-morpholinyl)ethyl]pyridine-3-sulfonamide
CAS No. 200270-65-1
项目整合开发状态: Preclinical 参考文献标题:The discovery of orally available thrombin inhibitors: Studies towards the optimisation of CGH1668
文献作者:Ambler,J.; Baker,E.; Brown,L.; Butler,P.; Farr,D.; Dunnet,K.; Le Grand,D.; Janus,D.; Jones,D.; Menear,K.; Mercer,M.; Smith,G.; Talbot,M.; Tweed,M.
参考来源:Bioorg Med Chem Lett 1998,8(24),3583

新产品编号:54297

Chemical Name: (2'S,5'S,6S,6'R,7S,11R,13S,15S,17aR,20R,20aR,20bS)-7-[2,6-Dideoxy-4-O-(2,6-dideoxy-3-O-methyl-alpha-L-mannopyranosyl)-3-O-methyl-alpha-L-mannopyranosyloxy]-4',4'-difluoro-20,20b-dihydro...
参考文献标题:Avermectin difluoro derivs.
文献作者:Meinke,P.T.; Mrozik,H.; Fisher,M.H.(Merck & Co.,Inc.)
参考来源:EP 0638078; JP 1995506361; US 5229416; WO 9322307