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

UR-3216

Chemical Name: 2-[5-[N-[4-(Hydroxyamidino)benzoyl]-4-nitro-L-phenylalanyl]-4,5,6,7-tetrahydro-2H-pyrazolo[4,3-c]pyridin-2-yl]acetic acid ethyl ester
CAS No. 220386-67-4
项目整合开发状态: Preclinical
...
参考文献标题:N-Acylamino acid amide cpds.and intermediates for preparation thereof
文献作者:Baba,K.; Tanaka,M.; Kuroki,Y.; Takata,K.; Motoyama,T.; Ueno,H.(Ube Industries,Ltd.)
参考来源:EP 1020467; US 6265418; WO 9906402

TY-12533

Chemical Name: N''-(2-Methyl-6,7,8,9-tetrahydro-5H-cyclohepta[b]pyridin-3-ylcarbonyl)guanidine maleate
CAS No. 212761-58-5, 212760-82-2 (free base)
项目整合开发状态: Preclinical
项目研究机构: Toa Eiyo (Ori...
参考文献标题:Cycloalka[b]pyridine-3-carbonylguanidine derivs.,process for producing the same,and drugs containing the same
文献作者:Kogi,K.; Takahashi,A.; Gengyou,K.; Aihara,K.; Yoneyama,F.; Sasamori,J.; Yoneyama,S.; Satoh,T.; Yamada,S.; Kimura,T.(Toa Eiyo Ltd.)
参考来源:EP 0972767; WO 9839300

DA-6034

Chemical Name: 2-[2-(3,4-Dimethoxyphenyl)-5-methoxy-4-oxo-4H-1-benzopyran-7-yloxy]acetic acid; 7-(Carboxymethoxy)-3',4',5-trimethoxyflavone
CAS No. 203191-10-0
项目整合开发状态: Phase I
项目研究机构: Dong-...
参考文献标题:Gastroprotective flavone/flavone cpds.with therapeutic effect on inflammatory bowel disease
文献作者:Yoo,M.; Son,M.W.; Kin,I.Y.; Kin,W.B.; Kin,S.H.; Lee,S.D.; Lim,G.J.; Lim,J.I.; Ahn,B.O.; Baik,N.G.; Kin,D.S.; Oh,T.Y.; Ryu,B.K.; Yang,J.S.; Shin,H.C.(Dong-A Pharmaceutical Co.,Ltd.)
参考来源:JP 1999514015; US 6025387; WO 9804541

V-93

Chemical Name: 2'-(Hydroxymethyl)-1'-methyl-5-(4-methyl-1-piperazinyl)[2,5'-bi-1H-benzimidazole]-4',7'-diol
CAS No. 188299-95-8
项目整合开发状态: Preclinical
项目研究机构: University of Alberta (Originator...
参考文献标题:Bis-benzimidazole anticancer agents: Targeting human tumour helicases
文献作者:Soderlind,K.-J.; et al.
参考来源:Anti-Cancer Drug Des 1999,14(1),19

AG-12275

Chemical Name: 1-[4-Amino-2-[4-(4-methyl-1-piperazinyl)phenylamino]thiazol-5-yl]-1-(2,6-difluorophenyl)methanone
CAS No. 223784-70-1
项目整合开发状态: Preclinical
项目研究机构: Agouron (Originator)
合成路线...
参考文献标题:4-Aminothiazole derivs.,their preparation and their use as inhibitors of cyclin-dependent kinases
文献作者:Yang,Y.; Xiao,W.; Chu,S.S.; Li,L.; Chong,W.K.M.; Duvadie,R.R.(Agouron Pharmaceuticals,Inc.)
参考来源:WO 9921845

SB-268091

Chemical Name: (3aS,4R,5S,6S,8R,9R,9aR,10R)-2-(Quinuclidin-4-ylsulfanyl)acetic acid 5-hydroxy-4,6,9,10-tetramethyl-1-oxo-6-vinyldecahydro-3a,9-propano-3aH-cyclopentacycloocten-8-yl ester
CAS No. 22...
参考文献标题:Pleuromutilin derivs.as antimicrobials
文献作者:Dabbs,S.; Hunt,E.; Berry,V.; Woodnutt,G.; Sanderson,F.D.; Frydrych,C.H.(SmithKline Beecham Corp.; SmithKline Beecham plc)
参考来源:EP 1028961; WO 9921855

新产品编号:546299

Chemical Name: 2-Thioxo-1,2,3,4-tetrahydroimidazo[1,5-a]pyrimidine-8-carbothioamide
CAS No. 222292-68-4
项目整合开发状态: Biological Testing
项目研究机构: Minophagen (Originator)
合成路线:The reaction of 5-...
参考文献标题:Novel imidazo[1,5-a]pyrimidine derivs.and their preparation
文献作者:Mizuno,Y.; Matsumoto,K.; Nagata,N.(Minophagen Pharmaceutical Co.,Ltd.)
参考来源:JP 1999092478

新产品编号:547881

Chemical Name: 2-Thioxo-1,2-dihydroimidazo[1,5-a]pyrimidine-8-carbothioamide
CAS No. 222292-72-0
项目整合开发状态: Biological Testing
项目研究机构: Minophagen (Originator)
合成路线:The reaction of 5-amino-1...
参考文献标题:Novel imidazo[1,5-a]pyrimidine derivs.and their preparation
文献作者:Mizuno,Y.; Matsumoto,K.; Nagata,N.(Minophagen Pharmaceutical Co.,Ltd.)
参考来源:JP 1999092478

CEB-1370

Chemical Name: 1-[3-(3,5-Di-tert-butyl-4-hydroxyphenyl)propyl]-3-hydroxy-2-methylpyridin-4(1H)-one methanesulfonate
CAS No. 224563-84-2, 224563-83-1 (free base)
项目整合开发状态: Preclinical
项目研究机构: ...
参考文献标题:Ortho-hydroxypyridinone derivs.as iron chelating and antioxidant agents
文献作者:Malcolm,C.; Porter,R.; Bebbington,D.; Palmer,A.; Gaur,S.; Monck,N.(Vernalis Research Ltd.)
参考来源:EP 1027335; WO 9923075

SUN-N8075

Chemical Name: 1-(4-Amino-2,3,5-trimethylphenoxy)-3-[4-[4-(4-fluorobenzyl)phenyl]piperazin-1-yl]propan-2(S)-ol dimethanesulfonate
CAS No. 224450-56-0, 224450-44-6 (free base)
项目整合开发状态: Phase I 参考文献标题:Arylpiperidinopropanol and arylpiperazinopropanol derivs.and pharmaceuticals containing the same
文献作者:Nakanishi,K.; Annoura,H.; Tamura,S.(Suntory Ltd.)
参考来源:CA 2276373; EP 0958280; WO 9923072