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

UCB-62106

Chemical Name: 4-[4-(Propylsulfanyl)-1,2,5-thiadiazol-3-yl]-1-azatricyclo[3.3.1.1(3,7)]decane hydrochloride
CAS No. 259529-33-4 (stereoisomer, free base), 259665-52-6 (stereoisomer, free base)
项...
参考文献标题:Muscarinic agonists and antagonists
文献作者:Cai,X.; Grewal,G.; Toy-Palmer,A.; Latham,G.M.(UCB SA)
参考来源:EP 1112272; JP 2002523416; US 6093724; WO 0011001

DJS-811

Chemical Name: Cyclo[2'-(aminomethyl)biphenyl-3ylcarbonyl-L-tyrosyl-D-tryptophyl-L-lysyl-L-valyl]
CAS No. 301317-91-9
项目整合开发状态: Preclinical
项目研究机构: Bristol-Myers Squibb (Originator)
合成路线:3...
参考文献标题:Template-constrained cyclic peptide analogues of somatostatin: Subtype-selective binding to somatostatin receptors and antiangiogenic activity
文献作者:Suich,D.J.; Mousa,S.A.; Singh,G.; Liapakis,G.; Reisine,T.; DeGrado,W.F.
参考来源:Bioorg Med Chem 2000,8(9),2229

(R)-HI-511

Chemical Name: N-(5-Bromopyridin-2-yl)-N'-[1(R)-phenylethyl]thiourea
CAS No. 307317-61-9
项目整合开发状态: Biological Testing
项目研究机构: Parker Hughes Institute (Originator)
合成路线:Condensation of 2-am...
参考文献标题:Stereochemistry of halopyridyl and thiazolyl thiourea compounds is a major determinant of their potency as nonnucleoside inhibitors of HIV-1 reverse transcriptase
文献作者:Venkatachalam,T.K.; Sudbeck,E.A.; Mao,C.; Uckun,F.M.
参考来源:Bioorg Med Chem Lett 2000,10(18),2071

SC-276

Chemical Name: 4-[4-(Phenylsulfanyl)phenylsulfonyl]-1-(2-propynyl)piperidine-4-carbohydroxamic acid hydrochloride
CAS No. 226388-60-9, 226393-68-6 (free base), 226393-69-7 (monomethane sulfonate sa...
参考文献标题:Design and synthesis of beta-sulfone and alpha-sulfone hydroxamates as potent and orally active MMP inhibitors
文献作者:Becker,D.P.; Hockerman,S.L.; Barta,T.E.; et al.
参考来源:222nd ACS Natl Meet (Aug 26 2001,Chicago) 2001,Abst MEDI 259

ER-127528

Chemical Name: (+)-2-Fluoro-2-[1-(3-fluorobenzyl)piperidin-4-ylmethyl]-5,6-dimethoxy-2,3-dihydro-1H-inden-1-one hydrochloride
CAS No. 290308-82-6 (undefined isomer), 290308-83-7 (undefined isomer, ...
参考文献标题:Fluorides of 4-substd.piperidine derivs.
文献作者:Sugimoto,H.; Yamanishi,Y.; Shibata,T.; Kosaka,T.; Suzuki,E.; Takeuchi,Y.; Imura,Y.(Eisai Co.,Ltd.)
参考来源:EP 1157989; JP 2000319258; WO 0051985

新产品编号:751959

Chemical Name: 6-O-[2-Acetamido-2-deoxy-6-O-methyl-4-O-phosphono-3-O-[3(R)-(tetradecanoyloxy)tetradecyl]-beta-D-glucopyranosyl]-2-deoxy-2-[3(R)-hydroxytetradecanamido]-3-O-[3(R)-hydroxytetradecyl]-D-g...
参考文献标题:Ether type lipid A1-carboxylic acid analogues
文献作者:Shiozaki,M.; Kurakata,S.; Kanai,S.; Kazama,Y.(Sankyo Co.,Ltd.)
参考来源:EP 1152007; JP 2000297096; US 2002161221; US 6511965; WO 0047595

TRK-851

Chemical Name: (4bS,8R,8aS,16bR)-7-(Cyclopropylmethyl)-11-fluoro-5,6,7,8,9,14,15,16b-octahydro-4,8-methano-8aH,13H-[1]benzofuro[2,3-a]dipyrido[4,3-b:3',2',1'-jk]carbazole-1,8a-diol
CAS No. 189015-2...
参考文献标题:Indole derivs.and medicinal use thereof
文献作者:Nagase,H.; Kawai,K.; Endo,T.; Ueno,S.; Maeda,M.; Sakami,S.(Toray Industries,Inc.)
参考来源:EP 0805157; US 5849731; WO 9711948

BIRT-0377, BIRT-377

Chemical Name: 5(R)-(4-Bromobenzyl)-3-(3,5-dichlorophenyl)-1,5-dimethylimidazolidine-2,4-dione
CAS No. 213211-10-0
项目整合开发状态: Preclinical
项目研究机构: Boehringer Ingelheim (Originator)
合成路线:The ...
参考文献标题:Small molecules useful in the treatment of inflammatory disease
文献作者:Bormann,B.J.; Frye,L.L.; Wu,J.-P.; Kelly,T.A.(Boehringer Ingelheim Pharmaceuticals Inc.)
参考来源:EP 0966447; WO 9839303

AE-3763

Chemical Name: 1-[N-[2-[3-(Carboxymethyl)-2-oxoimidazolidin-1-yl]acetyl]-L-valyl-L-prolinamide N-[3,3,3-trifluoro-1(S)-isopropyl-2-oxopropyl]amide
CAS No. 291778-77-3
项目整合开发状态: Phase I
项目研究机构...
参考文献标题:Heterocyclic cpds.,intermediates thereof and elastase inhibitors
文献作者:Sato,F.; Inoue,Y.; Honda,S.; Komiya,M.; Takemura,T.; Omodani,T.; Shiratake,R.(Dainippon Pharmaceutical Co.,Ltd.)
参考来源:EP 1157998; JP 2000256396; WO 0052032

CHAP-31

Chemical Name: Cyclo[L-isoleucyl-D-prolyl-2(S)-amino-8-(N-hydroxyamino)-8-oxooctanoyl-O-methyl-D-tyrosyl]; (3S,6R,9S,14aR)-6-[6-(4-Methoxybenzyl)-9-[1(S)-methylpropyl]-1,4,7,10-tetraoxoperhydropyrrolo...
参考文献标题:Novel cyclic tetrapeptide derivs.and medicinal use thereof
文献作者:Mimoto,T.; Komatsu,Y.; Horinouchi,S.; Nishino,N.; Yoshida,M.(Japan Energy Corp.)
参考来源:EP 1010705; WO 9911659