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

TDP-1040-(S)-[125I], (S)-[125I]-TDP-1040, Daizac-I-125, I-125-Daizac

Chemical Name: 5-Chloro-3-(125iodo)-2-methoxy-N-[3(S)-quinuclidinyl]benzamide
CAS No. 179872-27-6, 179871-95-5 (unlabelled)
项目整合开发状态: Preclinical
项目研究机构: Vanderbilt University (Originator) 参考文献标题:Labeling of (S)-des-4-amino-3-[125I]iodozacopride (DAIZAC),a high-affinity radioligand for the 5-HT-3 receptor
文献作者:Mason,N.S.; et al.
参考来源:J Label Compd Radiopharm 1996,38(11),955

AD-8717

Chemical Name: N-(2,6-Dimethyl-4-pyridyl)-2-(2,4-dimethoxybenzylsulfinyl)pyridine-3-carboxamide
CAS No. 181821-99-8
项目整合开发状态: Preclinical
项目研究机构: Dainippon Pharmaceutical (Originator)
合成路线...
参考文献标题:2-Sulfinylnicotinamide derivs.,intermediate thereof,process for producing 2-sulfinylnicotinamide derivs.,and medicinal compsn.containing the same as active ingredient
文献作者:Nishikawa,Y.; Terauchi,H.; Tanitame,A.; Tada,K.; Komiya,M.; Nakamura,K.; Tominaga,Y.(Dainippon Pharmaceutical Co.,Ltd.)
参考来源:WO 9732854

L-758115

Chemical Name: 6-(4-Ethylthiazol-2-ylsulfanyl)-5-(methanesulfonamido)isobenzofuran-1(3H)-one; N-[6-(4-Ethylthiazol-2-ylsulfanyl)-1-oxo-1,3-dihydroisobenzofuran-5-yl]methanesulfonamide
CAS No. 18148...
参考文献标题:5-Methanesulfonamido-3H-isobenzofuran-1-ones as inhibitors of cyclooxygenase-2
文献作者:Guay,D.; Li,C.-S.; Ouimet,N.(Merck Frosst Canada Inc.)
参考来源:US 5968958; WO 9623786

SC-5705, Sch-57050, EM-800

Chemical Name: (S)-4-Methyl-2-[4-[2-(1-piperidinyl)ethoxy]phenyl]-7-(pivaloyloxy)-3-[4-(pivaloyloxy)phenyl]-2H-1-benzopyran
CAS No. 182167-04-0
项目整合开发状态: Phase III
项目研究机构: Endorecherche (Orig...
参考文献标题:Benzopyran-containing cpds.and method for their use
文献作者:Labrie,F.; Merand,Y.; Gauthier,S.(Endorecherche Inc.)
参考来源:EP 0811006; EP 1167364; JP 1999500133; WO 9626201

NC-1175

Chemical Name: 3-(4-Chlorophenyl)-1-[4-[2(E)-(4-chlorophenyl)vinyl]-1-ethyl-4-hydroxy-3-piperidinyl]-2(E)-propen-1-one hydrochloride
CAS No. 205883-84-7 (free base), 211316-99-3 (free base, undefin...
参考文献标题:Mannich bases of conjugates styryl ketones
文献作者:Dimmock,J.R.; Manavathu,E.K.(University of Saskatchewan Technologies Inc.; Wayne State University)
参考来源:US 6017933

SB-236057A(hydrochloride), SB-236057

Chemical Name: 1'-Ethyl-5-[2'-methyl-4'-(5-methyl-1,3,4-oxadiazol-2-yl)biphenyl-4-ylcarbonyl]-2,3,6,7-tetrahydro-5H-spiro[furo[2,3-f]indole-3,4'-piperidine]
CAS No. 180083-49-2, 180084-01-9 (monohy...
参考文献标题:Tetracyclic spiro cpds.,process for their preparation and their use as 5HT1D receptor antagonists
文献作者:Gaster,L.M.; King,F.D.; Wyman,P.A.(GlaxoSmithKline plc)
参考来源:EP 0799226; JP 1998510821; US 5972951; WO 9619477

AT-760

Chemical Name: 6,6'-(1,4-Phenylene)bis[(E)-vinylene]bis(carbonyl)bis[8(S)-(chloromethyl)-4-hydroxy-2-(trifluoromethyl)-3,6,7,8-tetrahydrobenzo[1,2-b:4,3-b']dipyrrole-1-carboxylic acid methyl ester] 参考文献标题:The novel cyclopropapyrroloindole (CPI) bisalkylators bearing 3,3'-(1,4-phenylene)diacryloyl group as a linker
文献作者:Fukuda,Y.; Seto,S.; Furuta,H.; Ebisu,H.; Oomori,Y.; Terashima,S.
参考来源:Bioorg Med Chem Lett 1998,8(15),2003-2004

BO-653

Chemical Name: 4,6-Di-tert-butyl-2,2-dipentyl-2,3-dihydrobenzofuran-5-ol
CAS No. 157360-23-1
项目整合开发状态: Phase II
项目研究机构: Chugai (Originator)
合成路线:The condensation of 4-acetoxy-3,5-di-tert-b...
参考文献标题:4-Alkoxy-2,6-di-tert-butylphenol derivs.
文献作者:Yoshida,M.; Kato,Y.; Tamura,K.; Ohba,Y.; Cynshi,O.(Chugai Pharmaceutical Co.Ltd.)
参考来源:EP 0665208; US 5574178; WO 9408930

Madindoline A, K93-711-A

Chemical Name: 4-Butyl-2-[3a(R)-hydroxy-3,3a,8,8a(S)-tetrahydro-2H-furo[2,3-b]indol-8-ylmethyl]-2(R),5-dimethyl-4-cyclopentene-1,3-dione
CAS No. 184877-64-3 (error)
项目整合开发状态: Preclinical
项目研究...
参考文献标题:Total synthesis of (+)-madindoline A and (-)-madindoline B,potent,selective inhibitors of interleukin 6.Determination of the relative and absolute configurations
文献作者:Sunazuka,T.; et al.
参考来源:J Am Chem Soc 2000,122(9),2122

IDR-16084, GYKI-16084, Uroflux

Chemical Name: (+)-(R)-2-[3-(Benzo-1,4-dioxan-2-ylmethylamino)propyl]pyridazin-3(2H)-one hydrochloride
CAS No. 185739-21-3 (free base)
项目整合开发状态: Phase II
项目研究机构: Gedeon Richter (Originator), ...
参考文献标题:3(2H)-Pyridazinone derivs.and pharmaceutical compsns.containing these cpds.
文献作者:Horv醫h,E.; Simay,A.; Tomori,?; Druga,A.; Kasztreiner,E.; Tilahun,Y.; Makk,N.; Kir醠y,I.; Kos醨y,J.; Papp,?; Varga,M.; Z醨a,E.; Karim,M.; Sebesty閚,L.; Varga,I.; Bidl? M.; Horv醫h,K.; M醫h? I.; et al.(Gyogyszerkutato Intezet Kft.)
参考来源:WO 9638441