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

KT-8138, CEP-11004

Chemical Name: (9alpha,10beta,12alpha)-5,16-Bis(isopropylsulfanylmethyl)-9,12-epoxy-10-hydroxy-9-methyl-1-oxo-2,3,9,10,11,12-hexahydro-1H-diindolo[1,2,3-fg:3',2',1'-kl]pyrrolo[3,4-i][1,6]benzodiazocin...
参考文献标题:Protein kinase inhibitors for treatment of neurological disorders
文献作者:Lewis,M.E.; Kauer,J.C.; Neff,N.; Glicksman,M.; Roberts-Lewis,J.; Murakata,C.; Saito,H.; Matsuda,Y.; Kanai,F.; Kaneko,M.(Cephalon,Inc.; Kyowa Hakko Kogyo Co.,Ltd.)
参考来源:EP 0788501; JP 1998510514; WO 9613506; WO 9613506

新产品编号:986095

Chemical Name: N-Allyl-2-methoxy-N,N-dimethylbenzenaminium bromide
CAS No. 80573-82-6
项目整合开发状态: Preclinical
项目研究机构: Organon (Originator)
合成路线:Direct amination of veratrole (I) with lithium...
参考文献标题:Oxyaniliniums as acetylcholinesterase inhibitors for the reversal of neuromuscular block
文献作者:Grove,S.J.A.; Kaur,J.; Muir,A.W.; Pow,E.; Tarver,G.J.; Zhang,M.-Q.
参考来源:Bioorg Med Chem Lett 2002,12(2),193

新产品编号:736139

Chemical Name: 3(R)-[3'-[3-(1H-Benzimidazol-2-yl)ureido]-4-methoxybiphenyl-3-ylsulfonamido]-3-phenylpropionic acid
CAS No. 276261-99-5, 276259-37-1 (racemate)
项目整合开发状态: Biological Testing
项目研...
参考文献标题:New biphenyl and biphenyl-analogous cpds.as integrin antagonists
文献作者:Schmidt,D.; Urbahns,K.; Gerdes,C.; Keldenich,J.; H鋜ter,M.; Stahl,E.; Albers,M.; Vaupel,A.; Stelte-Ludwig,B.; Br黦gemeier,U.; Lustig,K.(Bayer AG)
参考来源:EP 1140809; JP 2002532465; US 6420396; WO 0035864

新产品编号:157127

Chemical Name: N-(5,11-Difluoro-2,3,3a,8-tetrahydrodibenzo[c,f]isoxazolo[2,3-a]azepin-2-ylmethyl)-N,N-dimethylamine
CAS No. 179404-40-1 (cis-isomer)
项目整合开发状态: Preclinical
项目研究机构: Janssen (Ori...
参考文献标题:Substd.tetracyclic azepine derivs.which have affinity for 5-HT2 receptors
文献作者:Sipido,V.K.; Fernandez-Gadea,F.J.; Andres-Gil,J.I.; Meert,T.F.; Gil-Lopetegui,P.(Janssen Pharmaceutica NV)
参考来源:EP 0789701; JP 1998508308; US 5552399; WO 9614320

新产品编号:378607

Chemical Name: (?-cis-3-Phenyl-4-[4-[2-(1-pyrrolidinyl)ethylsulfanyl]phenyl]-3,4-dihydro-2H-1-benzopyran-7-ol hydrochloride
CAS No. 207294-76-6 ((-)-cis-isomer), 207295-32-7 ((+)-cis-isomer)
项目整...
参考文献标题:Synthesis and biological evaluation of novel thio-substituted chromanes as high-affinity partial agonists for the estrogen receptor
文献作者:Christiansen,L.B.; Weckens,M.; Bury,P.S.; Gissel,B.; Hansen,B.S.; Thorpe,S.M.; Jacobsen,P.; Kanstrup,A.; Jorgensen,A.S.; Naerum,L.; Wasserman,K.
参考来源:Bioorg Med Chem Lett 2002,12(1),17

FR-137316

Chemical Name: 4-Hydroxy-N,1-dimethyl-6-(methylsulfanyl)-2-oxo-N-phenyl-1,2-dihydroquinoline-3-carboxamide
CAS No. 147079-63-8
项目整合开发状态: Preclinical
项目研究机构: Fujisawa (Originator)
合成路线:Nucl...
参考文献标题:Quinoline derivs.
文献作者:Matsuo,M.; Tsuji,K.; Nakamura,K.; Spears,G.W.(Fujisawa Pharmaceutical Co.,Ltd.)
参考来源:EP 0639182; JP 1994506925; WO 9218483

新产品编号:854789

Chemical Name: 1,1'-O-(1,7-Dioxoheptane-1,7-diyl)-bis[2,3,4,6-tetrakis-O-(3,4,5-trihydroxybenzoyl)-beta-D-glucopyranose]
CAS No. 341035-06-1
项目整合开发状态: Preclinical
项目研究机构: Pennsylvania State U...
参考文献标题:Gallotannins and ellagitannins as regulators of cytokine release
文献作者:Feldman,K.S.(Penn State Research Foundation)
参考来源:WO 0136436

HPH-Pep

Chemical Name: N,N'-(Pyridin-2,6-diyl)bis(carbonyl)bis(L-histidine) dimethyl diester
CAS No. 185031-56-5, 346607-04-3 (hydrate)
项目整合开发状态: Biological Testing
项目研究机构: Kumamoto University (Origi...
参考文献标题:An artificial Cu(II) complex with intriguing oxygen radical-quenching profile.X-ray structure,cytochrome c assay,and ESR study
文献作者:Otsuka,M.; Satake,H.; Murakami,S.; Doi,M.; Ishida,T.; Shibasaki,M.; Sugiura,Y.
参考来源:Bioorg Med Chem 1996,4(10),1703

新产品编号:601669

Chemical Name: 1,1'-(1,4-Phenylene)bis[2-[(3R,5aS,6R,8aS,9R,10S,12R,12aR)-3,6,9-trimethyl-3,12-epoxyperhydropyrano[4,3-j]-1,2-benzodioxepin-10-yl]ethanone]
CAS No. 229981-82-2 (diastereomer)
项目整...
参考文献标题:New chemical and biological aspects of artemisinin-derived trioxane dimers
文献作者:Posner,G.H.; Northrop,J.; Paik,I.-H.; Borstnik,K.; Dolan,P.; Kensler,T.W.; Xie,S.; Shapiro,T.A.
参考来源:Bioorg Med Chem 2002,10(1),227

新产品编号:103339

Chemical Name: 2-(5-Methyl-2-phenyloxazol-4-ylmethoxy)-5-[3-(1H-tetrazol-5-yl)propyl]pyridine
CAS No. 166254-17-7
项目整合开发状态: Preclinical
项目研究机构: Takeda (Originator)
合成路线:Coupling of 2-chlor...
参考文献标题:Tetrazole derivs.,their production and use
文献作者:Sohda,T.; Ikeda,H.; Momose,Y.(Takeda Chemical Industries,Ltd.)
参考来源:CA 2125549; EP 0629624; JP 1995053555; US 5591862