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:930725

Chemical Name: (+)-cis-2-(2-Adamantyl)-4-(3,4-dimethoxyphenyl)-1,2,4a,5,8,8a-hexahydrophthalazin-1-one
CAS No. 415927-51-4, 415927-52-5 (enantiomer), 415927-50-3 (racemate)
项目整合开发状态: Preclinical...
参考文献标题:Novel selective phosphodiesterase (PDE4) inhibitors.4.Resolution,absolute configuration,and PDE4 inhibitory activity of cis- tetra- and cis-hexahydrophthalazinones
文献作者:Van der Mey,M.; Boss,H.; Couwenberg,D.; Hatzelmann,A.; Sterk,G.J.; Goubitz,K.; Schenk,H.; Timmerman,H.
参考来源:J Med Chem 2002,45(12),2526

DR-4365

Chemical Name: N,N-Dimethyl-2-[4-[2-oxo-1,2,2a,3,4,5-hexahydrobenzo[cd]indol-2-yl]butyl]-2,3,4,9-tetrahydro-1H-beta-carboline-9-carboxamide
CAS No. 230300-64-8, 247082-25-3 ((S)-isomer)
项目整合开发状态...
参考文献标题:Tetrahydrobenzindole derivs.
文献作者:Koyama,M.; Okuno,M.; Hiranuma,T.; Ando,T.; Fuji,K.; Ushiroda,O.; Kikuchi,C.; Shiiyama,M.; Satoh,E.(Meiji Seika Kaisha,Ltd.)
参考来源:EP 1057814; JP 1999189585; US 6498251; WO 9933804

新产品编号:905413

Chemical Name: N-[4(S)-[N-[2-(1-Naphtyl)acetyl]-3-methyl-L-valylamino]-3(R)-hydroxy-2(R)-(3,4,5-trimethoxybenzylamino)-5-phenylpentanoyl]-L-valine 2-hydroxy-4-methoxybenzylamide
CAS No. 376644-14-3...
参考文献标题:2-Amino-3-hydroxy-4-tert-leucyl-amino-5-phenyl-pentanoic acid amide derivs.
文献作者:Lang,M.; Zimmermann,J.; Furet,P.; Garcia-Echeverria,C.; Imbach,P.(Novartis AG; Novartis Pharma GmbH)
参考来源:EP 1290012; US 2003166572; WO 0189282

YW-355

Chemical Name: (?-N-[2-[1-(Chloromethyl)-5-hydroxy-2,3-dihydro-1H-benzo[e]indol-3-ylcarbonyl]-1H-indol-5-yl]-5-nitro-1-benzofuran-2-carboxamide
CAS No. 500536-50-5
项目整合开发状态: Preclinical
项目研究机...
参考文献标题:CC-1065 analogues bearing different DNA-binding subunits: Synthesis,antitumor activity,and preliminary toxicity study
文献作者:Wang,Y.; Li,L.; Ye,W.; Tian,Z.; Jiang,W.; Wang,H.; Wright,S.C.; Larrick,J.W.
参考来源:J Med Chem 2003,46(4),634

L-870810

Chemical Name: 5-(1,1-Dioxoperhydro-1,2-thiazin-2-yl)-N-(4-fluorobenzyl)-8-hydroxy-1,6-naphthyridine-7-carboxamide
CAS No. 410544-95-5, 410545-86-7 (Na salt)
项目整合开发状态: Phase I
项目研究机构: Merck &...
参考文献标题:Aza- and polyaza-naphthalenyl carboxamides useful as HIV integrase inhibitors
文献作者:Young,S.D.; Guare,J.P.; Wai,J.S.; Fisher,T.E.; Perlow,D.S.; Anthony,N.J.; Egbertson,M.; Gomez,R.P.; Kuo,M.S.; Tran,L.; Zhuang,L.; Langford,H.M.; Melamed,J.Y.; Bennett,J.J.; Embrey,M.; Jolly,S.M.; Funk,T.W.(Merck & Co.,Inc.)
参考来源:WO 0230930; WO 0230931

T-226296

Chemical Name: (-)-N-[6-(Dimethylaminomethyl)-5,6,7,8-tetrahydronaphthalen-2-yl]-4'-fluorobiphenyl-4-carboxamide
CAS No. 331758-35-1, 331756-51-5 (undefined isomer), 331757-36-9 (undefined isomer m...
参考文献标题:Melanin concentrating hormone antagonist
文献作者:Kato,K.; Mori,M.; Suzuki,N.; Ishihara,Y.; Shimomura,Y.; Terauchi,J.; Takekawa,S.(Takeda Chemical Industries,Ltd.)
参考来源:JP 2002003370; WO 0121577

新产品编号:927561

Chemical Name: (3R,5aS,6R,8aS,9R,10R,12R,12aR)-3,6,9-Trimethyl-10-(trifluoromethyl)perhydro-3,12-epoxypyrano[4,3-j]-1,2-benzodioxepine; 10-Deoxo-10(R)-(trifluoromethyl)artemisin
CAS No. 408347-40-0...
参考文献标题:First synthesis of 10alpha-(trifluoromethyl)deoxoartemisinin
文献作者:Chorki,F.; Grellepois,F.; Crousse,B.; Hoang,V.D.; Van Hung,N.; Bonnet-Delpon,D.; Begue,J.-P.
参考来源:Org Lett 2002,4(5),757

新产品编号:908577

Chemical Name: 3-(Methylsulfanyl)-4-(2-propynylselanyl)quinoline
CAS No. 381246-67-9
项目整合开发状态: Preclinical
项目研究机构: Medical University of Silesia (Originator), Polish Academy of Science (Origi...
参考文献标题:Synthesis and antiproliferative activity in vitro of new propargyl thioquinolines
文献作者:Boryczka,S.; Wietrzyk,J.; Opolski,A.
参考来源:Pharmazie 2002,57(3),151

新产品编号:324819

Chemical Name: 5-[3,5-Bis(trifluoromethyl)phenyl]-4-(5-chloro-2-hydroxyphenyl)-3,4-dihydro-2H-1,2,4-triazol-3-one
CAS No. 202821-61-2
项目整合开发状态: Biological Testing
项目研究机构: Bristol-Myers Squibb...
参考文献标题:Diphenyl oxadiazolones as potassium channel modulators
文献作者:Meanwell,N.A.; Starrett,J.E.Jr.; Hewawasam,P.; Romine,J.L.; Martin,S.W.; Gribkoff,V.K.(Bristol-Myers Squibb Co.)
参考来源:JP 2000516925; US 5869509; WO 9804135

新产品编号:889593

Chemical Name: 8-(4'-Bromobiphenyl-4-yl)-8-oxooctanohydroxamic acid
CAS No. 362670-51-7
项目整合开发状态: Biological Testing
项目研究机构: MethylGene (Originator)
合成路线:The reaction of ethyl 7-bromohepta...
参考文献标题:Inhibitors of histone deacetylase
文献作者:Delorme,D.; Woo,S.H.; Vaisburg,A.(MethylGene Inc.)
参考来源:WO 0170675