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

A-222977

Chemical Name: 10-Methoxy-2,2,4-trimethyl-5-[3-(methylsulfanylmethoxy)phenyl]-2,5-dihydro-1H-1-benzopyran[3,4-f]quinoline
CAS No. 239067-64-2
项目整合开发状态: Preclinical
项目研究机构: Abbott (Originator)...
参考文献标题:Glucocorticoid-selective anti-inflammatory agents
文献作者:Wang,A.X.; Kym,P.R.; Jones,T.K.; Kort,M.E.; Edwards,J.P.; Moore,J.L.; Elmore,S.W.; Coughlan,M.J.; Pratt,J.K.(Abbott Laboratories Inc.; Ligand Pharmaceuticals,Inc.)
参考来源:EP 1053239; WO 9941256

KT6-207

Chemical Name: N-[4-[2-[2-[3,5-Bis(tert-butyl)-4-hydroxyphenyl]-5-methyloxazol-4-yl]ethoxy]phenyl]-1,1,1-trifluoromethanesulfonamide
CAS No. 350672-38-7
项目整合开发状态: Preclinical
项目研究机构: Kotobuki...
参考文献标题:Ether or amide derivs.,their preparation method and therapeutic agent for diabetes containing them
文献作者:Kuroiwa,K.; Tomiyama,H.; Tomiyama,T.(Kotobuki Pharmaceutical Co.,Ltd.)
参考来源:DE 10100772; JP 2001261662

KF-72926

Chemical Name: 2-Cyclopentyl-4-propyl-8(R)-(pyridin-4-ylmethyl)-4,5,7,8-tetrahydro-1H-imidazo[2,1-i]purin-5-one D-tartrate
CAS No. 349554-69-4, 348165-49-1 (free base)
项目整合开发状态: Preclinical
项...
参考文献标题:Fused purine derivs.
文献作者:Nomoto,Y.; Nakanishi,S.; Ohta,Y.; Ogawa,A.; Suzuki,C.; Ueno,K.; Yano,H.; Kusaka,H.; Takasaki,K.(Kyowa Hakko Kogyo Co.,Ltd.)
参考来源:EP 1251130; WO 0147931

CP-671906-01

Chemical Name: N-[3-(2,6-Dichloro-4-methoxyphenyl)-2,5-dimethylpyrazolo[1,5-a]pyrimidin-7-yl]-N'-(tetrahydro-2H-pyran-4-yl)ethane-1,2-diamine
CAS No. 332178-44-6, 332178-43-5 (hydrochloride)
项目整...
参考文献标题:Certain alkylene diamine-substd.pyrazolo[1,5-a]-1,5-pyrimidines and pyrazolo[1,5-a]-1,3,5-triazines
文献作者:Giangiordano,M.; Tran,J.; Darrow,J.W.; De Lombaert,S.; Blum,C.; Griffith,D.A.; Carpino,P.A.(Neurogen Corp.; Pfizer Inc.)
参考来源:US 6372743; WO 0123387

LY-503429

Chemical Name: N-[2(S)-Fluoro-2-[3'-(methylsulfonamido)biphenyl-4-yl]propyl]propane-2-sulfonamide
CAS No. 305446-95-1 (enantiomer), 305447-00-1 (enantiomer), 305447-26-1 (undefined isomer)
项目整合开...
参考文献标题:Monofluoroalkyl derivs.
文献作者:Jones,W.D.; Mitchell,D.; Fray,A.H.; Miller,W.D.; Cantrell,B.E.; Bender,D.M.; Zimmerman,D.M.; Simon,R.L.; Zarrinmayeh,H.(Eli Lilly and Company)
参考来源:EP 1183232; WO 0066546

A-324920

Chemical Name: 1-[2-[2,3-Dichloro-4-[trans-2-[N-[3-(2-oxopyrrolidin-1-yl)propyl]carbamoyl]cyclopropyl]phenylsulfanyl]phenyl]piperidine-3-carboxylic acid
CAS No. 350592-74-4, 350492-06-7 (diastereom...
参考文献标题:Discovery and SAR of diarylsulfide cyclopropylamide LFA-1/ICAM-1 interaction antagonists
文献作者:Link,J.T.; Sorensen,B.K.; Liu,G.; Pei,Z.; Reilly,E.B.; Leitza,S.; Okasinski,G.
参考来源:Bioorg Med Chem Lett 2001,11(8),973

新产品编号:876937

Chemical Name: 1-[4-(4-Fluorophenoxy)benzyl]-2-oxoimidazolidine-4(R)-carbohydroxamic acid
CAS No. 352665-40-8
项目整合开发状态: Biological Testing
项目研究机构: Pfizer (Originator)
合成路线:The alkylation o...
参考文献标题:Imidazolylbenzophenone derivs.
文献作者:Amada,H.; Miyata,N.; Kobayashi,Y.; Ishii,T.; Sato,M.(Taisho Pharmaceutical Co.,Ltd.)
参考来源:WO 0168610

BAL-1198, RO-0791198

Chemical Name: Cyclo[D-alanyl-L-tyrosyl-L-valyl-4(R)-hydroxy-L-prolyl-D-allothreonyl-L-threonyl-3(S)-hydroxy-L-prolyl-3(R)-hydroxy-L-glutaminyl-glycyl-D-allothreonyl-Ndelta-(2-aminoethyl)-Ndelta-[N2,N...
参考文献标题:Novel cyclic cpds.
文献作者:Okada,T.; Shimma,N.; Murata,T.; Masubuchi,K.; Kohchi,M.(Basilea Pharmaceutica AG)
参考来源:EP 1254161; WO 0153322

NMI-1093

Chemical Name: 4-[5-(Nitrooxymethyl)-3-phenylisoxazol-4-yl]benzenesulfonamide
CAS No. 346683-70-3
项目整合开发状态: Preclinical
项目研究机构: NitroMed (Originator)
合成路线:Treatment of deoxybenzoin (I) wit...
参考文献标题:Nitrosated and nitrosylated cyclooxygenase-2 inhibitors,compsns.and methods of use
文献作者:Garvey,D.S.; Tam,S.W.; Letts,L.G.; Schroeder,J.D.; Bandarage,U.K.; Fang,X.; Bandarage,R.R.(NitroMed Inc.)
参考来源:WO 0145703

新产品编号:883265

Chemical Name: P1-[2-Acetamido-3-O-[(2-carboxypropyl)(hydroxy)phosphorylmethyl]-2-deoxy-alpha-D-glucopyranosyl]-P2-(uridin-5'-yl)diphosphate
CAS No. 356785-78-9
项目整合开发状态: Biological Testing
项...
参考文献标题:Inhibitors of the bacterial cell wall biosynthesis enzyme MurC
文献作者:Reck,F.; Marmor,S.; Fisher,S.; Wuonola,M.A.
参考来源:Bioorg Med Chem Lett 2001,11(11),1451