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

HI-281

Chemical Name: 6-(3,5-Dimethylbenzyl)-5-isopropyl-2-(methylsulfanylmethylsulfanyl)-4(3H)-pyrimidinone
CAS No. 210645-96-8
项目整合开发状态: Biological Testing
项目研究机构: Parker Hughes Institute (Origina...
参考文献标题:Structure-based design of novel dihydroalkoxybenzyloxopyrimidine derivatives as potent nonnucleoside inhibitors of the human immunodeficiency virus reverse transcriptase
文献作者:Sudbeck,E.A.; Mao,C.; Vig,R.; Venkatachalam,T.K.; Tuel-Ahlgren,L.; Uckun,F.M.
参考来源:Antimicrob Agents Chemother 1998,42(12),3225

DDE-240, F-PBT, HI-240

Chemical Name: N-(5-Bromo-2-pyridinyl)-N'-[2-(2-fluorophenyl)ethyl]thiourea
CAS No. 219664-37-6
项目整合开发状态: Preclinical
项目研究机构: Parker Hughes Institute (Originator)
合成路线:2-Amino-5-bromopyrid...
参考文献标题:NNI for treatment of multi-drug resistant HIV
文献作者:Uckun,F.M.(Parker Hughes Institute)
参考来源:WO 0056736

BIO-1211

Chemical Name: N-[4-[3-(2-Methylphenyl)ureido]phenylacetyl]-L-leucyl-L-aspartyl-L-valyl-L-proline
CAS No. 187735-94-0
项目整合开发状态: Phase II
项目研究机构: Biogen Idec (Originator), Merck & Co. (Codevel...
参考文献标题:Cell adhesion inhibitor
文献作者:Lin,K.-C.; Adams,S.P.; Castro,A.C.; Zimmerman,C.N.; Cuervo,J.H.; Lee,W.-C.; Hammond,C.E.; Carter,M.B.; Almquist,R.G.; Ensinger,C.L.(Biogen,Inc.)
参考来源:EP 0842196; JP 1999511124; WO 9703094

新产品编号:726647

Chemical Name: 1-(4-Amino-5-hexenoyl)piperidine-3-carboxylic acid methyl ester
CAS No. 270905-51-6
项目整合开发状态: Preclinical
项目研究机构: Dong Kook (Originator)
合成路线:Boc-protected vigabatrin (II) w...
参考文献标题:Design and synthesis of anticonvulsive agents as gamma-Vinyl GABA-based potential dual acting prodrugs and their biological activities
文献作者:Kim,Y.; Zhao,L.X.; Kim,T.H.; Je,S.M.; Kim,E.K.; Choi,H.; Chae,W.G.; Park,M.; Choi,J.; Jahng,Y.; Lee,E.S.
参考来源:Bioorg Med Chem Lett 2000,10(7),609

3-Allyl farnesol, 3-alFOH

Chemical Name: (2Z,6E)-7,11-Dimethyl-3-(2-propenyl)-2,6,10-dodecatrien-1-ol
CAS No. 247942-40-1
项目整合开发状态: Biological Testing
项目研究机构: Karmanos Cancer Institute (Originator), Purdue University ...
参考文献标题:Novel farnesol and geranylgeraniol analogues: A potential new class of anticancer agents directed against protein prenylation
文献作者:Gibbs,B.S.; Zahn,T.J.; Mu,Y.; Sebolt-Leopold,J.S.; Gibbs,R.A.
参考来源:J Med Chem 1999,42(19),3800

MF-569, 3-IAABU

Chemical Name: N-[3-(Iodoacetamido)benzoyl]urea; N-Carbamoyl-3-(2-iodoacetamido)benzamide
CAS No. 218935-77-4
项目整合开发状态: Biological Testing
项目研究机构: Cytoskeleton (Originator), Mount Sinai Schoo...
参考文献标题:Synthesis,cancericidal and antimicrotubule activities of 3-(haloacetamido)-benzoylureas
文献作者:Bekesi,J.G.; Holland,J.F.; Jiang,J.-D.; Ma,L.; Roboz,J.; Deng,L.; Weisz,I.
参考来源:Anti-Cancer Drug Des 1998,13(7),735

PMT-13

Chemical Name: 5-[4-[2-[2-Ethyl-4-methyl-6-oxo-1,6-dihydro-1-pyrimidinyl]ethoxy]benzyl]thiazolidine-2,4-dione
CAS No. 199113-95-6, 199114-09-5 (sodium salt)
项目整合开发状态: Preclinical
项目研究机构: Dr. ...
参考文献标题:Heterocyclic cpds.,process for their preparation and pharmaceutical compsns.containing them and their use in the treatment of diabetes and related diseases
文献作者:Lohray,V.B.; Lohray,B.B.; Ramanujam,R.; Chakrabarti,R.; Gurram,R.M.; Paraselli,R.B.; Pakala,S.K.S.(Dr.Reddy's Research Foundation)
参考来源:EP 0958296; US 5885997; US 5985884; US 6372750; US 6573268; WO 9741097

R-116010

Chemical Name: N-[4-[2(S)-(Dimethylamino)-1(S)-(1H-imidazol-1-yl)propyl]phenyl]benzothiazol-2-amine; N-(2-Benzothiazolyl)-N-[4-[2(S)-(dimethylamino)-1(S)-(1H-imidazol-1-yl)propyl]phenyl]amine
CAS N...
参考文献标题:N-[4-(heteroarylmethyl)phenyl]-heteroarylamines
文献作者:Venet,M.G.; Mabire,D.J.-P.; Lacrampe,J.F.A.; Sanz,G.C.(Janssen Pharmaceutica NV)
参考来源:EP 0907650; JP 2000503670; US 6124330; WO 9749704

MLN-944, XR-5944

Chemical Name: N,N'-(1,2-Ethanediy)bis(imino-2,1-ethanediyl)bis(9-methylphenazine-1-carboxamide)
CAS No. 206531-58-0 (monohydrochloride)
项目整合开发状态: Phase I
项目研究机构: Xenova (Originator), Millenn...
参考文献标题:Bis(acridinecarboxamide) and bis(phenazinecarboxamide) as antitumour agents
文献作者:Denny,W.A.; Gamage,S.A.; Spicer,J.A.; Baguley,B.C.; Finlay,G.J.(Xenova Group plc)
参考来源:EP 0934278; GB 2334032; WO 9817650

TMC-95A

Chemical Name: (10S,11R,12S,15S,18S)-15-(Carbamoylmethyl)-10,11,23-trihydroxy-18-[3(S)-methyl-2-oxopentanamido]-9,14,17-trioxo-N-[1(Z)-propenyl]-8,13,16-triazatetracyclo[18.3.1.0(2,7).0(6,10)]tetracos...
参考文献标题:The total synthesis of proteasome inhibitors TMC-95A and TMC-95B: Discovery of a new method to generate cis-propenyl amides
文献作者:Lin,S.N.; Danishefsky,S.J.
参考来源:Angew Chem.Int Ed Engl 2002,41(3),512