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

RPR-131247

Chemical Name: 4-Hydroxy-3-[2-oxo-3(S)-(thieno[3,2-b]pyridin-2-ylsulfonamido)pyrrolidin-1-ylmethyl]benzamidine
CAS No. 205054-04-2, 205054-05-3 (trifluoroacetate)
项目整合开发状态: Biological Testing 参考文献标题:Substd.sulfonic acid N-[(aminoiminomethyl)phenylalkyl]-azaheterocyclamide cpds.
文献作者:Ewing,W.R.; Becker,M.R.; Choi-Sledeski,Y.M.; Pauls,H.W.; McGarry,D.G.; Davis,R.S.; Spada,A.P.(Aventis Pharma SA)
参考来源:EP 0894088; JP 2000505815; US 5731315; WO 9824784

NIP-141

Chemical Name: N-[(3R*,4S*)-4-(Cyclopropylamino)-3-hydroxy-2,2-dimethyl-7-nitro-3,4-dihydro-2H-1-benzopyran-6-yl]-2-(4-methoxyphenyl)acetamide hydrochloride
CAS No. 203002-58-8 (free base)
项目整合开...
参考文献标题:Chroman derivs.
文献作者:Tanikawa,K.; Ohrai,K.; Sato,M.; Yamashita,T.; Yanagihara,K.(Nissan Chemical Industry,Ltd.)
参考来源:EP 0934296; JP 1998087650; US 6066631; WO 9804542

5[Kpsi(CH2N)PR]-TASP, HB-19

Chemical Name: N2,N6-[H-L-Lys[psi(CH2N)]L-Pro-L-Arg]-L-Lys-L-Lys-N6-[H-L-Lys[psi(CH2N)]L-Pro-L-Arg]-L-Lys-Gly-L-Pro-N6-[H-L-Lys[psi(CH2N)]L-Pro-L-Arg]-L-Lys-L-Glu-N6-[H-L-Lys[psi(CH2N)]L-Pro-L-Arg]-L-...
参考文献标题:Inhibition of HIV infection by pseudopeptides blocking viral envelope glycoprotein-mediated membrane fusion and cell death
文献作者:Callebaut,C.; Jacotot,E.; Guichard,G.; Krust,B.; Rey-Cuille,M.; Cointe,D.; Benkirane,N.; Blanco,J.; Muller,S.; Briand,J.; Hovanessian,A.G.
参考来源:Virology 1996,218(1),181

TBC-3214

Chemical Name: N-(2-Acetyl-4,6-dimethylphenyl)-3-[N-(4-chloro-3-methylisoxazol-5-yl)sulfamoyl]thiophene-2-carboxamide
CAS No. 215501-47-6
项目整合开发状态: Preclinical
项目研究机构: Encysive Pharmaceutical...
参考文献标题:Sulfonamides for treatment of endothelin-mediated disorders
文献作者:Blok,N.; Keller,K.; Wu,C.; Kogan,T.; Woodard,P.(Texas Biotechnology Corp.)
参考来源:EP 0980369; US 5783705; WO 9849162

新产品编号:600087

Chemical Name: 1,1'-(1,4-Phenylene)bis[2-[(3R,5aS,6R,8aS,9R,10R,12R,12aR)-3,6,9-trimethyl-3,12-epoxyperhydropyrano[4,3-j]-1,2-benzodioxepin-10-yl]ethanone]
CAS No. 229981-82-2
项目整合开发状态: Preclini...
参考文献标题:C-10 carbon-substd.artemisinin-like trioxane cpds.having antimalarial,antiproliferative and antitumour activities
文献作者:Parker,M.H.; Shapiro,T.A.; Ploypradith,P.; Posner,G.H.; Northrup,J.; Daughenbaugh,R.J.; Woo,S.H.; Murray,C.; Elias,J.S.; Zheng,Q.Y.(Hauser,Inc.; Johns Hopkins University)
参考来源:EP 1043988; WO 9933461

新产品编号:339057

Chemical Name: 4-[N-(2,2,4,4-Tetramethyl-3,4-dihydro-2H-1-benzothiopyran-6-yl)carbamoyl]benzoic acid methyl ester
CAS No. 203855-93-0
项目整合开发状态: Preclinical
项目研究机构: Oklahoma State University (...
参考文献标题:Heteroarotinoids - Anticancer agents with receptor specificity and TGASE activity
文献作者:Nelson,E.C.; Madler,M.M.; Subramanian,S.; Birckbichler,P.J.; Berlin,K.D.; Patterson,M.K.Jr.; Benbrook,D.M.(Oklahoma State University)
参考来源:WO 9807716

PPO-294

Chemical Name: 6-Ethyl-6-phenylpyrido[3,2-b]pyrrolo[1,2-d][1,4]oxazepin-7(6H)-one
CAS No. 252010-39-2
项目整合开发状态: Preclinical
项目研究机构: Ist. di Ricerche Farmacol. Mario Negri (Originator)
合成路线...
参考文献标题:Pyrrolobenzoxazepinone derivatives as non-nucleoside HIV-1 RT inhibitors: Further structure-activity relationship studies and identification of more potent broad-spectrum HIV-1 RT inhibitors with antiviral activirty
文献作者:Campiani,G.; Morelli,E.; Fabbrini,M.; Nacci,V.; Greco,G.; Novellino,E.; Ramunno,A.; Maga,G.; Spadari,S.; Caliendo,G.; Bergamini,A.; Faggioli,E.; Uccella,I.; Bolacchi,F.; Marini,S.; Coletta,M.; Nacca,A.; Caccia,S.
参考来源:J Med Chem 1999,42(21),4462

R-2HMP

Chemical Name: N-Methyl-N-[1(R)-methylhexyl]-N-(2-propynyl)amine hydrochloride
CAS No. 7601-64-1 (racemate), 7665-88-5 (racemic free base)
项目整合开发状态: Preclinical
项目研究机构: University of Saskatch...
参考文献标题:Aliphatic propargylamines as selective MAO-B inhibitors and as neuroprotective agents
文献作者:Yu,P.H.; Davis,B.A.; Boulton,A.A.(University of Saskatchewan)
参考来源:JP 1994505241; US 5169868; WO 9215551

NGD-98-1

Chemical Name: N-[2-(Dimethylamino)ethyl]-N-isobutyl-N-[2-methyl-9-(2,4,6-trimethylphenyl)-9H-pyrido[2,3-b]indol-4-yl]amine
CAS No. 245733-79-3
项目整合开发状态: Preclinical
项目研究机构: Neurogen (Origina...
参考文献标题:Aminoalkyl substd.9H-pyridino[2,3-b]indole and 9H-pyrimidino[4,5-b]indole derivs.
文献作者:Darrow,J.W.; Maynard,G.D.; Horvath,R.F.(Neurogen Corp.)
参考来源:EP 1068207; US 6147085; WO 9951600

RP-463

Chemical Name: Trisodium (OC-6-54)-[N-formyl-L-methionyl-L-leucyl-L-phenylalanyl-N6-[6-(diazenyl-kappaN2)pyridin-3-ylcarbonyl]-L-lysinato(2-)][N-[2-hydroxy-1,1-bis(hydroxy-kappaO-methyl)ethyl]glycinat...
参考文献标题:RP463: A stabilized technetium-99m complex of a hydroazino nicotinamide derivatized chemotactic peptide for infection imaging
文献作者:Edwards,D.S.; et al.
参考来源:Bioconjugate Chem 1999,10(5),884