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

RWJ-58259

Chemical Name: N1-[3-Amino-1(S)-(benzylcarbamoyl)propyl]-Nalpha-[N-[1-(2,6-dichlorobenzyl)-3-(1-pyrrolidinylmethyl)-1H-indazol-6-yl]carbamoyl]-3,4-difluoro-L-phenylalaninamide
CAS No. 315203-31-7, ...
参考文献标题:Novel indazole peptidomimetics as thrombin receptor antagonists
文献作者:Zhang,H.-C.; Pandey,A.; Scarborough,R.M.; Maryanoff,B.E.(COR Therapeutics,Inc.; Ortho-McNeil Pharmaceutical,Inc.)
参考来源:WO 0100656

新产品编号:674441

Chemical Name: N-(3-Carboxypropionyl)-L-aspartyl-L-glutamyl-(2-methyl)-L-phenylalanyl-(3-methyl)-L-valyl-N1-[1(S)-(2-amino-2-oxoacetyl)pentyl]-L-leucinamide
CAS No. 254439-45-7
项目整合开发状态: Biologi...
参考文献标题:alpha-Ketoamide derivs.
文献作者:Jones,P.S.; Kay,P.B.; Wilson,F.X.; Raynham,T.M.; Hurst,D.N.(Hoffmann-La Roche,Inc.)
参考来源:US 6187905

新产品编号:266285

Chemical Name: N-Benzyl-N,3-dimethyl-4-phenylquinoline-2-carboxamide
CAS No. 194223-70-6
项目整合开发状态: Preclinical
项目研究机构: Universit?degli Studi di Catanzaro (Originator), Universit?degli Studi d...
参考文献标题:Mapping the peripheral benzodiazepine receptor binding site by conformationally restrained derivatives of 1-(2-chlorophenyl)-N-methyl-N-(1-methylpropyl)-3-isoquinolinecarboxamide (PK11195)
文献作者:Cappelli,A.; Anzini,M.; Vomero,S.; De Benedetti,P.G.; Menziani,M.C.; Giorgi,G.; Manzoni,C.
参考来源:J Med Chem 1997,40(18),2910

新产品编号:821567

Chemical Name: 4-(2,2-Dimethyl-1-oxopropyl)benzoic acid 2-[4-(2,2-dimethyl-1-oxopropyl)benzoyloxymethyl]-1,4-butanediyl diester
CAS No. 328397-37-1
项目整合开发状态: Preclinical
项目研究机构: Novartis (Ori...
参考文献标题:Reduction in glucose levels in STZ diabetic rats by 4-(2,2-dimethyl-1-oxopropyl)benzoic acid: A prodrug approach for targeting the liver
文献作者:Bebernitz,G.R.; Dain,J.G.; Deems,R.O.; Otero,D.A.; Simpson,W.R.; Strohschein,R.J.
参考来源:J Med Chem 2001,44(4),512

新产品编号:850043

Chemical Name: (Tricarbonyl)[(1,2,3,4,5-eta)-3-[1-(4-hydroxyphenyl)-1-[4-[4-(dimethylamino)butoxy]phenyl]-1-buten-2-yl]-2,4-cyclopentadien-1-yl]rhenium
CAS No. 339320-31-9 ((E)-isomer), 339320-29-5...
参考文献标题:First anti-oestrogen in the cyclopentadienyl rhenium tricarbonyl series.Synthesis and study of antiproliferative effects
文献作者:Jaouen,G.; et al.
参考来源:Chem Commun (London) 2001,(4),383

BMS-200532, MC-134-248

Chemical Name: 3(S)-Benzamido-2(R)-hydroxybenzenepropionic acid (2aR,4S,4aS,6R,9S,11S, 12S,12aR,12bS)-6-acetoxy-12b-(cyclopropylcarbonyloxy)-12-(2,4-difluorobenzoyloxy)-4,11-dihydroxy-4a,8,13,13- tetr...
参考文献标题:Synthesis and bioactivity of 2,4-diacyl analogues of paclitaxel
文献作者:Chordia,M.D.; Yuan,H.; Jagtap,P.G.; Kadow,J.F.; Long,B.H.; Fairchild,C.R.; Johnston,K.A.; Kingston,D.G.I.
参考来源:Bioorg Med Chem 2001,9(1),171

JI-38

Chemical Name: N-[3-(4-Hydroxyphenyl)propionyl]-L-alanyl-L-aspartyl-L-alanyl-L-isoleucyl-L-phenylalanyl-L-threonyl-L-glutaminyl-L-seryl-L-tyrosyl-L-arginyl-L-ornithyl-L-valyl-L-leucyl-L-(2-aminobutyry...
参考文献标题:Heterocyclycarboxamides and other cpds.for the treatment of the cardiac arrhythmias
文献作者:Nadler,G.M.M.G.(GlaxoSmithKline plc)
参考来源:WO 9627595

RPR-132552

Chemical Name: (3R,4R,5E,10E,12E,14S,16R,26aR)-16-Fluoro-14-hydroxy-3-isopropyl-4,12-dimethyl-3,4,8,9,14,15,16,17,24,25,26,26a-dodecahydro-7H-21,18-nitrilo-1H,22H-pyrrolo[2,1-c][1,8,4,19]dioxadiazacyc...
参考文献标题:Streptogramin derivs.,preparation and compsns.containing them
文献作者:Barriere,J.-C.; Achard,D.; Grisoni,S.; Bacque,E.; Ribeill,Y.; Bouquerel,J.; Desmazeau,P.; Leconte,J.-P.; Ronan,B.(Aventis Pharma SA)
参考来源:EP 1187847; FR 2795733; WO 0102427

KTC-5

Chemical Name: 5-Ethyl-4-methoxy-2-phenylquinoline
CAS No. 336100-71-1
项目整合开发状态: Preclinical
项目研究机构: Chang Gung University (Originator), China Medical College (Originator), National Taiwan Un...
参考文献标题:Synthesis of 4-alkoxy-2-phenylquinoline derivatives as potent antiplatelet agents
文献作者:Ko,T.-C.; Hour,M.J.; Lien,J.C.; Teng,C.M.; Lee,K.H.; Kuo,S.C.; Huang,L.J.
参考来源:Bioorg Med Chem Lett 2001,11(3),279

CPT-154

Chemical Name: 4(S)-Ethyl-4-hydroxy-11-[(E)-(phenylimino)methyl]-1H-pyrano[3',4':6,7]indolizino[1,2-b]quinoline-3,14(4H,12H)-dione; 7-(Phenyliminomethyl)camptothecin
CAS No. 292620-93-0
项目整合开发状态...
参考文献标题:Camptothecin derivs.having antitumor activity
文献作者:Carminati,P.; Penco,S.; Zunino,F.; Merlini,L.(Istituto Nazionale per lo Studio e la Cura dei Tumori; Sigma-Tau Industrie Farmaceutiche Riunite SpA)
参考来源:EP 1044977; WO 0053607