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

RP-60556A

Chemical Name: 7-Fluoro-8-[4-(4-fluorophenyl)piperazin-1-yl]-1-methyl-4-oxo-1,4-dihydrobenzo[b][1,8]naphthyridine-3-carboxylic acid 2-hydroxy-N,N,N-trimethyl-1-ethanaminium salt
CAS No. 278795-92-9...
参考文献标题:1,8-Benzonaphthyridine derivs.
文献作者:Wentzler,S.; Desconclois,J.-F.; Girard,P.; Picaut,G.; Tabart,M.(Aventis Pharma SA)
参考来源:FR 2787452; WO 0037467

Lamectacin, NB-2001

Chemical Name: (6R,7R)-3-[5-Chloro-2-(2,4-dichlorophenoxy)phenoxymethyl]-7-[2-(2-thienyl)acetamido]-3-cephem-4-carboxylic acid
CAS No. 371914-92-0
项目整合开发状态: Preclinical
项目研究机构: NewBiotics (Or...
参考文献标题:Improved beta-lactam antibiotics
文献作者:Lobl,T.J.; Chan,M.F.; Li,Q.; Doppalapudi,V.R.; Hixon,M.S.; Castillo,R.(NewBiotics,Inc.)
参考来源:WO 0183492

SCH-226374

Chemical Name: 4-[8-Chloro-6,11-dihydro-5H-benzo[5,6]cyclohepta[1,2-b]pyridin-11(S)-yl]-2(R)-[N-benzyl-N-[3-(4-methyl-1H-imidazol-1-yl)propyl]carbamoyl]piperazine-1-carboxylic acid cyclohexyl ester 参考文献标题:Tricyclic farnesyl protein transferase inhibitors
文献作者:Guzi,T.; Taveras,A.G.; Ferreira,J.A.; Desai,J.A.; Wang,J.J.S.; Lalwani,T.; Alvarez,C.; Afonso,A.; Girijavallabhan,V.M.; Mallams,A.K.; Doll,R.J.; Weinstein,J.; Cooper,A.B.; Chao,J.; Rane,D.F.; Aki,C.J.; Kelly,J.M.(Schering Corp.)
参考来源:EP 1140902; WO 0037459

Gallium maltolate, GaM

Chemical Name: Tris[3-(hydroxy-kappaO)-2-methyl-4H-pyran-4-onato-kappaO4]gallium; Tris(3-hydroxy-2-methyl-4H-pyran-4-onato-O3,O4)gallium
CAS No. 108560-70-9
项目整合开发状态: Phase I/II
项目研究机构: Titan...
参考文献标题:Methods and compsns.to inhibit keratinocyte proliferation
文献作者:Bernstein,L.R.(GeoMed,Inc.)
参考来源:WO 9804263; WO 9804264

PNU-193821

Chemical Name: N-[5-[N-(2-Amidinoethyl)carbamoyl]-1-methyl-1H-pyrrol-3-yl]-4-[4-[3-[4-(2-chloroethylsulfanyl)phenyl]-2(E)-propenamido]-1-methyl-1H-pyrrol-2-ylcarboxamido]-1-methyl-1H-pyrrole-2-carboxa...
参考文献标题:Sulfurated distamycin derivs.,process for preparing them,and their use as antitumor agents
文献作者:Beria,I.; Caldarelli,M.; Capolongo,L.; Geroni,M.C.; Cozzi,P.(Pharmacia & Upjohn SpA)
参考来源:WO 0006541

新产品编号:770943

Chemical Name: (-)-2(R,S)-Methyloctanoic acid (2R,3R)-5,7-dihydroxy-2-(3,4,5-trihydroxyphenyl)-3,4-dihydro-2H-1-benzopyran-3-yl ester; (-)-3-O-[2(R,S)-Methyloctanoyl]epigallocatechin
CAS No. 299462...
参考文献标题:Antitumor promoting activities of 3-O-acyl-(-)-epigallocatechins
文献作者:Uesato,S.; Kitagawa,Y.; Hara,Y.; Tokuda,H.; Okuda,M.; Mou,X.Y.; Mukainaka,T.; Nishino,H.
参考来源:Bioorg Med Chem Lett 2000,10(15),1673

CGH-1484A

Chemical Name: N-[1(S)-(Benzothiazol-2-ylmethyl)-2-[4-(2-fluoroethyl)piperidin-1-yl]-2-oxoethyl]-3,3-dimethyl-6-[3-[4-[2-(4-morpholinyl)-2-oxoethyl]piperazin-1-yl]-3-oxopropyl]-1,2,3,4-tetrahydroquino...
参考文献标题:Tetrahydroquinoline inhibitors of trypsin and thrombin
文献作者:Smith,G.P.; Brundish,D.E.; Menear,K.A.; Walker,C.V.; Herold,P.; Fullerton,J.D.; Allen,M.C.; Le Grand,D.M.; Kane,P.D.; Cockcroft,X.-L.; Wathey,W.B.; Butler,P.I.; Hatto,J.D.I.; Hayler,J.D.(Novartis AG)
参考来源:GB 2312674

新产品编号:386517

Chemical Name: Benzyloxycarbonyl-L-aspartyl-L-valyl-L-3-(2-methylphenyl)alanyl-L-(3-methyl)valyl-L-leucine N-(1-boronopropyl)amide
CAS No. 208520-63-2
项目整合开发状态: Biological Testing
项目研究机构: Roc...
参考文献标题:Antiviral peptide derivs.
文献作者:Attwood,M.R.; Hurst,D.N.; Jones,P.S.; Kay,P.B.; Raynham,T.M.; Wilson,F.X.(F.Hoffmann-La Roche AG)
参考来源:JP 2000508344; WO 9822496

SPD-756, BCH-13520

Chemical Name: (-)-(2R,4R)-4-[2-Amino-6-(cyclopropylamino)-9H-purin-9-yl]-1,3-dioxolane-2-methanol; (-)-(2R,4R)-4-[2-Amino-6-(cyclopropylamino)-9H-purin-9-yl]-2-(hydroxymethyl)-1,3-dioxolane; N6-Cyclo...
参考文献标题:Antiviral nucleoside analogues
文献作者:Nguyen-Ba,N.(Shire BioChem Inc.)
参考来源:EP 1140937; JP 2002533470; US 6358963; WO 0039143

NNC-25-2504

Chemical Name: 3-Cyano-4-hydroxy-N'-[1-(2,3,5,6-tetramethylbenzyl)-1H-indol-4-ylmethylene]benzohydrazide
CAS No. 280134-25-0
项目整合开发状态: Preclinical
项目研究机构: Novo Nordisk (Originator), Pfizer (O...
参考文献标题:Glucagon antagonists/inverse agonists
文献作者:Lau,J.; Madsen,P.; Truesdale,L.K.; Sams,C.; Feng,J.; Kiel,D.; Ling,A.; Kukl,A.; Shi,S.; Plewe,M.B.; May,J.(Agouron Pharmaceuticals,Inc.; Novo Nordisk A/S)
参考来源:JP 2002533439; WO 0039088