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

Bamet-R2

Chemical Name: cis-Diamminechloro[N-[(3alpha,5beta,7alpha,12alpha)-3,7,12-trihydroxycholan-24-yl]glycinato-kappaO]platinum
CAS No. 191595-91-2
项目整合开发状态: Preclinical
项目研究机构: Universidad de Sal...
参考文献标题:Synthesis and characterization of the new cytostatic complex cis-diammineplatinum(II)-chlorocholylglycinate
文献作者:Criado,J.J.; et al.
参考来源:Bioconjugate Chem 1997,8(4),453

ORG-25935

Chemical Name: cis-N-(6-Methoxy-1-phenyl-1,2,3,4-tetrahydronaphthalen-2-ylmethyl)-N-methylglycine hydrochloride
CAS No. 258887-13-7 ((+)-(R*,S*)-isomer), 258886-37-2 (diastereomer), 258886-39-4 (di...
参考文献标题:Aminomethylcarboxylic acid derivs.
文献作者:Jaap,D.R.; Gilfillan,R.; Gibson,S.G.; Thorn,S.N.(Akzo Nobel N.V.)
参考来源:EP 1100769; WO 0007978

新产品编号:500421

Chemical Name: 6-Chloro-N-isopropyl-4H-thieno[2,3-e][1,2,4]thiadiazin-3-amine 1,1-dioxide
CAS No. 220105-82-8
项目整合开发状态: Biological Testing
项目研究机构: Novo Nordisk (Originator)
合成路线:The thioca...
参考文献标题:Fused 1,2,4-thiadiazine derivs.,their preparation and use
文献作者:Tagmose,T.M.; Hansen,H.C.; Nielsen,F.E.; Mogensen,J.P.; Hansen,J.B.(Novo Nordisk A/S)
参考来源:EP 1000066; JP 2001510195; WO 9903861

PD-174424

Chemical Name: N2-(Benzofuran-2-ylmethoxycarbonyl)-alpha-(dimethylaminomethyl)-N1-[1(S)-phenylethyl]-D-tryptophanamide hydrochloride; N-[1(S)-(Dimethylaminomethyl)-2-(1H-indol-3-yl)-1-[N-[1(S)-phenyle...
参考文献标题:Utilization of an intramolecular hydrogen bond to increase the CNS penetration of an NK1 receptor antagonist
文献作者:Ashwood,V.A.; Field,M.J.; Horwell,D.C.; Julien-Larose,C.; Lewthwaite,R.A.; McCleary,S.; Pritchard,M.C.; Raphy,J.; Singh,L.
参考来源:J Med Chem 2001,44(14),2276

新产品编号:590595

Chemical Name: 2-[4-[2(S)-[N-[1-(4-Methoxybenzyl)-4-methyl-2-oxo-1,2-dihydropyridin-3-yl]carbamoyl]-2-[2-methyl-2-(2-naphthyl)propionamido]ethyl]phenyl]-2-methylpropionic acid
CAS No. 228408-75-1, ...
参考文献标题:Pyridones as Src family SH2 domain inhibitors
文献作者:Betageri,R.; Llinas-Brunet,M.; Moss,N.; Patel,U.; Cardozo,M.; Beaulieu,P.L.; Ferland,J.-M.; Proudfoot,J.R.(Boehringer Ingelheim Pharmaceuticals Inc.)
参考来源:EP 1045836; US 6054470; US 6156784; WO 9931066

D-Fluviabactin

Chemical Name: N,N-Bis[3-(2,3-dihydroxybenzamido)propyl]-2-(2,3-dihydroxyphenyl)-5(S)-methyl-4,5-dihydrooxazole-4(R)-carboxamide
CAS No. 357628-58-1
项目整合开发状态: Preclinical
项目研究机构: University o...
参考文献标题:Synthesis of parabactin and homologs thereof
文献作者:Bergeron,R.J.Jr.(University of Florida)
参考来源:US 4565874

SCH-351125, Schering C, SCH-C

Chemical Name: (Z)-1-(4-Bromophenyl)-1-[1'-(2,4-dimethyl-1-oxidopyridin-3-ylcarbonyl)-4'-methyl-1,4'-bipiperidin-4-yl]methanone O-ethyloxime
CAS No. 305792-46-5
项目整合开发状态: Phase I
项目研究机构: Sche...
参考文献标题:Piperidine derivs.useful as CCR5 antagonists
文献作者:McCombie,S.W.; Clader,J.W.; Baroudy,B.M.; McKittrick,B.A.; Josien,H.B.; Tagat,J.R.; Vice,S.F.; Steensma,R.; Laughlin,M.A.; Miller,M.W.; Neustadt,B.R.; Palani,A.(Schering Corp.)
参考来源:EP 1175402; WO 0066559

Etozolin, W-2900A

Chemical Name: 2-[3-Methyl-4-oxo-5-(1-piperidinyl)thiazolidin-2-ylidene]acetic acid ethyl ester
CAS No. 1973-09-6
项目整合开发状态: Not Determined
项目研究机构:
合成路线:The cyclization of a mixture of eth...
参考文献标题:
文献作者:Satzinger,G.
参考来源:DE 1160441; FR M2728; GB 1022047; GB 1022048; US 3072653

CRL-42796

Chemical Name: N-[4-(4-Piperidinyl)-2-[2-(4-piperidinyl)ethyl]butyryl]glycyl-2(S)-(naphthalen-2-ylsulfonyl)-beta-alanine dihydrochloride
CAS No. 255879-67-5, 255880-36-5 (diHCl)
项目整合开发状态: Precli...
参考文献标题:Bispiperidines as antithrombotic agents
文献作者:Lesur,B.; Henry,M.; Yue,C.; Giboulot,T.(Laboratoires L.Lafon)
参考来源:EP 1098878; FR 2781223; JP 2002520393; US 6333338; WO 0003986

S-35120

Chemical Name: 3-[6-(4-Chlorophenylsulfonamido)-3-[2-[4-(6-fluoro-1,2-benzisoxazol-3-yl)piperidin-1-yl]ethyl]-5,6,7,8-tetrahydronaphthalen-1-yl]propionic acid
CAS No. 351184-68-4
项目整合开发状态: Precl...
参考文献标题:Benzenesulfonamide derivs.,process for their preparation and pharmaceutical compsns.containing them
文献作者:Verbeuren,T.; Simonet,S.; Descombes,J.-J.; Cimetiere,B.; Lavielle,G.(ADIR et Cie.)
参考来源:EP 1118610; FR 2803848; JP 2001226353