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

新产品编号:432395

Chemical Name: (Tributyl)(2,3,5,6,8,9,11,12-Octahydro-1,4,7,10,13-benzopentaoxacyclopentadecin-15-ylcarbonyloxy)stannane; Tributyltin 4-carboxybenzo-15-crown-5
CAS No. 215233-50-4
项目整合开发状态: Biol...
参考文献标题:Tin polyoxaalkanecarboxylates and compsns.containing them
文献作者:De Vos,D.; Kemmer,M.; Biesemans,M.; Willem,R.; Gielen,M.(Pharmachemie BV)
参考来源:WO 0006583

新产品编号:641219

Chemical Name: N-[4-Cyano-3-(trifluoromethyl)phenyl]-2(R)-hydroxy-2-methyl-3-[4-(isothiocyanato)phenylsulfanyl]propionamide
CAS No. 247090-55-7, 247090-62-6 (S)
项目整合开发状态: Biological Testing
项...
参考文献标题:Chiral nonsteroidal affinity ligands for the androgen receptor.1.Bicalutamide analogues bearing electrophilic groups in the B aromatic ring
文献作者:Kirkovsky,L.; Mukherjee,A.; Yin,D.; Dalton,J.T.; Miller,D.D.
参考来源:J Med Chem 2000,43(4),581

新产品编号:710827

Chemical Name: 1,3-Dibutyl-7-(3-chloropropylsulfonyl)-3,7-dihydro-1H-purine-2,6-dione; 1,3-Dibutyl-7-(3-chloropropylsulfonyl)xanthine
CAS No. 263552-81-4
项目整合开发状态: Preclinical
项目研究机构: OSI (Or...
参考文献标题:Novel and selective calcitonin-inducing agents
文献作者:Gilbert,A.M.; Caltabiano,S.; Roberts,D.; Sum,S.F.; Francisco,G.D.; Lim,K.; Asselin,M.; Ellingboe,J.W.; Kharode,Y.; Cannistraci,A.; Francis,R.; TrailSmith,M.; Gralnick,D.
参考来源:J Med Chem 2000,43(6),1223

新产品编号:296343

Chemical Name: 3-[2-Oxo-3-[1-(2-thienylsulfonyl)piperidin-4-yl]perhydro-1,3-diazepin-1-yl]benzamidine hydrochloride
CAS No. 198824-33-8 (free base)
项目整合开发状态: Preclinical
项目研究机构: Bristol-Myers...
参考文献标题:N-(Amidinophenyl)-N'-(substd.)-3H-2,4-benzodiazepin-3-one derivs.as factor Xa inhibitors
文献作者:Maduskuie,T.P.Jr.; Galemmo,R.A.Jr.; Dominguez,C.; Quan,M.L.; Rossi,K.A.; Stouten,P.F.W.; Sun,J.H.; Wells,B.L.(DuPont Pharmaceuticals Co.)
参考来源:EP 0960104; US 5925635; WO 9738984

D83-7676

Chemical Name: 1-[2-Amino-6-[4-[3-[4-(3,5-difluorophenyl)piperazin-1-yl]-1(E)-propenyl]-5-methyl-1H-pyrazol-1-yl]pyrimidin-4-yl]azetidin-3-ol
CAS No. 256929-05-2 (hydrochloride)
项目整合开发状态: Precli...
参考文献标题:Pyrazole derivs.and salts thereof
文献作者:Naito,H.; Ohsuki,S.; Ejima,A.; Makino,C.; Ohki,H.(Daiichi Pharmaceutical Co.,Ltd.)
参考来源:EP 1103551; JP 2000169475; WO 0005230

TMC-95B

Chemical Name: (10S,11R,12S,15S,18S)-15-(Carbamoylmethyl)-10,11,23-trihydroxy-18-[3(R)-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

Lu-35-138

Chemical Name: 3-[1-[2-[1-Acetyl-2,3-dihydro-1H-indol-3(S)-yl]ethyl]-1,2,3,6-tetrahydropyridin-4-yl]-6-chloro-1H-indole ; 1-Acetyl-3(S)-[2-[4-(6-chloro-1H-indol-3-yl)-1,2,3,6-tetrahydropyridin-1-yl]et...
参考文献标题:Indane or dihydroindole derivs.
文献作者:Perregaard,J.K.; Pedersen,H.; Mikkelsen,I.; Bang-Andersen,B.; Dancer,R.(H.Lundbeck A/S)
参考来源:EP 0946542; JP 2000513731; US 2001021777; US 6262087; US 6352988; US 6552044; WO 9828293

新产品编号:310581

Chemical Name: 4(S)-Ethyl-4,9-dihydroxy-12-(2,2,2-trifluoroethoxy)-1H-pyrano[3',4':6,7]indolizino[1,2-b]quinoline-3,14(4H,12H)-dione; 10-Hydroxy-5-(2,2,2-trifluoroethoxy)-20(S)-camptothecin
CAS No....
参考文献标题:Short oligonucleotides for the inhibition of VEGF expression
文献作者:Bitonti,A.; Woessner,R.; Peyman,A.; Uhlmann,E.(Aventis Pharma Deutschland GmbH)
参考来源:EP 0979869; WO 0008141

新产品编号:563701

Chemical Name: 2-[8-(4-Chlorophenyl)-8-oxooctylsulfanyl]-5-(5-pyrimidinylmethyl)pyrimidin-4(1H)-one
CAS No. 224771-21-5
项目整合开发状态: Biological Testing
项目研究机构: GlaxoSmithKline (Originator)
合成...
参考文献标题:Pyrimidinone cpds.and pharmaceutical compsns.containing them
文献作者:Pinto,I.L.; Ife,R.J.; Hickey,D.M.B.; Smith,S.A.; Leach,C.A.; Porter,R.A.(SmithKline Beecham plc)
参考来源:EP 1028955; WO 9924420

NNC-45-0095

Chemical Name: 1-Ethyl-2-(4-hydroxyphenyl)pyrrolo[2,1,5-cd]indolizine; 4-(1-Ethylpyrrolo[2,1,5-cd]indolizin-2-yl)phenol
CAS No. 217318-90-6
项目整合开发状态: Preclinical
项目研究机构: Novo Nordisk (Origina...
参考文献标题:Pyrrolo[2,1,5-cd]indolizine derivs.useful in the prevention or treatment of estrogen related diseases or syndromes
文献作者:Christiansen,L.B.; Kanstrup,A.; Jacobsen,P.; Jorgensen,A.S.; Bury,P.S.(Novo Nordisk A/S)
参考来源:EP 0986560; US 6075036; WO 9855482