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

Eclanamine maleate, U-48753E

Chemical Name: trans-N-(3,4-Dichlorophenyl)-N-[2-(dimethylamino)cyclopentyl]propanamide (Z)-2-butenedioate (1:1); trans-3,4-Dichloro-N-[2-(dimethylamino)cyclopentyl]propionanilide maleate
CAS No. 7...
参考文献标题:U-48753 E
文献作者:Owen,R.T.; Serradell,M.N.; Castar,J.
参考来源:Drugs Fut 1984,9(11),846

Wy-44221

Chemical Name: (S,S)-1-(2-Methyl-3-sulfanyl-1-oxopropyl)-2,3-dihydro-1H-indole-2-carboxylic acid; (S,S)-1-(2-Methyl-3-sulfanyl-1-oxopropyl)indoline-2-carboxylic acid; (S,S)-1-(2-Methyl-3-sulfanylpropi...
参考文献标题:WY-44221
文献作者:Serradell,M.N.; Castar,J.; Blancafort,P.
参考来源:Drugs Fut 1983,8(11),953

PK-9084

Chemical Name: 2-Phenyl-4-(2-piperidin-3-ylethyl)quinoline; 2-Phenyl-4-[2-(3-piperidinyl)ethyl]quinoline
CAS No. 77472-99-2
项目整合开发状态: Biological Testing
项目研究机构: Pharmuka (Originator)
合成路线:...
参考文献标题:1-(4 Quinolyl) 2- or 3- (2- or 3- piperidyl or pyrrolidinyl) ethanone or propanone,process for their preparation and their use as medicaments
文献作者:Dubroeucq,M.C.; Gueremy,C.G.A.; Lefur,G.R.; Mizoule,J.(Pharmindustrie)
参考来源:EP 0042781

Benexate cyclodextrin, TKG01 clathrate cpd., TA-903, Lonmiel, Ulgut

Chemical Name: trans-4-(Guanidinomethyl)cyclohexanecarboxylic acid 2-(benzyloxycarbonyl)phenyl ester hydrochloride 1:1 complex with beta-cyclodextrin; trans-2-[4-(Guanidinomethyl)cyclohexylcarbonyloxy...
参考文献标题:Antihistaminic 11-(4-piperidylidene)-5H-benzo-[5,6
文献作者:Villani,F.J.(Schering Corp.)
参考来源:US 4282233

ICI-155387, CB-3717

Chemical Name: N-[4-[[(2-Amino-1,4-dihydro-4-oxo-6-quinazolinyl)methyl]-2-propynylamino]benzoyl]-L-glutamic acid; N-[4-[N-[(2-Amino-4-hydroxy-6-quinazolinyl)methyl]prop-2-ynylamino]benzoyl]-L-glutamic...
参考文献标题:CB-3717
文献作者:Hopkins,S.J.; Serradell,M.N.; Castar,J.
参考来源:Drugs Fut 1984,9(12),893

LL-11204, DL-204-IT

Chemical Name: 2-(3-Ethoxyphenyl)-5,6-dihydro-s-triazolo[5,1-a]isoquinoline; 2-(3-Ethoxyphenyl)-5,6-dihydro[1,2,4]triazolo[5,1-a]isoquinoline
CAS No. 55308-64-0
项目整合开发状态: Biological Testing
项...
参考文献标题:2-Substd.phenyl-5-triazols[5,1-a]isoquinoline cpds
文献作者:Consonni,P.; Lerner,L.; Omodei-Sal? A.(Lepetit SpA)
参考来源:US 4075341

Nordidemnin, Didemnin B, NorD, NSC-325319

Chemical Name: (3S,6S,8S,12S,13R,16S,17R,20S,23S)-16-[N-[2(S)-Hydroxypropionyl]-L-prolyl-D-(N-methyl)leucylamino]-12-hydroxy-3-isobutyl-8-isopropyl-20-(4-methoxybenzyl)-6,17,21-trimethyl-13-[1(S)-meth...
参考文献标题:Total synthesis and structural investigations of didemnins A,B,and C
文献作者:Li,W.-R.; et al.
参考来源:J Am Chem Soc 1990,112(21),7659

LY-178207(free base), GYKI-14451

Chemical Name: tert-Butyloxycarbonyl-D-phenylalanyl-L-prolyl-L-arginine aldehyde sulfate (2:1); (S)-N-[(1,1-Dimethylethoxy)carbonyl]-D-phenylalanyl-N-[4-[(aminoiminoethyl)amino]-1-formylbutyl]-L-proli...
参考文献标题:D-Phenylalanyl-L-prolyl-L-arginine aldehyde sulfate and process for the preparation thereof
文献作者:Bajusz,S.; Szell,E.; Barabas,E.; Bagdy,D.(Gedeon Richter Ltd.)
参考来源:DE 3200812; FR 2497799; GB 2091270; JP 57181046; US 4399065; US 4478745

LT-1

Chemical Name: N-Hydroxy-2-(2-pyridinylmethylene)hydrazinecarboximidamide mono(4-methylbenzenesulfonate) salt; 1-[(2-Pyridylmethylene)amino]-3-hydroxyguanidine tosylate
CAS No. 85894-16-2
项目整合开发...
参考文献标题:Improvements in or relating to benzylideneamino guanidine derivatives
文献作者:Houlihan,W.J.; Manning,R.E.(Novartis AG)
参考来源:BE 0727146; DE 1902449; ES 362712; ES 374472; ES 374475; FR 2000512; FR 2059987; FR 2061583; GB 1253548; GB 1253549

GYKI-11679, RGH-5526

Chemical Name: 1-(6-Morpholino-3-pyridazinyl)-2-[1-(tert-butoxycarbonyl)-2-propylidene]hydrazine; 3-[[6-(4-Morpholinyl)-3-pyridazinyl]hydrazono]butanoic acid 1,1-dimethylethyl ester
CAS No. 69579-1...
参考文献标题:Morpholino pyridazinylhydrazones
文献作者:Szilagyi,G.; et al.(Gedeon Richter Ltd.)
参考来源:DE 2825861; FR 2394535; GB 2000125; HU 176972; JP 54016486; US 4259328; US 4308386