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

ER-41114

1-[1-[2-(4-氟苯基)乙基]哌啶-4-基]-6-甲氧基-2,3-二氢吲哚Chemical Name: 1-[1-[2-(4-Fluorophenyl)ethyl]piperidin-4-yl]-6-methoxy-2,3-dihydro-1H-indole
CAS No. 214616-13-4
项目整合开发状态: Preclinical
项目研究机构: Eisai (O...
参考文献标题:1,4-Substd.cyclic amine derivs.
文献作者:Kimura,T.; Takahashi,K.; Matsunaga,M.; Kawano,K.; Kubota,A.; Kitazawa,N.; Okabe,T.; Ueno,K.; Komatsu,M.; Sasaki,A.(Eisai Co.,Ltd.)
参考来源:EP 0976732; WO 9843956

PNU-96415F(succinate), U-96415E

1-[2-(3,4-二氢-1H-异苯并吡喃-1-基)乙基]-4-(4-氟苯基)哌嗪二盐酸盐Chemical Name: 1-[2-(3,4-Dihydro-1H-2-benzopyran-1-yl)ethyl]-4-(4-fluorophenyl)piperazine dihydrochloride
CAS No. 170856-41-4, 170858-22-7 ((R)-isomer, ...
参考文献标题:Heterocyclic cpds.for the treatment of CNS and cardiovascular disorders
文献作者:Ten Brink,R.E.; Ennis,M.D.; Lin,C.-H.; Lahti,R.A.; Romero,A.G.; Sih,J.C.(Pharmacia Corp.)
参考来源:EP 0737189; JP 1997507224; US 5877317; WO 9518118

AGY-94806, Msc1, SA-4503

1-[2-(3,4-二甲氧基苯基)乙基]-4-(3-苯基丙基)哌嗪盐酸盐Chemical Name: 1-[2-(3,4-Dimethoxyphenyl)ethyl]-4-(3-phenylpropyl)piperazine dihydrochloride
CAS No. 165377-44-6
项目整合开发状态: Phase I
项目研究机构: Santen (Originat...
参考文献标题:Novel 1,4-di(phenylalkyl)piperazine deriv.
文献作者:Kawashima,Y.; Matsumoto,J.; Matsuno,K.; Senda,T.; Hirano,K.(Santen Pharmaceutical Co.,Ltd.)
参考来源:EP 0711763; JP 1995089949; US 5736546; WO 9504050

Nolpitantium besilate, SR-140333B, SR-140333A(chloride), SR-140333(cation)

1-[2-[3-(3,4-二氯苯基)-1-[2-(3-异丙氧基苯基)乙酰]哌啶-3(S)-酰基]-4-苯基-1-偶氮二环[2.2.2]辛烷苯磺酸盐 1-[2-[(3S)-3-(3,4-二氯苯基)-1-[2-[3-(1-甲基乙氧基)苯基]乙酰基]-3-哌啶基]乙基]-4-苯基-1-氮杂双环[2.2.2]氯化辛烷 1-Azonia双环[2.2.2]辛烷,1-[2-[(3S)-3-(3,4-二氯苯基)-...
参考文献标题:Quaternary basic amides as tachykinines antagonists
文献作者:Emonds-Alt,X.; Gueule,P.; Proietto,V.; Van Broeck,D.(Sanofi-Synthabo)
参考来源:EP 0591040; FR 2696178; JP 1998175976; US 5583134; US 5712288

ReN-1869, NNC-05-1869

1-[3-(10,11-二氢-5H-二苯并[a,d]环庚烯-5-亚基)丙基]哌啶-3(R)-羧酸 (3R)-1-[3-(5,6-二氢二苯并[1,2-a:1//',2//'-e][7]烯基-11-伊酮)丙基]哌啶-3-羧酸盐酸盐 Chemical Name: 1-[3-(10,11-Dihydro-5H-dibenzo[a,d]cyclohepten-5-ylidene)propyl]piperid...
参考文献标题:Novel heterocyclic cpds.
文献作者:Andersen,K.E.; Olsen,U.B.; Petersen,H.; Gr鴑vald,F.C.; Sonnewald,U.; J鴕gensen,T.K.; Andersen,H.S.(Novo Nordisk A/S)
参考来源:US 5595989; US 5668129; US 5688788; US 5693649; US 5712292; US 5721254; US 5795888; US 6043239; WO 9518793

Atevirdine mesylate, U-87201E

1-[3-(乙胺基)-2-吡啶基]-4-(5-甲氧基-1H-吲哚-2-基羰基)哌嗪单甲磺酸酯阿替韦啶 Chemical Name: 1-[3-(Ethylamino)-2-pyridyl]-4-(5-methoxy-1H-indol-2-ylcarbonyl)piperazine monomethanesulfonate
CAS No. 138540-32-6, 136816-75-6 (...
参考文献标题:Nonnucleoside reverse transcriptase inhibitors that potently and specifically block human immunodeficiency virus type 1 replication
文献作者:Romero,D.L.; Busso,M.; Tan,C.-K.; Reusser,F.; Palmer,J.R.; Poppe,S.M.; Aristoff,P.A.; Downey,K.M.; So,A.G.; Resnick,L.; et al.
参考来源:Proc Natl Acad Sci USA 1991,88(19),8806-10

Delavirdine mesilate, U-90152S, Rescriptor

1-[3-(异丙基氨基)-2-吡啶基]-4-[5-(甲磺酰氨基)-1H-吲哚-2-基羰基]哌嗪单甲磺酸酯地拉韦啶 Chemical Name: 1-[3-(Isopropylamino)-2-pyridyl]-4-[5-(methanesulfonamido)-1H-indol-2-ylcarbonyl]piperazine monomethanesulfonate
CAS No. 148...
参考文献标题:Diaromatic substd.cpds.as anti-HIV-1 agents
文献作者:Aristoff,P.A.; Romero,D.L.; Palmer,J.R.; Thomas,R.C.; Smith,H.W.(Pharmacia Corp.)
参考来源:US 5563142

NNC-26-9100

1-[3-[N-(5-溴吡啶-2-基)-N-(3,4-二氯苄基)氨基]丙基]-3-[3-(1H-咪唑-4-基)丙基]硫脲Chemical Name: N-[3-[N-(5-Bromo-2-pyridyl)-N-(3,4-dichlorobenzyl)amino]propyl]-N'-[3-(1H-imidazol-4-yl)propyl]thiourea
CAS No. 199522-35-...
参考文献标题:Nonpeptide somatostatin agonists with sst4 selectivity: Synthesis and structure-activity relationships of thioureas
文献作者:Liu,S.; Tang,C.; Ho,B.; Ankersen,M.; Stidsen,C.E.; Crider,A.M.
参考来源:J Med Chem 1998,41(24),4693

UCL-1972

1-[5-(4-硝基苯氧基)戊基]吡咯利定Chemical Name: 1-[5-(4-Nitrophenoxy)pentyl]pyrrolidine
CAS No. 220728-17-6
项目整合开发状态: Preclinical
项目研究机构: Bioprojet (Originator), INSERM (Originator)
合成路线:The reaction ...
参考文献标题:Non-imidazole aryloxy (or arylthio) alkylamines as histamine H3-receptor antagonists and their therapeutic applications
文献作者:Stark,H.; Ligneau,X.; Garbarg,M.; Schunack,W.G.; Ganellin,C.R.; Lecomte,J.-M.; Arrang,J.-M.; Leurquin,F.; Sigurd,E.; Schwartz,J.-C.(Societe Civile Bioprojet)
参考来源:EP 0978512

SK&F-96067

1-[8-甲氧基-4-[(2-甲基苯基)氨基]喹啉-3-基]丁烷-1-酮Chemical Name: 3-Butyryl-8-methoxy-4-(2-methylphenylamino)quinoline
CAS No. 115607-61-9, 115607-77-7 (monoHCl)
项目整合开发状态: Phase III
项目研究机构: GlaxoSmithKline ...
参考文献标题:4-Amino-3-substituted quinolines as inhibitors of gastric acid secretion
文献作者:Ife,R.J.; Brown,T.H.; Leach,C.A.(SmithKline Beecham plc)
参考来源:AU 8778741; EP 0259174; JP 1989500664; US 4806549; US 4806550; WO 8801621