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

SB-224289

(2'-甲基-4'-(5-甲基-1,2,4-恶二唑-3-基)-[1,1'-二苯基]-4-基)(1'-甲基-6,7-二氢螺[呋喃并[2,3-f]吲哚-3,4'-哌啶]-5(2H)-基)甲酮 1'-甲基-5-[[[2'-甲基-4'-(5-甲基-1,2,4-4-恶二唑-3-基)联苯-4-基]羰基]-2,3,6,7-四氢螺[呋喃[2,3-f]吲哚-3,4'-哌啶盐酸盐 Chemical Name: 1'-...
参考文献标题:The selective 5-HT1B receptor inverse agonist 1'-methyl-5-[[2'-methyl-4'-(5-methyl-1,2,4-oxadiazol-3-yl)biphenyl-4-yl]carbonyl]-2,3,6,7-tetrahydrospiro[furo[2,3-f]indole-3,4'-piperidine] (SB-224289) potently blocks terminal 5-HT autoreceptor function b
文献作者:Gaster,L.M.; Blaney,F.E.; Davies,S.; Duckworth,D.M.; Ham,P.; Jenkins,S.; Jennings,A.J.; Joiner,G.F.; King,F.D.; Mulholland,K.R.; Wyman,P.A.; Hagan,J.J.; Hatcher,J.; Jones,B.J.; Middlemiss,D.N.; Price,G.W.; Riley,G.; Roberts,C.; et al.
参考来源:J Med Chem 1998,41(8),1218

Aspalatone, AAME, BK-111

(2-甲基-4-氧代吡喃-3-基)2-乙酰基氧基苯甲酸酯Chemical Name: Acetylsalicylic acid maltol ester; 2-(Acetoxy)benzoic acid 2-methyl-4-oxo-4H-pyran-3-yl ester
CAS No. 147249-33-0
项目整合开发状态: Preclinical
项目研究机构: Bukw...
参考文献标题:Synthesis and antiplatelet effects of the new antithrombotic agent aspalatone with low ulcerogenicity
文献作者:Han,B.H.; Suh,D.-Y.; Yang,H.O.; Park,Y.-H.; Kang,Y.H.; Kim,Y.C.
参考来源:Arzneim-Forsch Drug Res 1994,44(10),1122-6

OP-2507

(3aR)-3,3aβ,4,5,6,aβ-六氢-5α-羟基-4β-[(1E,3S)-3-羟基-3-(4α-丙基环己链-1α-基)-1-丙基]环戊二酯[b]吡咯-2-戊酸甲基酯Chemical Name: 15-cis-(4-n-Propylcyclohexyl)-16,17,18,19,20-pentanor-9-deoxy-6,9alpha-nitrilo PGF1 methyl ester; ...
参考文献标题:New method of treatment using prostaglandin analogues
文献作者:Masuda,Y.(Ono Pharmaceutical Co.,Ltd.)
参考来源:EP 0169725; JP 1986030519

RP-67580

(3Ar,7ar)-八氢-2-[1-亚氨基-2-(2-甲氧基苯基)乙基]-7,7-二苯基-4H-异吲哚-4-酮Chemical Name: (+)-(3aR,7aR)-2-[1-Imino-2-(2-methoxyphenyl)ethyl]-7,7-diphenylperhydroisoindol-4-one
CAS No. 135911-02-3
项目整合开发状态: Phase I<...
参考文献标题:Synthesis of RP-67,580,a new potent nonpeptide substance P antagonist
文献作者:Peyronel,J.-F.; et al.
参考来源:Bioorg Med Chem Lett 1992,2(1),37

BAY-36-7620

(3aS,6aS)-六氢-5-亚甲基-6a-(2-萘甲基)-1H-环戊[c]呋喃-1-酮Chemical Name: (3aS,6aS)-5-Methylene-6a-(naphthalen-2-ylmethyl)perhydrocyclopenta[c]furan-1-one
CAS No. 232605-26-4, 232605-25-3 (racemate)
项目整合开发状态: ...
参考文献标题:Substd.alpha,beta-anellated butyrolactones
文献作者:Horv醫h,E.; De Vry,J.-M.-V.; Baumgarten,J.; Schreiber,R.; Lensky,S.; M黮ler,T.; Stropp,U.; Voerste,A.; M黮ler,G.; Antonicek,H.-P.; Stolle,A.; Von dem Bruch,K.(Bayer AG)
参考来源:DE 19801646; EP 1047684; WO 9936416

FR-900409, FK-409

(3E)-4-乙基-2-(羟基亚氨基)-5-硝基-3-己烯酰胺Chemical Name: 4-Ethyl-2-[(Z)-hydroxyimino]-5-nitro-3(E)-hexenamide
CAS No. 92454-60-9, 92454-83-6 (non-specified isomerism)
项目整合开发状态: Phase II
项目研究机构: Fujisawa...
参考文献标题:New nitro aliphatic cpds.,process for preparation thereof and use thereof
文献作者:Okamoto,M.; Iwami,M.; Takase,S.; Uchida,I.; Umehara,K.; Kohsaka,M.; Imanaka,H.(Fujisawa Pharmaceutical Co.,Ltd.)
参考来源:EP 0113106; JP 1990160750

Flindokalner, BMS-204352, MaxiPost

(3R)-3-(5-氯-2-甲氧基苯基)-3-氟-6-(三氟甲基)-1H-吲哚-2-酮 (3R)-3-(5-氯-2-甲氧基苯基)-3-氟-6-(三氟甲基)-1,3-二氢-2H-吲哚-2-酮 3-(5-氯-2-甲氧基苯基)-3-氟-1,3-二氢-6-三氟甲基-2H-吲哚-2-酮Chemical Name: (+)-3(S)-(5-Chloro-2-methoxyphenyl)-3-fluoro-6-...
参考文献标题:3-Substd.oxindole derivs.as potassium channel modulators
文献作者:Hewawasam,P.; Meanwell,N.A.; Gribkoff,V.K.(Bristol-Myers Squibb Co.)
参考来源:CA 2176183; EP 0747354; JP 1996333336; US 5565483; US 5602169

Robalzotan tartrate hydrate, NAD-299

(3R)-3-(二(环丁基)氨基)-8-氟色满-5-甲酰胺Chemical Name: 3(R)-(N,N-Dicyclobutylamino)-8-fluoro-3,4-dihydro-2H-1-benzopyran-5-carboxamide (R,R)-tartrate (1:1) hydrate
CAS No. 177255-04-8, 208516-87-4 (anhydrous)...
参考文献标题:Physiologically active substances TAN-1323,their preparation method and use
文献作者:Muroi,M.; Tobita,T.; Nozaki,Y.(Takeda Chemical Industries,Ltd.)
参考来源:JP 1991290193

(R)-Fluoxetine

(3R)-N-甲基-3-苯基-3-[4-(三氟甲基)苯氧基]丙烷-1-胺Chemical Name: (R)-N-Methyl-gamma-[4-(trifluoromethyl)phenoxy]benzenepropanamine; (R)-N-Methyl-3-phenyl-3-[(alpha,alpha,alpha-trifluoro-p-tolyl)oxy]propylamine
C...
参考文献标题:Fluoxetine process from benzoylpropionic acid
文献作者:Senanayake,C.H.; Hilborn,J.W.; Jurgens,A.R.(Sepracor Inc.)
参考来源:WO 9967196

Isofagomine hydrochloride, NN-42-1007

(3R,4R,5R)-3,4-二羟基-5-(羟甲基)哌啶盐酸盐Chemical Name: (3R,4R,5R)-3,4-Dihydroxy-5-(hydroxymethyl)piperidine hydrochloride
CAS No. 161302-93-8
项目整合开发状态: Preclinical
项目研究机构: Novo Nordisk (Originator) 参考文献标题:Piperidines and pyrrolidines
文献作者:Lundgren,K.; Kirk,O.(Novo Nordisk A/S)
参考来源:EP 0749423; JP 1997509947; WO 9524391