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

GNTI

5′-胍基诺曲因多尔二(三氟乙酸盐)盐水合物 Chemical Name: 17-(Cyclopropylmethyl)-4,5alpha-epoxy-3,14-dihydroxy-5'-guanidino-6,7-didehydroindolo[2',3':6,7]morphinan; N-[(4bS,8R,8aS,14bR)-7-(Cyclopropylmethyl)-1,8a-dihydr...
参考文献标题:Naltrindole analogs as potent and selective kappa-opioid receptor antagonists
文献作者:Sercel,A.D.; Stevens,W.C.Jr.; Ingals,S.; et al.
参考来源:218th ACS Natl Meet (Aug 22 1999,New Orleans) 1999,Abst MEDI 267

SNAP-6383, L-771688

5-嘧啶羧酸,6-(3,4-二氟苯基)-1,2,3,6-四氢-4-(甲氧基甲基)-2-氧基-1-[[[3-[4-(2-吡啶基)-1-哌啶基]丙基]氨基]羰基]-,甲酯,盐酸盐(1:2),(6S)- Chemical Name: 4(S)-(3,4-Difluorophenyl)-6-(methoxymethyl)-2-oxo-3-[3-[4-(2-pyridinyl)piperidin-1-yl...
参考文献标题:Dihydropyrimidines and uses thereof
文献作者:Wong,W.C.; Lagu,B.; Nagarathnam,D.; Marzabadi,M.R.; Gluchowski,C.(Synaptic Pharmaceutical Corp.)
参考来源:EP 1021185; JP 2000506904; WO 9742956

RVT, DPC-817, beta-D-D4FC, D-D4FC, Reverset

5-氟-1-(2',3'-二脱氧-2',3'-二脱氢β-D-呋喃阿糖基)-胞嘧啶(Dexelvucitabine) Chemical Name: beta-D-2',3'-Didehydro-2',3'-dideoxy-5-fluorocytidine
CAS No. 181785-83-1, 134379-77-4 (undefined isomer)
项目整合开发状态: Phas...
参考文献标题:Method for the synthesis of 2',3'-dideoxy-2',3'-didehydronucleosides
文献作者:Confalone,P.N.; Jin,F.(Pharmasset,Inc.)
参考来源:WO 0270533

SB-271046

5-氯-N-[4-甲氧基-3-(1-哌嗪基)苯基]-3-甲基苯并[b]噻吩-2-磺胺 Chemical Name: 5-Chloro-N-[4-methoxy-3-(1-piperazinyl)phenyl]-3-methylbenzo[b]thiophene-2-sulfonamide hydrochloride
CAS No. 209481-24-3, 209481-20-9 (fre...
参考文献标题:Sulphonamide derivs.,process for their preparation,and their use as medicaments
文献作者:King,F.D.; Bromidge,S.M.; Wyman,P.A.(SmithKline Beecham plc)
参考来源:WO 9827081

RWJ-54428, MC-02,479

5-硫-1-氮杂双环[4.2.0]辛-2-烯-2-羧酸,7-[[(2Z)-2-(2-氨基-5-氯-4-噻唑基)-2-(羟基氨基)乙基]氨基]-[[3-[(2-氨基乙基)硫]甲基]-4-吡啶基]-8-氧基-,(6R,7R)- Chemical Name: (6R,7R)-7-[2-(2-Amino-5-chlorothiazol-4-yl)-2(Z)-(hydroxyimino)acetamido...
参考文献标题:Cephalosporin antibiotics
文献作者:Cho,I.-S.; Hecker,S.; Glinka,T.; Lee,V.J.; Zhang,Z.J.(Microcide Pharmaceuticals,Inc.)
参考来源:EP 0874854; JP 1999513670; US 6057312; US 6066630; US 6087355; WO 9713772

LY-377604

6-(4-(2-((((2S)-3-(9H-卡巴唑-4-酰氧基)-2-羟丙基)氨基)-2-甲基丙基苯氧基)吡啶-3-羧酰胺 Chemical Name: 6-[4-[2-[3-(9H-Carbazol-4-yloxy)-2(S)-hydroxypropylamino]-2-methylpropyl]phenoxy]pyridine-3-carboxamide hydrochloride
C...
参考文献标题:Carbazole analogues as selective B3 adrenergic agonists
文献作者:Crowell,T.A.; Evrard,D.A.; Jones,C.D.; Muehl,B.S.; Rito,C.J.; Shuker,A.J.; Thorpe,A.J.; Thrasher,K.J.(Eli Lilly and Company)
参考来源:EP 0827746; WO 9809625

(S)-PD-148903

6-(二丙基氨基)-3,4,5,6,7,8-六氢萘-1(2H)-酮 Chemical Name: (-)-6(S)-(Dipropylamino)-1,2,3,4,5,6,7,8-octahydronaphthalen-1-one hydrochloride
CAS No. 335158-94-6, 256474-06-3 (undefined isomer, free base)
...
参考文献标题:Method for treating Parkinson's disease by administering (-)-5-keto-2-N,N-di-N-propylamino-tetrahydrotetralin
文献作者:Wise,L.D.; Wikstrom,H.V.; Wustrow,D.J.; Meltzer,L.T.; Dijkstra,D.; Venhuis,B.J.(Pfizer Inc.)
参考来源:WO 0128977

IMPY

6-碘-2-(4-二甲基氨基苯基)咪唑并[1,2-a]吡啶 Chemical Name: N-[4-[6-([125I]-Iodo)imidazo[1,2-a]pyridin-2-yl]phenyl]-N,N-dimethylamine
CAS No. 474012-78-7, 474012-75-4 (unlabeled)
项目整合开发状态: Preclinical
项目研究...
参考文献标题:Amyloid plaque aggregation inhibitors and diagnostic imaging agents
文献作者:Kung,H.; Kung,M.-P.; Zhuang,Z.-P.(University of Pennsylvania)
参考来源:CA 2444214; EP 1381604; US 2003059369; WO 0285903

D-4418

8-甲氧基-喹啉-5-甲酸Chemical Name: N-(3,5-Dichloro-4-pyridinyl)-8-methoxyquinoline-5-carboxamide
CAS No. 199871-63-1, 199871-80-2 (diHBr), 199871-79-9 (diHCl)
项目整合开发状态: Phase I
项目研究机构: Celltech (Or...
参考文献标题:Quinoline carboxamides as TNF inhibitors and as PDE-IV inhibitors
文献作者:Dyke,H.J.; Montana,J.G.; Lowe,C.; Kendall,H.J.; Sabin,V.M.(Celltech Group plc)
参考来源:EP 0952832; JP 2000510865; US 5804588; WO 9744036

Asulacrine isethionate, Amsalog, NSC-343499, CI-921

9-(2-甲氧基-4-(甲基磺酰基氨基)苯胺基)-N,5-二甲基吖啶-4-甲酰胺 Chemical Name: 9-[2-Methoxy-4-(methylsulfonylamino)phenylamino]-N,5-dimethyl-4-acridinecarboxamide 2-hydroxyethanesulfonate
CAS No. 80841-48-1, 80841-47-0 ...
参考文献标题:CI-921
文献作者:Denny,W.A.; Atwell,G.J.; Baguley,B.C.
参考来源:Drugs Fut 1984,9(8),575