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

KY-455

N-(4,6-二甲基-1-戊基-2,3-二氢-1H-鐲多-7-基)-2,2-二甲基丙酰胺Chemical Name: N-(4,6-Dimethyl-1-pentyl-2,3-dihydro-1H-indol-7-yl)-2,2-dimethylpropionamide
CAS No. 178469-71-1
项目整合开发状态: Preclinical
项目研究机构: Kyoto...
参考文献标题:Novel heterocyclic derivs.,process for producing the same,and medicinal use thereof
文献作者:Matsui,H.; Kamiya,S.; Shirahase,H.; Nakamura,S.; Wada,K.(Kyoto Pharmaceutical Industries,Ltd.)
参考来源:EP 0782986; JP 1996092210; US 5990150; WO 9609287

LY-395153

N-(4-{1-[(异丙基磺酰)氨基]-2-丙基}苯基)苯并胺Chemical Name: N-[4-[2-(Isopropylsulfonamido)-1-methylethyl]phenyl]benzamide
CAS No. 211313-51-8
项目整合开发状态: Biological Testing
项目研究机构: Lilly (Originator)
合成路线...
参考文献标题:Sulphonamide derivs.
文献作者:Arnold,M.B.; Bleakman,D.; Simon,R.L.; Cantrell,B.E.; Ornstein,P.L.; McKennon,T.E.; Tizzano,J.P.; Bleisch,T.J.; Zimmerman,D.M.; Baker,S.R.; Smith,E.; Zarrinmayeh,H.; Matsumoto,K.; Escribano,A.M.(Eli Lilly and Company)
参考来源:EP 0860428; WO 9833496

MX-76629

N-(4-乙氧基-2-硝基苯基)-6-甲基烟酰胺Chemical Name: N-(4-Ethoxy-2-nitrophenyl)-6-methylpyridine-3-carboxamide
CAS No. 352228-58-1
项目整合开发状态: Biological Testing
项目研究机构: Maxim (Originator)
合成路线:1) The rea...
参考文献标题:Substd.nicotinamides and analogs as activators of caspases and inducers of apoptosis and the use thereof
文献作者:Cai,S.X.; Drewe,J.A.(Cytovia,Inc.)
参考来源:WO 0155115

PATP

N-(4-吡啶基羰基氨基)-1,2,3,6-四氢吡啶Chemical Name: N-(4-Pyridylcarbonylamino)-1,2,3,6-tetrahydropyridine; N-(4-Pyridylcarbonylamino)-1,2,5,6-tetrahydropyridine; N-(3,6-Dihydro-1(2H)-pyridinyl)-4-pyridinecarboxa...
参考文献标题:N-(Carbonylamino)-tetrahydropyridyl derivatives
文献作者:Knaus,E.E.; Corleto,L.A.; Redda,K.(Canadian Patents & Development Ltd.)
参考来源:CA 1094073; US 4338445

N1,N8-Bisnorcymserine

N-(4-异丙基苯基)氨基酸(3aS,8aR)-3a-甲基-1,2,3,3a,8,8a-六氢吡咯罗[2,3-b]吲哚-5-基酯Chemical Name: N-(4-Isopropylphenyl)carbamic acid (3aS,8aR)-3a-methyl-1,2,3,3a,8,8a-hexahydropyrrolo[2,3-b]indol-5-yl ester
CAS No. 21...
参考文献标题:Highly selective butyrylcholinesterase inhibitors for the treatment and diagnosis of Alzheimer's disease and dementias
文献作者:Soncrant,T.T.; Brossi,A.; Greig,N.H.; Hausman,M.; Yu,Q.-S.(Axonyx Inc.; National Institutes of Health)
参考来源:CA 2264750; EP 0949920; WO 9902154

JTC-801

N-(4-氨基-2-甲基-6-喹啉基)-2-[(4-乙基苯氧基)甲基]苯甲酰胺盐酸盐 N-(4-氨基-2-甲基-6-喹啉)-2-[(4-乙基苯氧基)甲基]苯甲酰胺 Chemical Name: N-(4-Amino-2-methylquinolin-6-yl)-2-(4-ethylphenoxymethyl)benzamide hydrochloride
CAS No. 244218-51-...
参考文献标题:Amide derivs.and nociceptin antagonists
文献作者:Shinkai,H.; Yamada,H.; to,T.(Japan Tobacco Inc.)
参考来源:EP 1072263; JP 1999335355; WO 9948492

Isocainide hydrochloride, Socainide hydrochloride, Lorcainide hydrochloride, R-15,889, Remivox

N-(4-氯苯基)-n-(1-异丙基-4-哌啶)苯乙酰胺盐酸盐洛开酰胺 Chemical Name: N-(4-Chlorophenyl)-N-(1-isopropylpiperidin-4-yl)phenylacetamide hydrochloride; 4'-Chloro-N-(1-isopropyl-4-piperidyl)-2-phenylacetanilide hydrochlori...
参考文献标题:Lorcainide hydrochloride
文献作者:Castar,J.; Weetman,D.F.
参考来源:Drugs Fut 1978,3(7),518

SM-19712

N-(4-氯苯基磺酰)-N'-(4-氰基-3-甲基-1-苯基吡哧唑-5-基)尿素钠盐Chemical Name: N-(4-Chlorophenylsulfonyl)-N'-(4-cyano-3-methyl-1-phenylpyrazol-5-yl)urea sodium salt
CAS No. 194542-56-8
项目整合开发状态: Preclinical
项目研究机构...
参考文献标题:Sulfonylureidopyrazole derivs.
文献作者:Matsushita,K.; Hasegawa,H.; Kuribayashi,Y.; Ohashi,N.(Sumitomo Pharmaceuticals Co.,Ltd.)
参考来源:EP 0885890; JP 1998007658; WO 9730978

MRS-1754

N-(4-氰基苯基)-2-[4-(2,3,6,7-四氢-2,6-二氧代-1,3-二丙基-1H-嘌呤-8-基)苯氧基]乙酰胺Chemical Name: N-(4-Cyanophenyl)-2-[4-(1,3-dipropylxanthin-8-yl)phenoxy]acetamide
CAS No. 264622-58-4
项目整合开发状态: Preclinical
项目研究机构...
参考文献标题:Substd.8-phenylxanthines useful as antagonists of A2B adenosine receptors
文献作者:Kim,Y.-C.; Linden,J.M.; Jocobson,K.A.(University of Virginia)
参考来源:WO 0073307

ZD-4190

N-(4-溴-2-氟苯基)-7-[2-(1H-1,2,3-三唑-1-基)乙氧基]-6-甲氧基喹喕啉-4-盐酸胺Chemical Name: N-(4-Bromo-2-fluorophenyl)-7-[2-(1H-1,2,3-triazol-1-yl)ethoxy]-6-methoxyquinazoline-4-amine hydrochloride
CAS No. 257938-36-6 参考文献标题:Design and structure-activity relationship of a new class of potent VEGF receptor tyrosine kinase inhibitors
文献作者:Hennequin,L.F.; Thomas,A.P.; Johnstone,C.; Stokes,E.S.; Lohmann,J.J.; Ogilvie,D.J.; Dukes,M.; Wedge,S.R.; Curwen,J.O.; Kendrew,J.; Lambert-van der Brempt,C.
参考来源:J Med Chem 1999,42(26),5369