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

Phenserine tartrate

苯丝氨酸Chemical Name: (-)-5-O-(N-Phenylcarbamoyl)eseroline L-tartrate; N-Phenylcarbamic acid (3aS,8aR)-1,3a,8-trimethyl-1,2,3,3a,8,8a-hexahydropyrrolo[2,3-b]indol-5-yl ester L-tartrate
CAS No. 156910-...
参考文献标题:Physostigmine derivs.with acetylcholinesterase inhibition properties,and the relative production process
文献作者:Pomponi,M.; Brufani,M.; Marta,M.; Pavone,F.; Oliverio,A.; Castellano,C.(Consiglio Nazionale delle Ricerche)
参考来源:EP 0154864; EP 0354594

Hoe-263

苯乙胺,N-[2-(二苯甲氧基)乙基]-3-甲氧基-镰,a-二甲基-盐酸盐(1:1)Chemical Name: N-[2-(Diphenylmethoxy)ethyl]-m-methoxy-N,alpha-dimethylphenethylamine hydrochloride; N-[2-(Benzhydryloxy)ethyl]-N-methyl-[1-methyl-2-(3-methoxy...
参考文献标题:m-Methoxy-alpha-methyl-phenethyl-amino-diphenylmethyl ethers
文献作者:Lindner,E.; Ehrhart,G.; Ott,H.(Aventis Pharma AG)
参考来源:US 3565955

Antineoplaston AS2-5

苯乙酰谷氨酰胺(钠) N-苯乙酰基-L-谷氨酰胺 Chemical Name: N2-Phenylacetyl-L-glutamine sodium salt
CAS No. 104771-87-1, 28047-15-6 (free acid), 31427-44-8 (free acid)
项目整合开发状态: Phase II
项目研究机构: Burzynski Resear...
参考文献标题:Benzoselenino[4,3,2-cd]indazole compound,compositions comprising the compounds and processes for producing the compounds
文献作者:Berman,E.M.; Gregor,V.E.; Showalter,H.H.D.(Pfizer Inc.)
参考来源:AU 8544154; EP 0170412; ES 8704956

Oxiperomide, R-4714

苯乙醚咪唑苯哌咪酮Chemical Name: 1-[1-(2-Phenoxyethyl)piperidin-4-yl]-2,3-dihydro-1H-benzimidazol-2-one
CAS No. 5322-53-2
项目整合开发状态: Not Determined
项目研究机构:
合成路线:By condensation of 4-(2-oxo-1-benzim...
参考文献标题:
文献作者:Janssen,P.A.J.
参考来源:BE 663431; DE 1545998; FR 1455874; GB 1046053; US 3225052

Benclonidine, ST-2225

苯可乐定Chemical Name: N-[1-Benzoylimidazolidin-2-ylidene]-N-(2,6-dichlorophenyl)amine
CAS No. 57647-79-7
项目整合开发状态: Biological Testing
项目研究机构:
合成路线:Benclonidine has been synthesized by variou...
参考文献标题:Benclonidine
文献作者:Koch,H.
参考来源:Drugs Fut 1984,9(6),408

Befuraline hydrochloride, DIV-154

苯呋拉林Chemical Name: N-Benzyl-coumarilic acid piperazide hydrochloride; N-Benzo[b]furan-2-ylcarbonyl-N'-benzylpiperazine hydrochloride; 1-(2-Benzofuranylcarbonyl)-4-(phenylmethyl)piperazine hydrochlorid...
参考文献标题:Cyclic diamine derivatives
文献作者:Soeder,A.; et al.(Aventis Pharma AG)
参考来源:DE 2157424; DE 2240665; ES 408565; FR 2160611; GB 1407854; US 4374990

PD-117302

苯并[b]噻吩-4-乙酰胺,N-甲基-N-[(1R,2R)-2-(1-吡咯里二基)环己基]-,rel-Chemical Name: (?-trans-N-Methyl-N-[2-(1-pyrrolidinyl)cyclohexyl]benzo[b]thiophene-4-acetamide
CAS No. 111728-01-9
项目整合开发状态: Preclinical
项目研...
参考文献标题:Synthesis of carbon-14 labeled PD 117,302 and PD 126,212,potential new analgesic agents
文献作者:Huang,C.C.; Hicks,J.L.; Butler,D.E.; Hays,S.J.
参考来源:J Label Compd Radiopharm 1990,28(1),15

T-588

苯并[b]噻吩-5-甲醇,a-[[2-(二乙胺基)乙氧基]甲基,盐酸盐(1:1),(aR)-Chemical Name: (-)-(R)-1-(Benzothiophen-5-yl)-2-[2-(diethylamino)ethoxy]ethanol hydrochloride
CAS No. 142935-03-3, 131965-06-5 (undefined isomer)
项目...
参考文献标题:1,2-Ethanediol deriv.and salt thereof,process for producing the same,and cerebral function-improving agent comprising them
文献作者:Ono,S.; Yamafuji,T.; Chaki,H.; Maekawa,M.; Todo,Y.; Narita,H.(Toyama Chemical Co.,Ltd.)
参考来源:EP 0383281; EP 0587193; EP 0587194; EP 0589484; FR 2643079; JP 1991047158; JP 1991197422; US 5280032; US 5472984; US 5612381; US 5658904

新产品编号:995587

苯并噻吩-2-硼酸Chemical Name: Benzo[b]thiophene-2-boronic acid
CAS No. 98437-23-1
项目整合开发状态: Biological Testing
项目研究机构: Northwestern University (Originator)
合成路线:The reaction of benzo[b]thiophene...
参考文献标题:Inhibitors of beta-lactamases and uses therefor
文献作者:Shoichet,B.K.; Weston,G.S.(Northwestern University)
参考来源:WO 9856392

Pyrrophenone

苯并胺,N-[[(2S,4R)-1-[2-(2,4-二氟苯甲酰)苯甲酰]-4-[(三苯甲基)硫代]-2-吡咯里丁基]甲基]-4-[(Z)-(2,4-二氧二氧基-5-噻唑烷基苯)甲基]-Chemical Name: N-[1-[2-(2,4-Difluorobenzoyl)benzoyl]-4(R)-(triphenylmethylsulfanyl)pyrrolidin-2(S)-ylmethyl]...
参考文献标题:Pyrrolidine inhibitors of human cytosolic phospholipase A2.Part 2: Synthesis of potent and crystallized 4-triphenylmethylthio derivative "pyrrophenone"
文献作者:Seno,K.; Okuno,T.; Nishi,K.; Murakami,Y.; Yamada,K.; Nakamoto,S.; Ono,T.
参考来源:Bioorg Med Chem Lett 2001,11(4),587