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

R-755

Chemical Name: N-(2,6-Diethylphenyl)-N'-[3-(2-methylphenyl)-6,7-dihydro-5H-indeno[5,6-b]thiophen-2-yl]urea
CAS No. 159387-63-0
项目整合开发状态: Preclinical
项目研究机构: Nihon Nohyaku (Originator)
合成路线...
参考文献标题:N-Heteroaryl-N'-phenylurea derivs.,their production and use
文献作者:Nagamine,M.; Yamamoto,K.; Matsui,Y.; Horiuchi,K.; Yoshida,M.(Nihon Nohyaku Co.,Ltd.)
参考来源:CA 2116286; EP 0613894; JP 1994340647; US 5464863

ABS-103

Chemical Name: 2-Propyl-4-hexynoic acid
CAS No. 51577-99-2
项目整合开发状态: Preclinical
项目研究机构: American Biogenetic Sciences (Originator)
合成路线:The alkylation of diethyl n-propylmalonate (I) with ...
参考文献标题:VPA-analogous antiepileptics
文献作者:Hauck,R.-S.; Elmazar,M.M.E.; Nau,H.; Bojic,U.
参考来源:DE 4231085; US 5786380; WO 9406743

L-733060

Chemical Name: (2S,3S)-3-[3,5-Bis(trifluoromethyl)benzyloxy]-2-phenylpiperidine
CAS No. 148700-84-9, 148700-91-8 ((-)-cis-isomer), 148687-78-9 ((-)-cis-isomer, HCl), 148700-85-0 ((+)-cis-isomer), 1...
参考文献标题:Azacyclic cpds.,processes for their preparation and pharmaceutical compsns.containing them
文献作者:Baker,R.; Harrison,T.; Swain,C.J.; Williams,B.J.(Merck Sharp & Dohme Ltd.)
参考来源:EP 0528495; EP 0600952; JP 1994510034; WO 9304040

Labradimil, Lobradimil, Receptor mediated permeabilizer, RMP-7, Cereport

Chemical Name: Nalpha-[2(S)-[L-Arginyl-L-prolyl-[4(R)-hydroxy]-L-prolyl-glycyl-[3-(2-thienyl)]-L-alanyl-L-seryl-L-prolylamino]-3-(4-methoxyphenyl)propyl]-L-arginine
CAS No. 159768-75-9
项目整合开发状态:...
参考文献标题:Increasing blood-brain barrier permeability with permeabilizer peptides
文献作者:Kozarich,J.W.; Musso,G.F.; Malfroy-Camine,B.(Alkermes,Inc.)
参考来源:WO 9218529

NCA-0424

Chemical Name: 2-Methyl-2-(6-methylindolo[2,3-b]quinoxalin-4-ylmethylamino)propane-1,3-diol hydrochloride
CAS No. 161224-75-5
项目整合开发状态: Preclinical
项目研究机构: Taisho (Originator)
合成路线:The con...
参考文献标题:Indolo[2,3-b]quinoxaline derivs.
文献作者:Matsumoto,T.; Wada,H.; Migita,Y.; Hatayama,K.; Sekiguchi,Y.(Taisho Pharmaceutical Co.,Ltd.)
参考来源:EP 0695754; JP 1995522993; WO 9424135

IsoddA-(S,S), 191W91

Chemical Name: (2S,4S)-9-[2-(Hydroxymethyl)tetrahydrofuran-4-yl]adenine; 2-(6-Amino-9H-purin-9-yl)-1,4-anhydro-2,3-dideoxy-D-arabinitol
CAS No. 143191-77-9
项目整合开发状态: Preclinical
项目研究机构: Glaxo...
参考文献标题:Synthesis of purine and pyrimidine isodideoxynucleosides from (S)-glycydol using iodoetherification as key step.Synthesis of (S,S)-iso-ddA
文献作者:D韆z,Y.; et al.
参考来源:J Org Chem 1999,64(17),6508

OPC-29030

Chemical Name: (S)-(+)-6-[3-[1-(2-Methylphenyl)imidazol-2-ylsulfinyl]propoxy]-1,2,3,4-tetrahydroquinolin-2-one
CAS No. 161190-38-1
项目整合开发状态: Clinical
项目研究机构: Otsuka (Originator)
合成路线:Alkyl...
参考文献标题:Carbostyril derivs.
文献作者:Nishi,T.; Uno,T.; Shu,Y.; Tamura,K.; Okada,M.(Otsuka Pharmaceutical Co.,Ltd.)
参考来源:EP 0651747; JP 1995033765; US 5541198; WO 9426732

RWJ-50172

Chemical Name: N-(2,6-Difluorophenyl)-3-oxo-1,2,3,5-tetrahydropyrido[1,2-a]benzimidazole-4-carboxamide
CAS No. 155201-46-0
项目整合开发状态: Preclinical
项目研究机构: R.W. Johnson (Originator)
合成路线:Conj...
参考文献标题:3-Oxo-pyrido(1,2-a)benzimidazole-4-carboxyl and 4-oxo-azepino(1,2-a)benzimidazole-5-carboxyl derivs.useful in treating central nervous system disorders
文献作者:Maryanoff,B.E.; McComsey,D.F.; Winston,H.(Ortho-McNeil Pharmaceutical,Inc.)
参考来源:EP 0656002; WO 9404532

CT-2584, Apra

Chemical Name: 1-[11-(Dodecylamino)-10-hydroxyundecyl]-3,7-dimethylxanthine
CAS No. 160944-05-8 (racemate)
项目整合开发状态: Phase III
项目研究机构: Cell Therapeutics (Orphan Drug), Cell Therapeutics (Orig...
参考文献标题:Second messenger cell signaling inhibitors
文献作者:Michnick,J.; Underiner,G.E.; Klein,J.P.; Rice,G.C.; Sunkara,P.S.(Cell Therapeutics,Inc.)
参考来源:CH 686830; EP 0719267; JP 1996508981; US 5470878; WO 9422863

FR-161282

Chemical Name: 4'-Methyl-N-[4-[5-[2-(4-methylpiperazin-1-yl)-2-oxoethyl]-4-oxo-2,3,4,5-tetrahydro-1H-1,5-benzodiazepin-1-ylcarbonyl]phenyl]biphenyl-2-carboxamide
CAS No. 168046-41-1, 168046-43-3 (m...
参考文献标题:Synthesis and characterization of orally active nonpeptide vasopressin V2 receptor antagonists
文献作者:Ohkawa,T.; Zenkoh,T.; Tomita,M.; Hosogai,N.; Hemmi,K.; Tanaka,H.; Setoi,H.
参考来源:Chem Pharm Bull 1999,47(4),501