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

DO-897, BP-4.897, BP-897

N-{4-4-(2-甲氧基苯基)哌嗪-1-yl丁基}萘-2-羧酰胺Chemical Name: N-[4-[4-(2-Methoxyphenyl)-1-piperazinyl]butyl]naphthalene-2-carboxamide
CAS No. 192384-87-5
项目整合开发状态: Phase I
项目研究机构: Bioprojet (Originator), I...
参考文献标题:2-Naphthamide derivs.and their therapeutic applications
文献作者:Mann,A.; Sokoloff,P.; Schwartz,J.-C.; Wermuth,C.-G.; Garrido,F.; Lecomte,J.-M.(INSERM (Institut National de la Sante et de la Recherche Medicale); Societe Civile Bioprojet)
参考来源:EP 0779284; FR 2742149; US 5872119; US 5985895

DE-333, BE-333, CI-1006, DENSPM, BENSPM

N1,N3-二[3-(乙基氨基)丙基]-1,3-丙烷二胺Chemical Name: 1,11-Bis(ethylamino)-4,8-diazaundecane; N1,N11-Bis(ethyl)norspermine; N1,N11-Diethylnorspermine
CAS No. 121749-39-1
项目整合开发状态: Phase II
项目研究机构: Genzy...
参考文献标题:Preparation of polyamine(s),substd.on terminal nitrogen atoms
文献作者:Mignonac,S.; Guy,A.; De Lamer,V.(Sanofi-Synthabo)
参考来源:FR 2714052

TNF-484, SDZ-242-484, PKF-242-484

N1-[2,2-二甲基-1(S)-(N-甲基氨甲酰)丙基]-N4-羟基-3(R)-(羟基甲基)-2(S)-(4-甲氧基苯基)琥珀酰胺Chemical Name: N1-[2,2-Dimethyl-1(S)-(N-methylcarbamoyl)propyl]-N4-hydroxy-3(R)-(hydroxymethyl)-2(S)-(4-methoxyphenyl)succinamide
C...
参考文献标题:Hydroxamic acid derivs.
文献作者:Kottirsch,G.; Neumann,U.(Novartis AG)
参考来源:EP 0929517; JP 2000508338; US 2002003804; US 6500983; WO 9814424

BN-80933

N1-[4-[4-[6-羟基-2,5,7,8-四甲基-3,4-二氢-2H-1-苯并哋-2(S)-羰基]哌嗪-1-基]苯基]噻吩-2-羧脚Chemical Name: N1-[4-[4-[6-Hydroxy-2,5,7,8-tetramethyl-3,4-dihydro-2H-1-benzopyran-2(S)-ylcarbonyl]piperazin-1-yl]phenyl]thiophene-2...
参考文献标题:Novel 2-(iminomethyl)amino-phenyl derivs.,preparation,application as medicines and pharmaceutical compsns.containing same
文献作者:Chabrier de Lassauniere,P.-E.; Auguet,M.; Auvin,S.; Bigg,D.(SCRAS (Societ?de Conseils de Recherches et d'Applications Scientifiques))
参考来源:EP 0973763; WO 9842696

PD-0220245

N1-[6,7-二氯-3-[5-(2-哌基)呻-2-基]喹沙林-2-基]-N4,N4-二乙基丁烷-1,4-二胺盐酸盐Chemical Name: N1-[6,7-Dichloro-3-[5-(2-thienyl)thien-2-yl]quinoxalin-2-yl]-N4,N4-diethylbutane-1,4-diamine hydrochloride
CAS No. 239094-97...
参考文献标题:Structure-activity relationship of 2-amino-3-heteroaryl-quinoxalines as potent,non-peptide interleukine-8-receptor antagonists
文献作者:Li,J.J.; Yue,W.-S.; Trivedi,B.K.; et al.
参考来源:220th ACS Natl Meet (Aug 20 2000,Washington DC) 2000,Abst MEDI 144

新产品编号:228317

N2-(顺-2-氨基环己基)-N6-(3-氯苯基)-9-乙基-9H-嘌呤-2,6-二胺Chemical Name: N2-(cis-2-Aminocyclohexyl)-N6-(3-chlorophenyl)-9-ethyl-9H-purine-2,6-diamine
CAS No. 190653-73-7, 190653-77-1 (trans-isomer)
项目整合开发状态: B...
参考文献标题:Purine derivs.and processes for their preparation
文献作者:Capraro,H.-G.; Zimmermann,J.; Furet,P.; Peterli,P.(Novartis AG)
参考来源:JP 1999514336; WO 9716452

Aranoza, Aranose, CRC-0510375

N-2-L-阿拉伯唑并丙环烯基-N-甲基-N-亚硝基脲Chemical Name: 3-(alpha-L-Arabinopyranosyl)-1-methyl-1-nitrosourea
CAS No. 167396-23-8, 95342-54-4 (alpha-D-isomer), 103667-91-0 (undefined isomer)
项目整合开发状态: Phase III...
参考文献标题:Method of synthesis of 3-(1-alpha-L-arabinopyranozyl)-1-methyl-1-nitrosourea (aranose) - an antitumor preparation
文献作者:Preobrazhenskaja,M.N.; Miniker,T.D.; Yartseva,I.V.; Kikot,B.S.; Nikitina,T.V.; Ignat'eva,E.V.; Pichugina,L.V.; Timofeeva,A.K.; Kenke,I.K.; Murkhanov,V.I.
参考来源:SU 1711456

Andolast, CR-2039

N-4-(1H-四唑-5-基)苯基-4-(1H-四唑-5-基)苯甲酰胺Chemical Name: 4-(1H-Tetrazol-5-yl)-N-[4-(1H-tetrazol-5-yl)phenyl]benzamide
CAS No. 132640-22-3
项目整合开发状态: Phase II
项目研究机构: Rotta (Originator)
合成路线:Coupli...
参考文献标题:Derivs.of N-phenylbenzamide with anti-ulcer and anti-allergy activity and a method for their preparation
文献作者:Makovec,F.; Peris,W.; Rovati,A.L.(Rotta Research Laboratorium SpA)
参考来源:EP 0460083; JP 1992503514; US 5232937; WO 9009989

Falnidamol, BIBX-1382, BIBX-1382BS

N4-(3-氯-4-氟-苯基)-N6-(1-甲基-4-哌啶)嘧啶并5,4-d嘧啶-4,6-二胺Chemical Name: 8-(3-Chloro-4-fluorophenylamino)-2-(1-methyl-4-piperidinylamino)pyrimido[5,4-d]pyrimidine; N8-(3-Chloro-4-fluorophenyl)-N2-(1-methyl-4-pip...
参考文献标题:Pyrimido[5,4-d]pyrimidines,medicaments containing these cpds.,their use and process for their production
文献作者:Himmelsbach,F.; Dahmann,G.; von R黡en,T.; Metz,T.(Dr.Karl Thomae GmbH)
参考来源:DE 19608588; EP 0888351; JP 2000506151; US 5821240; WO 9732880

GMC-1111

N6,N6-二丙基-6,7-二氢-5H-茚[5,6-d][1,3]噻唑-2,6-二胺 5H-茚(5,6-d)噻唑-2,6-二胺,6,7-二氢氮-N6,N6-二丙基-,二盐酸盐 Chemical Name: N6,N6-Dipropyl-6,7-dihydro-5H-indeno[5,6-d][1,3]thiazole-2,6-diamine; N-(2-Amino-6,7-dihydro-5H-i...
参考文献标题:New 2-aminothiazol-fused-2-aminoindans and 2-aminotetralins and their use
文献作者:Van Vliet,L.A.; Wikstr鰉,H.V.; Dukstra,D.; Gunne,L.; Carlsson,P.A.E.; Andr閚,P.E.
参考来源:WO 0001680