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

BMS-433771

1-环丙基-3-((1-(3-羟丙基)-1H-苯并[d]吡达唑-2-基甲基)-1H-吡啶[4,5-c]吡啶-2(3H)-1Chemical Name: 1-Cyclopropyl-3-[1-(3-hydroxypropyl)-1H-benzimidazol-2-ylmethyl]-2,3-dihydro-1H-imidazo[4,5-c]pyridin-2-one
CAS No. 38060...
参考文献标题:Imidazopyridine and imidazopyrimidine antiviral agents
文献作者:Meanwell,N.A.; Yu,K.-L.; Combrink,K.D.; Wang,X.; Civiello,R.L.; Gulgeze,H.B.; Sin,N.; Venables,B.L.(Bristol-Myers Squibb Co.)
参考来源:EP 1311268; US 2002016309; US 6489338; WO 0195910

Alifedrine hydrochloride, D-13625

1-环己基-3-[[(1R,2S)-1-羟基-1-苯基丙烷-2-基]氨基]丙-1-酮盐酸盐阿利非君 Chemical Name: 1-Cyclohexyl-3-[(1S,2R)-2-hydroxy-1-methyl-2-phenethylamino]propan-1-one hydrochloride; 1-Cyclohexyl-3-[[(alphaS,betaR)-beta-hydroxy-a...
参考文献标题:Alifedrine
文献作者:B鋒re,M.; Thiemer,K.; Engel,J.; Breuel,H.P.; Stroman,F.; Kleemann,A.
参考来源:Drugs Fut 1984,9(10),727

LY-426965

1-环己基-4-[4-(2-甲氧基苯基)-1-哌嗪基]-2-甲基-2-苯基-1-丁酮Chemical Name: (+)-1-Cyclohexyl-4-[4-(2-methoxyphenyl)piperazin-1-yl]-2(S)-methyl-2-phenylbutan-1-one monohydrochloride
CAS No. 228418-79-9 (undefined isom...
参考文献标题:Arylpiperazines having activity at the serotonin 1A receptor
文献作者:Kohlman,D.T.; O'Toole,J.C.; Godfrey,A.G.; Xu,Y.-C.; Zhang,T.Y.(Eli Lilly and Company)
参考来源:EP 0924205; WO 9931077

SR-265579, WIN-65579

1-环戊基-6-(3-乙氧基-4-吡啶基)-3-乙基-4,5-二氢-1H-吡唑并[3,4-d]嘧啶-4-酮Chemical Name: 1-Cyclopentyl-6-(3-ethoxy-4-pyridinyl)-3-ethyl-4,5-dihydro-1H-pyrazolo[3,4-d]pyrimidin-4-one
CAS No. 158020-82-7
项目整合开发状态: Pre...
参考文献标题:6-Heterocyclyl pyrazolo[3,4-d]pyrimidin-4-ones and compsns.and method of use
文献作者:Bacon,E.R.; Singh,B.; Lesher,G.Y.; Lesher,L.E.(Sanofi-Synthabo)
参考来源:US 5294612

D-21151

1-苯氧基二氮杂萘Chemical Name: 1-Phenoxyphthalazine
CAS No. 100537-30-2
项目整合开发状态: Preclinical
项目研究机构: Asta Medica (Originator)
合成路线:D-21151 is easily obtained by a two-step sequence starting from...
参考文献标题:Phthalazines substd.on position 1 by an ether or a thioether group and process for their preparation
文献作者:Scheffler,G.; Fleischhauser,I.; Kutscher,B.; Engel,J.; Szelenyi,S.; Werner,U.(Asta Medica AG)
参考来源:DE 4234933; EP 0539805; JP 1993222002

Piberaline fumarate, EGYT-475, Trelibet

1-苯甲基-4-(2-吡啶基羰基)哌拉嗪(E)-2-丁烯二酸盐(1:1)吡贝拉林Chemical Name: 1-Phenylmethyl-4-(2-pyridylcarbonyl)piperazine (E)-2-butenedioate (1:1); 1-Benzyl-4-picolinoylpiperazine fumarate (1:1)
CAS No. 39640-14-7, 39...
参考文献标题:Preparation of pyridinecaboxylic acid piperazides
文献作者:Budai,Z.; Mezei,T.; Lay,A.(Egis Pharmaceuticals Ltd.)
参考来源:DE 2828888; GB 2001062; HU 175075

FK-448

1-萘羧酸,1,2,3,4-四氢,4-(4-(1-甲基乙基)-1-吡嗪基)羰基)苯酯,单甲烷磺酸盐Chemical Name: 1,2,3,4-Tetrahydro-1-naphthalenecarboxylic acid 4-[[4-(1-methylethyl)-1-piperazinyl]carbonyl]phenyl ester monomethanesulfonate
CAS No...
参考文献标题:Benzoylpiperazine esters and a process for their production
文献作者:Fujii,S.; Hattori,E.; Hirata,M.; Watanabe,K.; Onogi,K.; Nagakura,M.(Kowa Co.,Ltd.)
参考来源:EP 0098713; JP 83225080; US 4898876

FR-110302

1-萘醇,2,2-丁基-1,2,3,4-四氢-5-(2-喹啉甲氧基)-Chemical Name: (+)-2,2-Dibutyl-5-(2-quinolylmethoxy)-1,2,3,4-tetrahydro-1-naphthol
CAS No. 119257-22-6, 119257-23-7 (HCl), 119256-94-9 (undefined isomer)
项目整合开...
参考文献标题:Studies on 5-lipoxygenase inhibitors.II.Discovery,optical resolution and enantioselective synthesis of FR110302,a highly potent non-redox type 5-lipoxygenase inhibitor
文献作者:Yatabe,T.; Kayakiri,H.; Kawai,Y.; Oku,T.; Tanaka,H.
参考来源:Chem Pharm Bull 1998,46(10),1556

NC-1300

2-((2-二甲基氨基苄基)亚磺酰)苯并咪唑Chemical Name: 2-[2-(Dimethylamino)benzylsulfinyl]benzimidazole
CAS No. 100924-68-3
项目整合开发状态: Phase II
项目研究机构: Nippon Chemiphar (Originator)
合成路线:By condensation of p...
参考文献标题:Benzimidazole derivs.and antiulcer agents contain
文献作者:Susumu,O.; Masaru,S.; Tomio,Y.; Yutaka,N.; Masatoshi,H.(Nippon Chemiphar Co.,Ltd.)
参考来源:AU 8546409; BE 0903128; CH 665417; DE 3531487; ES 8703142; FR 2569691; GB 2163747; JP 1986060660; JP 1986221175; JP 1986221176; JP 1991223260; JP 1991223261; JP 1991223262; JP 1991227927

SDZ-NDD-094, NDD-094

2-((2-甲基-1h-咪唑-1-基)甲基)吡啶Chemical Name: Bis[2-(2-methylimidazol-1-ylmethyl)pyridine] trifumarate
CAS No. 148257-48-1 (free base)
项目整合开发状态: Phase II
项目研究机构: Novartis (Originator)
合成路线:The co...
参考文献标题:Imidazolylmethyl-pyridines
文献作者:Giger,R.K.A.(Novartis AG; Novartis Deutschland GmbH)
参考来源:DE 4131584; EP 0534904; JP 1993194491; US 5635521