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

M-5011, T-3788, M-5010

(2R)-2-[4-(3-甲基噻吩-2-基)苯基]丙酸Chemical Name: 2(R)-[4-(3-Methyl-2-thienyl)phenyl]propionic acid
CAS No. 76604-64-3
项目整合开发状态: Phase II
项目研究机构: Maruho (Licensee)
合成路线:The Darzen's condensation o...
参考文献标题:2-[4-(3-Methyl-2-thienyl)phenyl]propionic acid derivs.and its non-toxic salts
文献作者:Kodama,T.; Nakabayashi,M.; Watanabe,I.; Hirano,Y.; Abe,N.; Tanaka,K.; Arai,H.(Toyama Chemical Co.,Ltd.)
参考来源:DE 2850485; JP 1981049376

Presinteine, ITA-275

(2R)-2-氨基-3-[(3-甲基丁-2-烯-1-基)硫]丙酸Chemical Name: S-(3-Methyl-2-butenyl)-L-cysteine
CAS No. 5287-46-7
项目整合开发状态: Not Determined
项目研究机构:
合成路线:By condensation of prenylchloride (I) with L-cyste...
参考文献标题:
文献作者:Adsar? J.; et al.
参考来源:BE 875717; DE P-29-16-118.0; ES 469060; FR 79/10579; GB 79-12686; IT 67786-A/79; JP 49625/79; US 31612

Bay-x-1005

(2R)-2-环戊基-2-[4-(喹啉-2-基甲氧基)苯基]乙酸苯醋酸,a-环戊酰-4-(2-喹林甲氧基)-Chemical Name: (R)-2-Cyclopentyl-2-[4-(quinolin-2-ylmethoxy)phenyl]acetic acid; (R)-alpha-Cyclopentyl-4-(2-quinolinylmethoxy)benzeneacetic acid 参考文献标题:Substd.4-(quinoline-2-yl-methoxy)phenyl-acetic acid derivs
文献作者:Mohrs,K.; Raddatz,S.; Perzborn,E.; Fruchtmann,R.; Kohlsdorfer,C.; M黮ler-Peddinghaus,R.; Theisen,P.(Bayer AG)
参考来源:AU 8935270; DE 3900261; EP 0344519; JP 1990019359; JP 1998053577; US 4970215

Pipethiadene tartrate, VUFB-12384

(2R,3R)-2,3-二羟基丁二酸:1-甲基-4-(5H-噻吩并[2,3-c][2]苯并硫杂卓-10-亚基)哌啶Chemical Name: 4-(1-Methyl-4-piperidylidene)-4,9-dihydrothieno[2,3-c][2]benzothiepin hydrogen (+)-tartrate; 4-(1-Methyl-4-piperidylidene)-4,9-d...
参考文献标题:Pipethiadene tartrate
文献作者:Protiva,M.
参考来源:Drugs Fut 1983,8(4),334

Atrasentan, A-147627, (+)-A-127722, ABT-627, Xinlay

(2R,3R,4S)-4-(1,3-苯并二氧戊环-5-基)-1-[2-(二丁基氨基)-2-氧代乙基]-2-(4-甲氧基苯基)吡咯烷-3-羧酸盐酸阿曲生坦 Chemical Name: 1-(N,N-Dibutylcarbamoylmethyl)-2(R)-(4-methoxyphenyl)-4(S)-(3,4-methylenedioxyphenyl)pyrrolidine-3(R)-carbo...
参考文献标题:Novel benzo-1,3-dioxolyl- and benzofuranyl substd.pyrrolidine derivs.as endothelin antagonists
文献作者:Winn,M.; Boyd,S.A.; Hutchins,C.W.; Tasker,A.S.; Von Geldern,T.W.; Kester,J.A.; Sorensen,B.K.; Szczepankiewicz,B.G.; Henry,K.J.Jr.; Liu,G.; Wittenberger,S.J.; King,S.A.(Abbott Laboratories Inc.)
参考来源:EP 0885215; WO 9730045

GW-3333

(2R,3S)-3-(甲基羟基氨基)-4-甲基-2-(2-甲基丙基)-N-[(1S,2S)-2-甲基-1-(吡啶-2-甲基甲酰)丁基]戊酰胺Chemical Name: Nalpha-[3(S)-(N-Hydroxyformamido)-2(R)-isobutyl-4-methylpentanoyl]-N1-(2-pyridyl)-L-isoleucylamide
CAS No. 21260...
参考文献标题:Reverse hydroxamate derivs.as metalloprotease inhibitors
文献作者:Chan,J.H.; Bubacz,D.G.; Andersen,M.W.; McDougald,D.L.; Stanford,J.B.; Andrews,R.C.; Gaul,M.D.; Rabinowitz,M.H.; Musso,D.L.; Cowan,D.J.; Wiethe,R.W.(GlaxoSmithKline plc)
参考来源:EP 1019386; JP 2001513767; WO 9838179

CP-195494

(2R,3S,4R)-N-[3-[6-(5-氟苯并噻唑-2-甲氧基)-4-羟基-2-甲基-3,4-二氢-2H-1-苯并吡喃-3-甲基]苯基]三氟甲酰磺酰胺Chemical Name: (2R,3S,4R)-N-[3-[6-(5-Fluorobenzothiazol-2-ylmethoxy)-4-hydroxy-2-methyl-3,4-dihydro-2H-1-benzopyran-3-ylmet...
参考文献标题:Development of new chromanol antagonists of leukotriene D4
文献作者:Chambers,R.J.; Antognoli,G.W.; Cheng,J.B.; Marfat,A.; Pillar,J.S.; Shirley,J.T.; Watson,J.W.
参考来源:Bioorg Med Chem Lett 1998,8(14),1791

N-Butylgalactonojirimycin, N-Butyldeoxygalactonojirimycin, CDP-923, OGT-923

(2R,3S,4R,5S)-1-丁基-2-(羟基甲基)-3,4,5-哌啶三醇Chemical Name: 1,5-(Butylimino)-1,5-dideoxy-D-galactitol; N-Butyldeoxygalactonojirimycin; (2R,3S,4R,5S)-1-Butyl-2-(hydroxymethyl)-3,4,5-piperidinetriol
CAS No....
参考文献标题:Novel deoxygalactonojirimycin derivs.
文献作者:Platt,F.M.; Neises,G.R.; Dwek,R.A.; Butters,T.D.(Pharmacia Corp.)
参考来源:EP 0698012; JP 1996510244; US 5399567; US 6291657; WO 9426714

Amdoxovir, (-)-DAPD, DAPD

(2R,4R)-4-(2,6-二氨基-9H-嘌呤-9-基)-1,3-二氧戊环-2-甲醇Chemical Name: (-)-(2R,4R)-4-(2,6-Diamino-9H-purin-9-yl)-2-(hydroxymethyl)-1,3-dioxolane; (2R,4R)-4-(2,6-Diamino-9H-purin-9-yl)-1,3-dioxolane-2-methanol
C...
参考文献标题:Enantiomerically pure beta-D-dioxolane-nucleosides
文献作者:Chu,C.K.; Schinazi,R.F.(Emory University; University of Georgia)
参考来源:US 5925643; WO 9404154

Vamicamide, FK-176, Urocut

(2R,4R)-4-二甲基氨基-2-苯基-2-吡啶-2-基戊酰胺Chemical Name: (?-(R*)-alpha-[(R*)-2-(Dimethylamino)propyl]-alpha-phenyl-2-pyridineacetamide; (?-(2R*,4R*)-4-(Dimethylamino)-2-phenyl-2-(2-pyridyl)pentanamide
CAS No...
参考文献标题:Synthesis and anticholinergic activity of the four stereoisomers of 4-(dimethylamino)-2-phenyl-2-(2-pyridyl)pentanamide
文献作者:Akahane,A.; Tada,T.; Matsuo,M.; Nagano,M.; Oyasu,H.; Tomoi,M.
参考来源:J Med Chem 1994,37(9),1378-81