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

Ravuconazole, BMS-207147, ER-30346

立福康唑Chemical Name: 4-[2-[2(R)-(2,4-Difluorophenyl)-2-hydroxy-1(R)-methyl-3-(1,2,4-triazol-1-yl)propyl]thiazol-4-yl]benzonitrile; (2R,3R)-3-[4-(4-Cyanophenyl)thiazol-2-yl]-2-(2,4-difluorophenyl)-1-(1H-...
参考文献标题:Azole antifungal agents,process for the preparation thereof and intermediates
文献作者:Naito,T.; Hata,K.; Kaku,Y.; Tsuruoka,A.; Tsukada,I.; Yanagisawa,M.; Toyosawa,T.; Nara,K.(Eisai Co.,Ltd.)
参考来源:CA 2141731; EP 0667346; JP 1995223950; JP 1996020578; JP 1996053426; US 5648372; US 5789429; US 5792781

Remacemide hydrochloride, FPL-12924AA, PR-1032-646 [(-)-isomer], PR-1032-644 [(+)-isomer], PR-934-423A

立马醋胺盐酸瑞马酰胺 Chemical Name: (?-2-Amino-N-(1-methyl-1,2-diphenylethyl)acetamide hydrochloride; (?-N1-(1-Methyl-1,2-diphenylethyl)glycinamide hydrochloride
CAS No. 128298-28-2 (free base), 111686-79-4...
参考文献标题:Preparation of remacemide hydrochloride labelled with carbon-14,carbon-13,deuterium and tritium
文献作者:Dawson,G.E.; Coombs,M.E.; Fedorchuk,M.; et al.
参考来源:J Label Compd Radiopharm 2000,43(6),533

Mixidine fumarate, McN-1589(free base)

米克昔定Chemical Name: N-[2-(3,4-Dimethoxyphenyl)ethyl]-N-[1-methylpyrrolidin-2-ylidene]amine fumarate
CAS No. 27737-38-8, 67958-13-8 (free base)
项目整合开发状态: Biological Testing
项目研究机构:
合成路线:By ...
参考文献标题:
文献作者:Poos,G.I.
参考来源:CA 850116; CH 536301; FR 1576111; FR M8129; GB 1210848; JP 7425266; JP 7530618; JP 7539662

Milrinone lactate, YM-018, Win-47203, Corotrope, Primacor

米力农Chemical Name: 2-Methyl-6-oxo-1,6-dihydro-[(3,4'-bipyridine)-5-carbonitrile lactate
CAS No. 78415-72-2 (free base)
项目整合开发状态: Launched-1988
项目研究机构: Sanofi-Aventis (Originator)
合成路线:The c...
参考文献标题:5-(pyridinyl)-2(1H)-pyridinones,useful as cardiotonic agents and their preparation
文献作者:Lehser,G.Y.; Philion,R.E.; Page,D.F.; Opalka,C.J.(Sterling Winthrop Inc.)
参考来源:DE 3044568; FR 2470124; GB 2065642; NL 8006399

Micafungin sodium, FK-463, Mycamine, Funguard

米卡芬净钠米卡芬净 Chemical Name: (3S,6S,9S,11R,15S,18S,20R,21R,24S,25R,26S)-3-[3-Amino-1(R)-hydroxy-3-oxopropyl]-6-[1(S),2(S)-dihydroxy-2-(4-hydroxy-3-sulfooxyphenyl)ethyl]-11,20,21,25-tetrahydroxy-15-[1(R)-...
参考文献标题:Cyclic hexapeptides having antibiotic activity
文献作者:Ohki,H.; Tomishima,M.; Yamada,A.; Takasugi,H.(Fujisawa Pharmaceutical Co.,Ltd.)
参考来源:EP 0788511; JP 1998324695; JP 1998507174; US 6107458; WO 9611210

Miglitol, SK-983, Bay-m-1099, Plumarol, Diastabol, Glyset

米各尼醇Chemical Name: 1,5-Dideoxy-1,5-[(2-hydroxyethyl)imino]-D-glucitol; (2R,3R,4R,5S)-1-(2-Hydroxyethyl)-2-(hydroxymethyl)-3,4,5-piperidinetriol
CAS No. 72432-03-2
项目整合开发状态: Launched-1998
项目研究...
参考文献标题:Lipophilic prodrugs of 1-deoxynojirimycin derivatives
文献作者:Therisod,M.; Fouacea,S.
参考来源:Tetrahedron Lett 2000,41(38),7313

Midostaurin, PKC-412, CGP-41251

米哚妥林Chemical Name: N-[(9S,10R,11R,13R)-10-Methoxy-9-methyl-1-oxo-9,13-epoxy-2,3,10,11,12,13-hexahydro-1H,9H-diindolo[1,2,3-gh:3',2',1'-lm]pyrrolo[3,4-j][1,7]benzodiazonin-11-yl]-N-methylbenzamide; N-B...
参考文献标题:Staurosporine derivs.substd.for the nitrogen atom of the methylamino group
文献作者:Caravatti,G.; Fredenhagen,A.(Novartis AG)
参考来源:EP 0296110; JP 1989034989; US 5093330

Midesteine, MR-889

米地司坦Chemical Name: N-(2-oxo-2,3,4,5-tetrahydro-3-thienyl)-2-(2-thienylcarbonylthio)propionamide; 2-Thiophenecarbothioic acid S-[1-methyl-2-oxo-2-[(2-oxotetrahydro-3-thienyl)amino]ethyl] ester
CAS N...
参考文献标题:MR-889
文献作者:Quadro,G.
参考来源:Drugs Fut 1990,15(10),997

Azolastone, Mitozolomide, CCRG-81080, NSC-353451, M&B-39565, 46241-RP

米托唑胺Chemical Name: 3-(2-Chloroethyl)-3,4-dihydro-4-oxoimidazo[5,1-d]-as-tetrazine-8-carboxamide; 8-Carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3H)-one
CAS No. 85622-95-3
项目整合开发状...
参考文献标题:Tetrazine derivs.,process for their preparation and pharmaceutical compsns.containing them
文献作者:Lunt,E.; Stevens,M.F.G.; Stone,R.; Woolbridge,K.R.H.(Cancer Research Campaign Technology Ltd.)
参考来源:BE 894175; DE 3231255; FR 2511679; GB 2104522; JP 1983043975; US 5260291

Flavoneacetic acid, Mitoflaxone, CRC-85/31, LM-975, FAA, NSC-347512

米托拉酮Chemical Name: 4-Oxo-2-phenyl-4H-1-benzopyran-8-acetic acid
CAS No. 87626-55-9
项目整合开发状态: Phase II
项目研究机构: Lipha (Originator)
合成路线:Treatment of 8-bromomethyl-2-phenylflavone (I) with KC...
参考文献标题:8-Haloalkyl-4H-(1)-benzopyran-4-ones and preparati
文献作者:Berthelon,J.-J.; Collonges,F.; Briet,P.(Lipha Sant?
参考来源:EP 0080419