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

Darbufelone mesilate, PD-136095-0073, CI-1004

甲磺酸达布非龙 (5Z)-2-氨基-5-[(4-羟基-3,5-二叔丁基苯基)亚甲基]-1,3-噻唑-4-酮 (5z)-5-[4-羟基-3,5-双(2-甲基-2-丙烯基)苄苯]-2-伊明 O-1,3-噻唑烷-4-1Chemical Name: (Z)-2-Amino-5-(3,5-di-tert-butyl-4-hydroxybenzylidene)thiazol-4(5H)-one methan...
参考文献标题:3,5-Di-tertiary-butyl-4-hydroxyphenyl-methylene derivs.of 2-substd.thiazolidinones,oxazolidinones,and imidazolidinones as antiinflammatory agents
文献作者:Cetenko,W.A.; Connor,D.T.; Sircar,J.C.; Sorenson,R.J.; Unangst,P.C.(Pfizer Inc.)
参考来源:EP 0449216; JP 1992221371; US 5143928

Danofloxacin mesylate, CP-76136-27, Advocin

甲磺酸达氟沙星达诺沙星 Chemical Name: 1-Cyclopropyl-6-fluoro-7-[(1S,4S)-5-methyl-2,5-diazabicyclo[2.2.1]hept-2-yl]-4-oxo-1,4-dihydroquinoline-3-carboxylic acid monomethanesulfonate
CAS No. 119478-55-6, 1123...
参考文献标题:The synthesis and antibacterial activity of danofloxacin (CP-76,136): A new quinolone for veterinary medicine
文献作者:Jefson,M.R.; Shryock,T.R.; Schaaf,T.K.; McGuirk,P.R.
参考来源:29th Intersci Conf Antimicrob Agents Chemother (Sept 17-20,Houston) 1989,Abst 1187

Rasagiline mesilate, TVP-1012, (+)-AGN-1135, Agilect

甲磺酸雷沙吉兰雷沙吉兰 Chemical Name: 1(R)-(Propargylamino)indane methanesulfonate; 1(R)-(2-Propynylamino)indane methanesulfonate; (R)-N-2-Propynyl-1-indanamine methanesulfonate
CAS No. 161735-79-1, 136236-...
参考文献标题:R-Enantiomers of N-propargyl-1-aminoindan cpds.,their preparation and pharmaceutical compsns.containing them
文献作者:Youdim,M.B.H.; Finberg,J.P.M.; Levy,R.; Sterling,J.; Lerner,D.; Berger-Paskin,T.(Teva Pharmaceutical Industries Ltd.)
参考来源:EP 0436492; JP 1991294248; US 5453446

Denzimol, Rec-151533

登齐醇Chemical Name: (?-1-[(4-Phenethyl)phenyl]-2-(N-imidazolyl)ethanol; (?-alpha-(p-Phenethylphenyl)imidazole-1-ethanol; (?-alpha-[4-(2-Phenylethyl)phenyl]-1H-imidazole-1-ethanol
CAS No. 73931-96-1<...
参考文献标题:Imidazole derivs.
文献作者:Nardi,D.; Tajana,A.; Magistretti,M.J.(Recordati Industria Chimica e Farmaceutica SpA)
参考来源:DE 2929777

Ivabradine hydrochloride, S-16260-2 (R-isomer), S-16257-2, S-16257, Procoralan

盐酸伊伐布雷定伊伐雷定 Chemical Name: (+)-3-[3-[N-[4,5-Dimethoxybenzocyclobutan-1(S)-ylmethyl]-N-methylamino]propyl]-7,8-dimethoxy-2,3,4,5-tetrahydro-1H-3-benzazepin-2-one hydrochloride
CAS No. 148849-67-6,...
参考文献标题:Benzocyclobutyl- or indanyl-alkyl-amino-alkyl substd.3-benzazepin-2-ones useful in the treatment of cardiovascular diseases
文献作者:Peglion,J.-L.; Vian,J.; Vilaine,J.-P.; Villeneuve,N.; Janiak,P.; Bidouard,J.-P.(ADIR et Cie.)
参考来源:EP 0534859; FR 2681862; JP 1993213890; US 5296482

Clinafloxacin, CI-960(hydrochloride), Bay-v-3545, PD-127391, AM-1091

盐酸克林沙星克林沙星Chemical Name: (?-7-(3-Amino-1-pyrrolidinyl)-8-chloro-1-cyclopropyl-6-fluoro-1,4-dihydro-4-oxo-3-quinolinecarboxylic acid
CAS No. 122842-92-6 (HCl), 105956-99-8 (monoHCl), 105956-97-6 ...
参考文献标题:7-(1-Pyrrolidinyl)-3-quinolinecarboxylic acid derivs.
文献作者:Irikura,T.; Suzue,S.; Murayama,S.; Hirai,K.; Ishizaki,T.(Kyorin Pharmaceutical Co.,Ltd.)
参考来源:AU 8542829; AU 8654272; EP 0195316; EP 0195841; ES 8606330; ES 8704932; JP 1986205235; JP 1986205237; JP 1986205238; JP 1986205239; JP 1986205258; JP 1986205259

Halofantrine hydrochloride, SK&F-102866, WR-171669, Halfan

盐酸卤泛群卤方特瑞 Chemical Name: (?-1,3-Dichloro-9-[3-(dibutylamino)-1-hydroxypropyl]-6-(trifluoromethyl)phenanthrene hydrochloride
CAS No. 36167-63-2, 69756-53-2 (free base), 66051-63-6 (racemic, free b...
参考文献标题:Halofantrine hydrochloride
文献作者:Hillier,K.; Castar,J.; Blancafort,P.; Serradell,M.N.
参考来源:Drugs Fut 1980,5(11),547

Pioglitazone hydrochloride, AA-10090, U-72107(free base), U-72107A, U-72107E(as AcOH solvate), AD-4833(free base), Glustin, Zactos, Actos

盐酸吡格列酮匹格列酮匹格列酮Chemical Name: (?-5-[4-[2-(5-Ethylpyridin-2-yl)ethoxy]benzyl]thiazolidine-2,4-dione monohydrochloride
CAS No. 112529-15-4, 111025-46-8 (free base), 105355-27-9 (free base, undefin...
参考文献标题:Thiazolidinedione derivs.,their production and use
文献作者:Meguro,K.; Fujita,T.(Takeda Chemical Industries,Ltd.)
参考来源:EP 0193256; ES 8705886; JP 1986267580; US 4687777

Cefozopran hydrochloride, SCE-2787.HCl, Firstcin

盐酸头孢唑兰头孢唑兰Chemical Name: [6R-[6alpha,7beta(Z)]]-1-[[7-[[(5-Amino-1,2,4-thiadiazol-3-yl)(methoxyimino)acetyl]amino]-2-carboxy-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-en-3-yl]methyl]-1H-imidazo[1,2-b]py...
参考文献标题:Antibacterial cpds.,their production and use
文献作者:Miyake,A.; Kondo,M.; Fujino,M.(Takeda Chemical Industries,Ltd.)
参考来源:AU 8541700; AU 8654168; EP 0160252; EP 0203271; ES 8606363; ES 8705892; ES 8706692; ES 8707245; JP 1985231684; JP 1987149682; WO 8504879; WO 8505620; WO 8605183; WO 8605184

Cefmenoxime hydrochloride, SCE-1365(free acid), Bestron, Cemix, Tacef, Bestcall

盐酸头孢甲肟Chemical Name: 7beta-[2-(2-Aminothiazol-4-yl)-(Z)-2-(methoxyiminoacetamido)]-3-[(1-methyl-1H-tetrazol-5-yl)thiomethyl]ceph-3-em-4-carboxylic acid hemihydrochloride; 7-[[(2-Amino-4-thiazolyl)(me...
参考文献标题:Thiazolylacetamido cephasloporin type compounds
文献作者:Ochiai,M.; et al.(Takeda Chemical Industries,Ltd.)
参考来源:DE 2556736; ES 464772; FR 2294690; GB 1536283; NL 7514811; US 4098888