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

Daxalipram, Mesopram

美索普兰-13C-D3Chemical Name: (-)-(R)-5-(4-Methoxy-3-propoxyphenyl)-5-methyloxazolidin-2-one
CAS No. 189940-24-7
项目整合开发状态: Phase II
项目研究机构: Schering AG (Originator)
合成路线:3'-Methoxy-4'-propylox...
参考文献标题:Chiral methyl phenyl oxazolidinones
文献作者:Laurent,H.; Ottow,E.; Kirsch,G.; Wachtel,H.; Schneider,H.; Faulds,D.; Dinter,H.(Schering AG)
参考来源:DE 19540475; EP 0859766; JP 1999513093; US 6025376; WO 9715561

Mespirenone, ZK-94679, SH-467

美螺利酮Chemical Name: 15alpha,16alpha-Dihydro-17-hydroxy-7alpha-mercapto-3-oxo-3'H-cyclopropa[15,16]-17alpha-pregna-1,4,15-triene-21-carboxylic acid,gamma-lactone acetate
CAS No. 87952-98-5
项目整合开发状...
参考文献标题:7alpha-Acylthio-15,16-methylene-3-oxo-17alpha-pregna-1,4-diene-21,17-carbonolactones,their preparation and use as medicinal agents
文献作者:Bittler,D.; Laurent,H.; Losert,W.; Nickisch,K.; Wiechert,R.(Schering AG)
参考来源:DE 3227598; US 4500522

Menogaril, TUT-7, U-52047, 7-Omen, NSC-269148, Tomosar

美诺立尔美诺立尔 Chemical Name: (2R,3S,4R,5R,6R,11R,13R)-4-(Dimethylamino)-3,4,5,6,11,12,13,14-octahydro-3,5,8,10,13-pentahydroxy-11-methoxy-6,13-dimethyl-2,6-epoxy-2H-naphthaceno[1,2-b]oxocine-9,16-dione 参考文献标题:7-Con-O-methylnogarol
文献作者:Cabanillas,F.; Castar,J.
参考来源:Drugs Fut 1980,5(8),400

Mefenidil, McN-2378-46(fumarate), McN-2378

美非尼地 L-丝氨酸,N-(1-甲基乙基)-,甲基酯 Chemical Name: 5-Methyl-2-phenyl-1H-imidazole-4-acetonitrile; 4-Cyanomethyl-2-phenyl-5-methylimidazole
CAS No. 58261-91-9, 83153-38-2 (fumarate)
项目整合开发状态: Biological T...
参考文献标题:McN-2378
文献作者:Blancafort,P.; Hillier,K.; Serradell,M.N.; Castar,J.
参考来源:Drugs Fut 1982,7(4),262

Oxaprotiline hydrochloride(Rec INNM, USAN), C-49802-B-Ba

羟丙替林羟丙替林 Chemical Name: 1-(3-Methylamino-2-hydroxy-1-propyl)dibenzo[b,e]bicyclo[2.2.2]octadine hydrochloride; alpha-(Methylaminomethyl)-9,10-dihydro-9,10-ethanoanthracene-9(10H)-ethanol hydrochloride...
参考文献标题:C-49802-B-Ba and CGP-6085A
文献作者:Castar,J.
参考来源:Drugs Fut 1978,3(6),429

Droxicainide, S-1249, AL-S-1249

羟卡尼Chemical Name: (?-N-(2,6-Dimethylphenyl)-1-(2-hydroxyethyl)piperidine-2-carboxamide
CAS No. 78421-12-2
项目整合开发状态: Biological Testing
项目研究机构:
合成路线:A pyridine carboxylic acid anilide (III...
参考文献标题:Droxicainide
文献作者:Aberg,G.
参考来源:Drugs Fut 1983,8(6),492

Transcainide, R-54718

群司卡尼Chemical Name: (?-trans-4-(Dimethylamino)-N-(2,6-dimethylphenyl)-1-(2-hydroxycyclohexyl)-4-piperidinecarboxamide
CAS No. 88296-62-2
项目整合开发状态: Phase II
项目研究机构: Janssen (Originator)
合成路线...
参考文献标题:N-Aryl-alpha-aminocarboxamide derivs.
文献作者:De Bruyn,M.F.L.; Van Daele,G.H.P.; Verdonck,M.G.C.(Janssen Pharmaceutica NV)
参考来源:EP 0121972; ES 8506615

Trandolapril, RU-44570, Preran, Mavik, Tarka(comb. with verapamil), Udrik, Gopten, Odrik

群多普利Chemical Name: (2S,3aR,7aS)-1-[(S)-N-[(S)-1-Carboxy-3-phenylpropyl]alanyl]hexahydro-2-indolinecarboxylic acid 1-ethyl ester; (3aR,7aS)-1-[N-[1(S)-(Ethoxycarbonyl)-3-phenylpropyl]-(S)-alanyl]octahy...
参考文献标题:Novel bicyclic amino acid derivs.,process for their preparation and their use ,as well as bicyclic amino acids as intermediates and process for their preparation
文献作者:Ubach,H.; Henning,R.; Teetz,V.; Geiger,R.; Becker,R.; Gaul,H.(Aventis SA)
参考来源:DE 3151690; EP 0084164; EP 0170775; JP 1989301659; JP 1989301695

Carboxyamidotriazole, CAI, NSC-609974, L-651582

羧基酰胺Chemical Name: 5-Amino-1-[3,5-dichloro-4-(4-chlorobenzoyl)benzyl]-1,2,3-triazole-4-carboxamide
CAS No. 99519-84-3
项目整合开发状态: Phase III
项目研究机构: Merck & Co. (Originator), National Cancer Ins...
参考文献标题:5-(Amino or substd.amino)-1,2,3-triazoles
文献作者:Bochis,R.J.; Chabala,J.C.; Fisher,M.H.(Merck & Co.,Inc.)
参考来源:EP 0151529; JP 1985188376; US 4590201

Colestilan, Colestimide, MCI-196, Cholebine

考来替兰Chemical Name: 2-Methyl-1H-imidazole polymer with (chloromethyl oxirane); 2-Methylimidazole polymer with 1-chloro-2,3-epoxypropane
CAS No. 95522-45-5
项目整合开发状态: Launched-1999
项目研究机构: Mitsu...
参考文献标题:Oral hypocholesterolemic agents
文献作者:Nomura,T.; Hamada,Y.; Kurihara,Y.(Mitsubishi Chemical Corp.)
参考来源:JP 1992013627