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

Elliptinium acetate, NSC-264137, HME, Celiptium

依利醋铵 6H-吡啶[4,3-b]卡巴唑铵,9-羟基-2,5,11-三甲基-,碘化物(1:1) Chemical Name: 9-Hydroxy-2-methylellipticinium acetate; 9-Hydroxy-2,5,11-trimethyl-6H-pyrido[4,3-b]carbazolium acetate
CAS No. 58337-35-2, 58447-24-8...
参考文献标题:Derivatives of 9-hydroxy-ellipticine and a process fo their preparation
文献作者:Le Pecq,J.B.; et al.(ANVAR (Agence Natl.Valor.Rech.))
参考来源:CH 616937; DE 2618223; FR 2308365; GB 1508388

Epinastine

依匹斯汀Chemical Name: 3-Amino-9,13b-dihydro-1H-dibenz[c,f]imidazo[1,5-a]azepine
CAS No. 80012-43-7
项目整合开发状态: Launched
项目研究机构: Boehringer Ingelheim (Originator)
合成路线:By cyclization of 6-(amino...
参考文献标题:Fused dibenzo imidazolo compounds,compositions and use
文献作者:Walther,G.; Schneider,C.S,,Weber,K.-H.; Fuegner,A.(Boehringer Ingelheim GmbH)
参考来源:DE 3008944

Epinastine hydrochloride, WAL-801CL, Elestat, Relestat, Flurinol, Alesion

依匹斯汀Chemical Name: 3-Amino-9,13b-dihydro-1H-dibenz[c,f]imidazol[1,5-a]azepine hydrochloride
CAS No. 80012-43-7 (free base)
项目整合开发状态: Launched-1994
项目研究机构: Boehringer Ingelheim (Originator), N...
参考文献标题:New tetracyclic guanidine derivatives with H1-antihistaminic properties.Chemistry of epinastine
文献作者:Walther,G.; Bechtel,W.D.; Daniel,H.; Brandt,K.
参考来源:Arzneim-Forsch Drug Res 1990,40(4),440-6

Epiroprim, Ro-11-8958

依匹普林Chemical Name: 5-(3,5-Diethoxy-4-pyrrolidinobenzyl)pyrimidine-2,4-diamine
CAS No. 73090-70-7
项目整合开发状态: Phase I
项目研究机构: Roche (Originator)
合成路线:3,5-Dihydroxybenzoic acid (I) was carboxy...
参考文献标题:Epiroprim
文献作者:St鯿kel,K.; Kompis,I.; Then,R.L.; Stephan-G黮dner,M.; Hartman,P.G.
参考来源:Drugs Fut 1994,19(5),446

Ecadotril, Sinorphan, (S)-Acetorphan, S-049, BP-1.02, Bay-y-7432

依卡曲尔Chemical Name: N-[2(S)-(Acetylthiomethyl)-3-phenylpropionyl]glycine benzyl ester
CAS No. 112573-73-6
项目整合开发状态: Phase III
项目研究机构: Bioprojet (Originator), Bayer (Licensee)
合成路线:Reaction ...
参考文献标题:Enantiomeric derivs.of amino acids,process for their preparation and their pharmaceutical applications
文献作者:Duhamel,P.; Duhamel,L.; Danvy,D.; Plaquevent,J.-C.; Giros,B.; Gros,C.; Schwartz,J.-C.; Lecomte,J.-M.(Societe Civile Bioprojet)
参考来源:EP 0318377; FR 2623498; JP 1990000161; JP 1996059606; US 5296509; US 5331008

Ecabamide, Ecabapide, DQ-2511, Muralis

依卡派特Chemical Name: 3-[[2-[[2-(3,4-Dimethoxyphenyl)ethyl]amino]-2-oxoethyl]amino]-N-methylbenzamide
CAS No. 104775-36-2
项目整合开发状态: Phase III
项目研究机构: Daiichi Pharmaceutical (Originator)
合成路线:...
参考文献标题:Aminobenzamide derivatives
文献作者:Miki,T.; Asano,M.; Hosokami,T.(Daiichi Seiyaku Co.,Ltd.)
参考来源:EP 0185368

Edelfosine, Ro-14-5243, (?-ET-18-OMe, (?-ET-18-OCH3

依地芬Chemical Name: (?-1-O-Octadecyl-2-O-methyl-rac-glycero-3-phosphocholine; (?-4-Hydroxy-7-methoxy-N,N,N-trimethyl-3,5,9-trioxa-4-phosphaheptacosan-1-aminium hydroxide inner salt, 4-oxide
CAS No. 7...
参考文献标题:ET-18-OCH3
文献作者:Castar,R.M.; Castar,J.; Serradell,M.N.
参考来源:Drugs Fut 1987,12(4),341

Elbanizine, HWA-214

依巴尼嗪Chemical Name: 2,6-Dimethyl-3-nitro-4-[2-(4-diphenylmethyl-1-piperazinyl)ethylamino]pyridine; 1-[2-[(2,6-Dimethyl-3-nitro-4-pyridyl)amino]ethyl]-4-(diphenylmethyl)piperazine
CAS No. 110629-41-9...
参考文献标题:Pyridine derivs.
文献作者:(Aventis SA)
参考来源:DE 3541428; EP 0224159; JP 1987129271; US 4792554

Ebastine, RP-64305, LAS-W-090, W-090, Evastel, No-Sedat, Kestine, Bastel, Ebastel

依巴斯汀Chemical Name: 4'-tert-Butyl-4-[4-(diphenylmethoxy)piperidin-1-yl]butyrophenone; 4-Diphenylmethoxy-1-[3-(4-tert-butylbenzoyl)propyl]piperidine
CAS No. 90729-43-4
项目整合开发状态: Launched-1990
项...
参考文献标题:EBASTINE
文献作者:Moragues,J.; Roberts,D.J.
参考来源:Drugs Fut 1990,15(7),674

Etonogestrel, Org-3236

依托孕烯Chemical Name: (17alpha)-13-Ethyl-17-hydroxy-11-methylene-18,19-dinorpregn-4-en-20-yn-3-one; 13-Ethyl-11-methylene-18,19-dinor-17alpha-pregn-4-en-20-yn-3-one-17-ol; 11-Methylene-17alpha-ethynyl-17...
参考文献标题:ORG-3236
文献作者:Hillier,K.; Castar,J.
参考来源:Drugs Fut 1978,3(9),664