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

BXL-628, Ro-26-9228

艾洛骨化醇Chemical Name: (23E)-1alpha-Fluoro-25-hydroxy-16,17,23,24-tetradehydro-26,27-bishomo-20-epivitamin D3; (23E)-1alpha-Fluoro-25-hydroxy-16,17,23,24-tetradehydro-26,27-bishomo-20-epicholecalciferol...
参考文献标题:Vitamin D3 analogs
文献作者:Batcho,A.D.; Bryce,G.F.; Hennessy,B.M.; Iacobelli,J.A.; Uskokovic,M.R.(F.Hoffmann-La Roche AG)
参考来源:EP 0808833; JP 1998045713; US 5939408

Icopezil maleate, CP-118954-11, CP-118954

艾考哌齐 Chemical Name: 3-[2-(1-Benzylpiperidin-4-yl)ethyl]-6,7-dihydro-5H-pyrrolo[3,2-f]-1,2-benzisoxazol-6-one maleate salt (1:1)
CAS No. 145815-98-1, 145508-78-7 (free base)
项目整合开发状态: Phase II 参考文献标题:5,7-Dihydro-3-[2-[1-(phenylmethyl)-4-piperidinyl]ethyl]-6H-pyrrolo[3,2-f]-1,2-benzisoxaxol-6-one: A potent and centrally-selective inhibitor of acetylcholinesterase with an improved margin of safety
文献作者:Villalobos,A.; Butler,T.W.; Chapin,D.S.; Chen,Y.L.; DeMattos,S.B.; Ives,J.L.; Jones,S.B.; Liston,D.R.; Nagel,A.A.; Nason,D.M.; et al.
参考来源:J Med Chem 1995,38(15),2802

Ruprintrivir, AG-7088

芦平曲韦Chemical Name: 4(S)-[2(R)-(4-Fluorobenzyl)-6-methyl-5(S)-(5-methylisoxazol-3-ylcarboxamido)-4-oxoheptanamido]-5-[2-oxo-3(S)-pyrrolidinyl]-2(E)-pentenoic acid ethyl ester
CAS No. 223537-30-2 参考文献标题:3-Phenylpyrrole alpha-1 adrenergic cpds.
文献作者:Meyer,M.D.; Daanen,J.F.; Ehrlich,P.P.; Ralston,J.W.(Abbott Laboratories Inc.)
参考来源:WO 9957122

Fenbufen, CL-82204, Lederfen, Cinopal

芬布芬Chemical Name: 4-(4-Biphenylyl)-4-oxobutyric acid
CAS No. 36330-85-5
项目整合开发状态: Launched-1976
项目研究机构: Wyeth Pharmaceuticals (Originator)
合成路线:By condensation of biphenyl (I) and succini...
参考文献标题:Compositions containing substituted benzoylpropionic acids and method of use to treat inflammation and pain
文献作者:Tomeufeik,A.; et al.(American Cyanamid Co.)
参考来源:DE 2147111; FR 2107848; GB 1320076; US 3784701

RS-635

苯丁酸,4-[5,5,6,6,6-五氟-1-[[[(4-氟苯基)磺酰]氨基]己基]- Chemical Name: (+)-4-[4-[5,5,6,6,6-Pentafluoro-1-(4-fluorophenylsulfonamido)hexyl]phenyl]butanoic acid
CAS No. 208118-97-2, 207987-59-5 (undefined isomer...
参考文献标题:Benzenesulfonamide derivs.and drugs containing the same
文献作者:Yasuda,S.; Ogawa,N.; Sakurai,S.(Hokuriku Seiyaku Co.,Ltd.)
参考来源:EP 0943606; JP 1998195038; WO 9821177

Tecalcet hydrochloride, NPS-568R, KRN-568, R-568, NPS-R-568, Norcalcin

苯丙萺,2-氯-酼-[(1R)-1-(3-甲氧基苯基)乙基]- Chemical Name: 3-(2-Chlorophenyl)-N-[1(R)-(3-methoxyphenyl)ethyl]propylamine hydrochloride
CAS No. 177172-49-5, 148717-54-8 (free base)
项目整合开发状态: Phase II
项目研...
参考文献标题:Method of making a benzylpropanamine
文献作者:D'Ambra,T.E.; Vanwagenen,B.C.; Duff,S.R.; Nelson,W.A.(NPS Pharmaceuticals,Inc.)
参考来源:WO 9602492

Binodalina, Binedaline, Sgd-Sch-1059, Scha-1059

苯奈达林 1,2-乙二胺,N1,N1,N2-三甲基-N2-(3-苯基-1H-鐲哚-1-基)-,盐酸盐(1:1) Chemical Name: 1-[N-[2-(Dimethylamino)ethyl]-N-methylamino]-3-phenylindole; N,N,N'-Trimethyl-N'-(3-phenyl-1H-indol-1-yl)-1,2-ethanediamine
C...
参考文献标题:N-Amino indole derivatives having pharmacological activity
文献作者:Schatz,F.; et al.(Siegfried AG)
参考来源:US 4204998

CX-546

苯并二氧六环-6-(1-哌啶基)甲酰胺 Chemical Name: 1-(2,3-Dihydro-1,4-benzodioxin-6-ylcarbonyl)piperidine
CAS No. 205510-63-0, 215923-54-9
项目整合开发状态: Preclinical
项目研究机构: Cortex (Originator), University of Ca...
参考文献标题:Endocrine modulation with positive modulators of AMPA type glutamate receptors
文献作者:Van der Klish,P.; Lynch,G.(University of California,Oakland)
参考来源:US 6329368; WO 9850036

Centchroman, Ormeloxifene, 6720-CDRI, Centron, Saheli, Choice 7

苯并吡喃 Chemical Name: (?-trans-1-[2-[4-(7-Methoxy-2,2-dimethyl-3-phenyl-3,4-dihydro-2H-1-benzopyran-4-yl)phenoxy]ethyl]pyrrolidine; (?-trans-7-Methoxy-2,2-dimethyl-3-phenyl-4-[4-(2-pyrrolidinoethoxy)ph...
参考文献标题:Centchroman
文献作者:Castar,J.; Hillier,K.
参考来源:Drugs Fut 1977,2(7),441

BRL-32872(free base), BRL-32872A

苯扎米,N-(3,4-二甲氧基苯基)-N-[3-[[[2-(3,4-二甲氧基苯基)乙基]甲基氨基]丙基]-4-硝基-盐酸盐(1:1) Chemical Name: N-(3,4-Dimethoxyphenyl)-N-[3-[N'-methyl-N'-[2-(3,4-dimethoxyphenyl)ethyl]amino]propyl]-4-nitrobenzamide hydrochloride...
参考文献标题:Synthesis,electrophysiological properties and analysis of structural requirements of a novel class of antiarrhythmic agents with potassium and calcium channel blocking properties
文献作者:Nadler,G.; Faivre,J.F.; Forest,M.C.; Cheval,B.; Martin,M.; Souchet,M.; Gout,B.; Bril,A.
参考来源:Bioorg Med Chem 1998,6(11),1993