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

Duloxetine hydrochloride, LY-248686(free base), LY-264453, Xeristar, Ariclaim, Yentreve, Cymbalta

度洛西汀盐酸度洛西汀Chemical Name: (+)-(S)-N-Methyl-3-(naphthalen-1-yloxy)-3-(2-thienyl)propylamine hydrochloride
CAS No. 116817-77-7, 116539-59-4 (free base), 136434-34-9 (HCl), 116817-86-8 (maleate)
...
参考文献标题:Asymmetric synthesis
文献作者:Berglund,R.A.(Eli Lilly and Company)
参考来源:EP 0650965; JP 1995188065; US 5362886

Doxercalciferol, TSA-840, One-alpha D2, 1alpha-D2, Hectorol

度骨化醇Chemical Name: 1alpha-Hydroxyvitamin D2; 1alpha-Hydroxyergocalciferol; 9,10-Secoergosta-5(Z),7(E),10(19),22(E)-tetraene-1alpha,3beta-diol
CAS No. 54573-75-0
项目整合开发状态: Launched-1999
项目研究机...
参考文献标题:Process for preparing 1-hydroxylated vitamin D cpds.from 5,6-trans-vitamin D cpds.
文献作者:Schnoes,H.K.; Paaren,H.E.; DeLuca,H.F.; Hamer,D.E.(Wisconsin Alumni Research Foundation)
参考来源:US 4265822

Isepamicin, HAPA-B, Sch-21420, Isepalline, Isepacin

异帕米星Chemical Name: 1-N-(S-3-Amino-2-hydroxypropionyl)betamycin; 1-N-(S-3-Amino-2-hydroxypropionyl)gentamycin B; (S)-O-6-Amino-6-deoxy-alpha-D-glucopyranosyl-(1--4)-O-[3-deoxy-4-C-methyl-3-(methylamin...
参考文献标题:Novel pseudotrisaccharides and methods for their production
文献作者:Daniels,P.J.L.; Testa,R.; Tattanahalli,L.; Mallams,A.K.; Wright,J.J.; Weinstein,M.J.; Wagman,G.H.(Schering Corp.)
参考来源:DE 2437160; FR 2240015; GB 1473733; US 4029882

Ifosfamide, NSC-109724, Z-4942, MJF-9325, Mitoxana, Holoxan, Ifex

异环磷酰胺Chemical Name: 3-(2-Chloroethyl)-2-(2-chloroethylamino)tetrahydro-2H-1,3,2-oxazaphosphorin-2-oxide
CAS No. 3778-73-2
项目整合开发状态: Launched-1976
项目研究机构: Baxter Oncology (Not Determined), Br...
参考文献标题:Verfahren zur Herstellung von neuen N-substituierten Amiden und Esteramiden der Phosphos鋟re und Thiophosphos鋟re
文献作者:Arnold,H.; et al.(Asta Medica AG)
参考来源:DE 1645921

ANG-615

德尼布林Chemical Name: N-[5-[4-(L-Alanylamino)phenylsulfanyl]-1H-benzimidazol-2-yl]carbamic acid methyl ester
CAS No. 284019-34-7
项目整合开发状态: Preclinical
项目研究机构: Angiogene Pharmaceuticals (Origina...
参考文献标题:Benzimidazole vascular damaging agents
文献作者:Davis,P.D.(Angiogene Pharmaceuticals Ltd.)
参考来源:EP 1140078; WO 0041669

Propafenone hydrochloride, Pronon, Rytmonorm, Rhythmol

心律平普罗帕酮 Chemical Name: 1-[2-[2-Hydroxy-3-(propylamino)propoxy]phenyl-3-phenyl-1-propanone hydrochloride
CAS No. 34183-22-7, 54063-53-5 (free base)
项目整合开发状态: Launched-1979
项目研究机构: Abbott (Or...
参考文献标题:Propafenone
文献作者:Castar,J.; B鋒ring-Kuhmley,S.R.
参考来源:Drugs Fut 1977,2(5),325

Endixaprine, SR-41378

思地普令Chemical Name: 6-(2,4-Dichlorophenyl)-3-(4-hydroxypiperidino)pyridazine; 1-[6-(2,4-Dichlorophenyl)-3-pyridazinyl]-4-piperidinol
CAS No. 93181-85-2
项目整合开发状态: Phase II
项目研究机构: Sanofi-Avent...
参考文献标题:SR-41378
文献作者:Dubois,M.
参考来源:Drugs Fut 1986,11(4),286

Englitazone sodium, CP-72467-2, CP-68722(racemate), CP-72467-02

恩格列酮2,4-硫唑里地二酮,5-[[3,4-二氢-2-(苯甲基)-2H-1-苯并吡喃-6-基]甲基]-,钠盐(1:1)Chemical Name: (-)-5-[2(R)-Benzyl-3,4-dihydro-2H-benzopyran-6-ylmethyl]thiazolidine-2,4-dione sodium salt
CAS No. 109229-58-5 (free acid...
参考文献标题:Substituted dihydrobenzopyran and dihydrobenzofuran thiazolidine-2,4-diones as hypoglycemic agents
文献作者:Clark,D.A.; Goldstein,S.W.; Volkmann,R.A.; Eggler,J.F.; Holland,G.F.; Hulin,B.; Stevenson,R.W.; Kreutter,D.K.; Gibbs,E.M.; Krupp,M.N.; et al.
参考来源:J Med Chem 1991,34(1),319

Enciprazine, Wy-48624(diHCl), D-13112

恩西拉嗪Chemical Name: (R,S)-1-[4-(2-Methoxyphenyl)piperazin-1-yl]-3-[3,4,5-trimethoxyphenoxy]propan-2-ol; (?-4-(o-Methoxyphenyl)-alpha-[(3,4,5-trimethoxyphenoxy)methyl]-1-piperazineethanol
CAS No. 68...
参考文献标题:Enciprazine
文献作者:Engel,J.; Jakovlev,V.; Kleemann,A.
参考来源:Drugs Fut 1981,6(5),278

Valrubicin, NSC-246131, AD-32, Valtaxin, Valstar

戊柔比星Chemical Name: N-Trifluoroacetyladriamycin-14-valerate; N-Trifluorodoxorubicin-14-valerate; (2S-cis)-2-[[4-(3-Trifluoroacetylamino-2,3,6-trideoxy-alpha-L-lyxo-hexapyranosyl)oxy]-1,2,3,4,6,11-hexa...
参考文献标题:N-trifluoroacetyladriamycin-14-alkanoates and therapeutic compositions containing same
文献作者:Israel,M.; Modest,E.J.(Sidney Farber Cancer Institute,Inc.)
参考来源:CA 1060003; US 4035566