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

Cimoxatone, MD-780515

西莫沙酮Chemical Name: 3-[4-[(3-Cyanophenyl)methoxy]phenyl]-5-(methoxymethyl)-2-oxazolidinone; 3-[[4-[5-(Methoxymethyl)-2-oxo-3-oxazolidinyl]phenoxy]methyl]benzonitrile
CAS No. 73815-11-9
项目整合开发状态:...
参考文献标题:Cimoxatone
文献作者:Ancher,J.F.
参考来源:Drugs Fut 1984,9(6),412

Squalamine, MSI-1256F(lactate)

角鲨胺Chemical Name: 3beta-[3-(4-Aminobutylamino)propylamino]-7alpha-hydroxy-24(R)-(sulfooxy)-5alpha-cholestane
CAS No. 148717-90-2, 320725-47-1 (lactate)
项目整合开发状态: Phase II
项目研究机构: Genaera (Or...
参考文献标题:Chemical synthesis of squalamine
文献作者:Moriarty,R.M.; Guo,L.; Tuladhar,S.M.(Genaera Corp.)
参考来源:WO 9419366

Nosantine, NPT-15392

诺次黄嘌呤Chemical Name: erythro-9-(2-Hydroxy-3-nonyl)hypoxanthine; erythro-9-(2-Hydroxy-3-nonyl)-1,9-dihydro-6H-purin-6-one; (R*,S*)-1,9-Dihydro-9-[1-(1-hydroxyethyl)heptyl]-6H-purin-6-one
CAS No. 766...
参考文献标题:9-(Hydroxy alkyl)purines
文献作者:Giner-Sorolla,A.(Newport Pharmaceuticals International Inc.; Sloan-Kettering Institute)
参考来源:US 4221910

Norzimelidine, Botiacrine, CPP-199, A-24356

诺美立定Chemical Name: N-[3-(4-Bromophenyl)-3-(3-pyridinyl)-2(Z)-propenyl]-N-methylamine
CAS No. 60324-59-6
项目整合开发状态: Biological Testing
项目研究机构:
合成路线:The condensation of 4-bromophenyl-3-pyri...
参考文献标题:Nomelidine
文献作者:Blancafort,P.; Serradell,M.N.; Castar,J.; Sweetman,A.J.
参考来源:Drugs Fut 1979,4(12),885

F-13640

贝非拉醇Chemical Name: 1-(3-Chloro-4-fluorophenyl)-1-[4-fluoro-4-(5-methylpyridin-2-ylmethylaminomethyl)piperidin-1-yl]methanone fumarate
CAS No. 208110-64-9 (free base)
项目整合开发状态: Phase I
项目研究机构...
参考文献标题:Pyridin-2-yl-methylamine derivs.,method of preparing and application as medicine
文献作者:Vacher,B.; Bonnaud,B.; Koek,W.(Pierre Fabre M閐icament)
参考来源:EP 0946546; JP 2001504129; US 6020345; WO 9822459

PA-457, YK-FH312

贝韦立马Chemical Name: [1S-(1alpha,3abeta,5aalpha,5bbeta,7aalpha,9beta,11abeta,11balpha,13abeta,13balpha)]-1-Isopropenyl-9-(3,3-dimethylsuccinyloxy)-5a,5b,8,8,11a-pentamethylperhydrocyclopenta[a]chrysene...
参考文献标题:Betulinic acid derivs.and uses thereof
文献作者:Lee,K.-H.; Kashiwada,Y.; Hashimoto,F.; Cosentino,L.M.; Manak,M.(Biotech Research Laboratories; University of North Carolina)
参考来源:US 5679828; WO 9639033

Dalbavancin, V-Glycopeptide, VER-001, BI-397 factor B0, BI-397

达巴万星Chemical Name: 5,31-Dichloro-38-de(methoxycarbonyl)-7-demethyl-19-deoxy-56-O-[2-deoxy-2-(10-methylundecanamido)-beta-D-glucopyranuronosyl]-38-[N-[3-(dimethylamino)propyl]carbamoyl]-42-O-alpha-D-m...
参考文献标题:New semisynthetic glycopepetides MDL 63,246 and MDL 63,042,and other amide derivatives of antibiotic A-40,926 active against glycopeptide-resistant VanA enterococci
文献作者:Malabarba,A.; Ciabatti,R.; Scotti,R.; Goldstein,B.P.; Ferrari,P.; Kurz,M.; Andreini,B.P.; Denaro,M.
参考来源:J Antibiot 1995,48(8),869

Dapoxetine, LY-210448

达泊西汀盐酸达泊西汀 Chemical Name: (S)-(+)-N,N-Dimethyl-3-(1-naphthyloxy)-1-phenylpropylamine; (+)-(S)-N,N-Dimethyl-alpha[2-(1-naphthyloxy)ethyl]benzylamine
CAS No. 119356-77-3, 129938-20-1 (HCl)
项目整合开...
参考文献标题:1-Phenyl-3-naphthalenyloxypropanamines
文献作者:Robertson,D.W.; Thompson,D.C.; Wong,D.T.(Eli Lilly and Company)
参考来源:AU 8814335; EP 0288188; JP 1988258837; US 5135947

Zolpidem tartrate, SL-80-0750-23N, Ambien CR, Myslee, Stilnoct, Ivadal, Ambien, Bikalm, Niotal, Stilnox

酒石酸唑吡坦唑吡坦 Chemical Name: N,N,6-Trimethyl-2-(4-methylphenyl)imidazo[1,2-a]pyridine-3-acetamide L-(+)-tartrate (2:1)
CAS No. 99294-93-6, 82626-48-0 (free base)
项目整合开发状态: Launched-1988
项目研究机构:...
参考文献标题:Method for the production of zolpidem
文献作者:Wohlleben,W.; Sauter,M.(Boehringer Ingelheim Pharma KG)
参考来源:DE 10121638; WO 0290356

Lasofoxifene tartrate, CP-336156

酒石酸拉索昔芬拉索昔芬 β-D-阿拉伯-六吡喃糖,4-氨基-2,4,6-三脱氧-(9CI)Chemical Name: (-)-(5R,6S)-6-Phenyl-5-[4-[2-(1-pyrrolidinyl)ethoxy]phenyl]-5,6,7,8-tetrahydronaphthalen-2-ol (-)-D-tartrate salt
CAS No. 190791-29-8,...
参考文献标题:Estrogen agonists/antagonists.
文献作者:Cameron,K.O.; Jardine,P.A.(Pfizer Inc.)
参考来源:EP 0802910; JP 1998503215; US 5552412; WO 9621656