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

Gallopamil hydrochloride, D-600, Algocor, Procorum

戈洛帕米Chemical Name: 5-[N-[2-(3,4-Dimethoxyphenyl)ethyl]-N-methylamino]-2-isopropyl-2-(3,4,5-trimethoxyphenyl)pentanenitrile hydrochloride
CAS No. 16662-47-8 (free base)
项目整合开发状态: Launched-1983 参考文献标题:Verfahren zur herstellung basisch substituerter phenylacetonitrile
文献作者:Dengel,F.(Knoll AG)
参考来源:DE 1154810; DE 1158083

Besigomsin, Gomisin A, Schisandrol B, TJN-101

戈米辛AChemical Name: (6S-trans)-5,6,7,8-Tetrahydro-1,2,3,13-tetramethoxy-6,7-dimethylbenzo[3,4]cycloocta[1,2-f][1,3]benzodiox-6-ol; (+)-(6S,7S-R-biar)-5,6,7,8-Tetrahydro-1,2,3,12-tetramethoxy-6,7-dimeth...
参考文献标题:Synthesis and optically pure gomisin A and schizandrin: The first total synthesis of gomisin A and schizandrin having naturally occurring configurations
文献作者:Mitsuhashi,H.; Wakamatsu,T.; Mukaiyama,C.; Tanaka,M.
参考来源:Tetrahedron Lett 1992,33(29),4165

Pentamorphone, A-4492, RX-77989

戊吗酮Chemical Name: 7,8-Didehydro-4,5alpha-epoxy-3-hydroxy-17-methyl-14-(pentylamino)morphinan-6-one; 14beta-(Pentylamino)morphinone
CAS No. 68616-83-1
项目整合开发状态: Phase III
项目研究机构: BOC (Originat...
参考文献标题:Morphine derivs.,process for their preparation and medicines containing them
文献作者:Kobylecki,R.J.; Guest,I.G.; Lewis,J.W.; Kirby,G.W.(Reckitt & Colman Pharmaceuticals)
参考来源:DE 2812581

Pentrinitrol, W-2197

戊硝醇Chemical Name: 2,2-Bis[(nitrooxy)methyl]propane-1,3-diol nitrate
CAS No. 1607-17-6
项目整合开发状态: Not Determined
项目研究机构:
合成路线:It can be prepared in two different ways:1) By careful nitratio...
参考文献标题:A new synthesis of pentaerythritol trinate
文献作者:Camp,A.T.; et al.
参考来源:J Am Chem Soc 1955,77751-752

Ciprostene calcium, U-61431F(anhydrous)

戊酸,5-[(3aS,5R,6R,6aR)-六氢-5-羟基-6-[(1E,3S)-3-羟基-1-辛基]-3a-甲基-2(1H)-戊二烯基]-钙盐(2:1),(5Z)-(9CI) 西前列烯 Chemical Name: 9beta-Methylcarbacyclin calcium salt hydrate; (5Z)-9beta-Methyl-6a-carbaprostaglandin I2 ca...
参考文献标题:Composition and process
文献作者:Aristoff,P.A.(Pharmacia Corp.)
参考来源:US 4420632

Zaltoprofen, ZC-102, CN-100, Peon, Soleton

扎托布洛芬扎托洛芬 Chemical Name: (?-2-(10-Oxo-10,11-dihydrodibenzo[b,f]thiepin-2-yl)propionic acid; (?-alpha-Methyl-10-oxo-10,11-dihydrodibenzo[b,f]thiepin-2-acetic acid
CAS No. 89482-00-8, 74711-43-6 (un...
参考文献标题:Dibenzothiepine derivs.,process for their prepara
文献作者:Fujimoto,Y.; Yamabe,S.(Nippon Chemiphar Co.,Ltd.)
参考来源:DE 2941869; US 4247706

Zaprinast, M&B-22948

扎普司特Chemical Name: 2-o-Propoxyphenyl-8-azapurin-6-one; 1,4-Dihydro-5-(2-propoxyphenyl)-1,2,3-triazolo[4,5-d]pyrimidin-7-one
CAS No. 37762-06-4
项目整合开发状态: Preclinical
项目研究机构: May & Baker (Origi...
参考文献标题:Pharmaceutical compositions comprising azapurinones useful in treating allergic respiratory disorders
文献作者:Broughton,B.J.; et al.(May & Baker,Ltd.)
参考来源:DE 2162096; FR 2118078; GB 1338235; US 3987160

Xamoterol fumarate, TI-31, ICI-118587, Sepan, Corwin

扎莫特罗Chemical Name: (?-1-(p-Hydroxyphenoxy)-3-[2-(morpholinocarbonamido)ethylamino]-2-propanol hemifumarate; (?-N-[2-[[2-Hydroxy-3-(4-hydroxyphenoxy)propyl]amino]ethyl]-4-morpholinecarboxamide (E)-2-bu...
参考文献标题:Morpholine carboxamides and use thereof
文献作者:Main,B.G.; Barlow,J.J.(AstraZeneca plc)
参考来源:FR 2391997; JP 53147038; US 4143140; US 4172150

Zaldaride maleate, KW-5617, Zy-17617B, CGS-9343B

扎达来特马来酸盐 1,3-二氢-1-[1-[(4-甲基-4H,6H-吡咯并[1,2-a][4,1]苯并氮杂-4-基)甲基]-4-哌啶]-2H-苯并咪唑-2-酮 Chemical Name: 1-[1-(4-Methyl-4H,6H-pyrrolo[1,2-a][4,1]benzoxazepin-4-ylmethyl)piperidin-4-yl]-2,3-dihydro-1H-benzimidaz...
参考文献标题:Pyrrolo[1,2-a][4,1]benzoxazepins,process for their preparation,pharmaceutical compsns.containing them as well as therapeutic use
文献作者:Wasley,J.W.F.; Norman,J.(Novartis AG)
参考来源:EP 0233483; JP 1987169791; JP 1995089966; US 4758559

Zanapezil fumarate, TAK-147

扎那哌齐Chemical Name: 8-[3-(1-Benzylpiperidin-4-yl)propanoyl]-2,3,4,5-tetrahydro-1H-1-benzazepine fumarate; 3-(1-Benzylpiperidin-4-yl)-1-(2,3,4,5-tetrahydro-1H-1-benzazepin-8-yl)-1-propanone fumarate
...
参考文献标题:Condensed heterocyclic cpds.,their production and use
文献作者:Goto,G.; Ishihara,Y.; Miyamoto,M.(Takeda Chemical Industries,Ltd.)
参考来源:EP 0487071; US 5273974