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

Dronedarone hydrochloride, SR-33589B

决奈达隆Chemical Name: 2-Butyl-3-[4-[3-(dibutylamino)propoxy]benzoyl]-5-(methylsulfonamido)benzofuran hydrochloride
CAS No. 141626-36-0 (free base)
项目整合开发状态: Phase III
项目研究机构: Sanofi-Aventis (Ori...
参考文献标题:Benzofuran derivs.,benzothiophenes,indoles or indolizines,process for production and compsns.containing them
文献作者:Gubin,J.; Lucchetti,J.; Inion,H.; Chatelain,P.; Rosseels,G.; Kilenyi,S.(Sanofi-Synthabo)
参考来源:EP 0471609; FR 2665444; JP 1992316554; US 5223510

Vandetanib, AZD-6474, ZD-6474

凡德他尼Chemical Name: N-(4-Bromo-2-fluorophenyl)-6-methoxy-7-(1-methylpiperidin-4-ylmethoxy)quinazolin-4-amine
CAS No. 338992-00-0, 338992-48-6 (HCl), 338992-53-3 (monotrifluoroacetate)
项目整合开发状态: P...
参考文献标题:Quinazoline derivs.as VEGF inhibitors
文献作者:Hennequin,L.F.A.; Stokes,E.S.E.; Thomas,A.P.(AstraZeneca AB; AstraZeneca plc)
参考来源:WO 0132651

Ricasetron, BRL-46470

利卡司琼Chemical Name: endo-3,3-Dimethyl-N-(8-methyl-8-azabicyclo[3.2.1]oct-3-yl)-2,3-dihydroindole-1-carboxamide
CAS No. 117086-68-7
项目整合开发状态: Phase II
项目研究机构: GlaxoSmithKline (Originator)
合成...
参考文献标题:New camptothecin derivs.and process for preparing same
文献作者:Miyasaka,T.; Mutai,M.; Nokata,K.; Sawada,S.; Sugino,E.(Yakult Honsha Co.,Ltd.)
参考来源:EP 0137145; JP 1985019790

Ritanserin, R-55667, Tiserton

利坦丝林Chemical Name: 6-[2-[4-[Bis(p-fluorophenyl)methylene]piperidino]ethyl]-7-methyl-5H-thiazolo[3,2-a]pyrimidin-5-one
CAS No. 87051-43-2
项目整合开发状态: Phase III
项目研究机构: Janssen (Originator)
合成...
参考文献标题:Novel ((bis(aryl)methylene)-1-piperidinyl)alkyl-pyrimidinones
文献作者:Kennis,L.E.J.; Mertens,J.C.; Vandenberk,J.(Janssen Pharmaceutica NV)
参考来源:EP 0110435; ES 8601965; US 4485107

Risperidone, R-64766, Risperdal M-Tab, Risperdal Consta, Rispolept, Belivon, Risperdal

利培酮Chemical Name: 3-[2-[4-(6-Fluoro-1,2-benzisoxazol-3-yl)piperidin-1-yl]ethyl]-2-methyl-6,7,8,9-tetrahydro-4H-pyrido[1,2-a]pyrimidin-4-one
CAS No. 106266-06-2
项目整合开发状态: Launched-1993
项目研究机构:...
参考文献标题:Novel 1,2-benzisoxazol-3-yl and 1,2-benzisothiazo
文献作者:Kennis,L.E.J.; Vandenberk,J.(Janssen Pharmaceutica NV)
参考来源:EP 0196132; ES 8705881; JP 1986221186; US 4804663

Lidorestat, EML-676, IDD-000676-01, IDD-676

利多司他Chemical Name: 3-(4,5,7-Trifluorobenzothiazol-2-ylmethyl)-1H-indole-1-acetic acid
CAS No. 245116-90-9
项目整合开发状态: Discontinued
项目研究机构: Institute for Diabetes Discovery (Originator), Merck K...
参考文献标题:Methods of reducing serum glucose and triglyceride levels and for inhibiting angiogenesis using substd.indolealkanoic acids
文献作者:Jacot,J.; Sredy,J.(The Institutes for Pharmaceutical Discovery,Inc.)
参考来源:WO 0032180

Ridogrel, R-68070, Ibidel

利多格雷Chemical Name: (E)-5-[(3-Pyridinyl)[3-(trifluoromethyl)phenyl]methylenaminooxy]pentanoic acid; (E)-5-[[[alpha-3-Pyridyl-m-(trifluoromethyl)benzylidene]amino]oxy]valeric acid
CAS No. 110140-89-1...
参考文献标题:Pharmaceutical use of [[[(3-pyridinyl)methylen]amino]oxy]alkanoic acid and esters
文献作者:Freyne,E.J.E.; Raeymaekers,A.H.; Sipido,V.; Venet,M.G.(Janssen Pharmaceutica NV)
参考来源:EP 0221601; JP 1987161759; JP 1991068556; US 4746671

Linetastine, Linazolast, YM-257, TMK-688

利奈他斯汀Chemical Name: N-[2-[4-(Diphenylmethoxy)piperidin-1-yl]ethyl]-5-[4-(ethoxycarbonyloxy)-3-methoxyphenyl]-2(E),4(E)-pentadienamide
CAS No. 159776-68-8, 110501-66-1 (undefined isomer)
项目整合开发状态...
参考文献标题:TMK-688
文献作者:Tasaka,K.
参考来源:Drugs Fut 1988,13(12),1056

Linezolid, PNU-100766, U-100766, Zyvoxid, Zyvoxam, Zyvoxa, Zyvox

利奈唑胺Chemical Name: N-[3-[3-Fluoro-4-(4-morpholinyl)phenyl]-2-oxooxazolidin-5(S)-ylmethyl]acetamide
CAS No. 165800-03-3
项目整合开发状态: Launched-2000
项目研究机构: Pfizer (Originator)
合成路线:The condensa...
参考文献标题:Substd.oxazine and thiazine oxazolidinone antimicrobials
文献作者:Barbachyn,M.R.; Brickner,S.J.; Hutchinson,D.K.(Pharmacia Corp.)
参考来源:EP 0717738; JP 1997502436; WO 9507271

Rioprostil, TR-4698, ORF-15927

利奥前列素Chemical Name: (11alpha,13E)-1,11,16-Trihydroxy-16-methylprost-13-en-9-one; (2R,3R,4R)-4-Hydroxy-2-(7-hydroxyheptyl)-3-[(E)-(4RS)-(4-hydroxy-4-methyl-1-octenyl)]cyclopentanone
CAS No. 77287-05...
参考文献标题:Preparation of 15-deoxy-16-hydroxyprostaglandins
文献作者:Woessner,W.D.; Biddlecom,W.G.; Kluender,H.C.(Bayer Corp.)
参考来源:US 4132738