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

新产品编号:941799

Chemical Name: 1-(3-Fluorophenyl)-1-[6-[4-(methylsulfonyl)phenyl]-1,3-benzodioxol-5-yl]methanone
CAS No. 445039-17-8
项目整合开发状态: Preclinical
项目研究机构: NitroMed (Originator)
合成路线:Piperonal (I) ...
参考文献标题:Substd.aryl cpds.as novel cyclooxygenase-2 selective inhibitors,compsns.and methods of use
文献作者:Earl,R.A.; Garvey,D.S.; Khanapure,S.P.; Gaston,R.D.; Fang,X.; Ezawa,M.(NitroMed Inc.)
参考来源:US 2002119977; WO 0260378

JNJ-17297709

Chemical Name: (2R*,3aR*,12bS*)-N,N-Dimethyl-N-(3,3a,8,12b-tetrahydro-2H-dibenzo[3,4:6,7]cyclohepta[1,2-b]furan-2-ylmethyl)amine
CAS No. 198644-59-6 (no stereoch. at 2), 198644-93-8 (undefined isom...
参考文献标题:Substd.tetracyclic tetrahydrofuran derivs.
文献作者:Gil-Lopetegui,P.; Fern醤dez-Gadea,F.J.; Meert,T.F.(Janssen Pharmaceutica NV)
参考来源:EP 0892793; JP 2000508327; WO 9738991

新产品编号:895921

Chemical Name: (-)-4-Benzyl-1-[2-(4-hydroxyphenoxy)ethyl]piperidine-3(R),4(R)-diol
CAS No. 370086-22-9
项目整合开发状态: Preclinical
项目研究机构: Roche (Originator)
合成路线:Acylation of 4-benzyl-4-hydroxy...
参考文献标题:Neuroprotective substd.piperidine cpds.with activity as NMDA NR2B subtype selective antagonists
文献作者:Wyler,R.; Buettelmann,B.; Alanine,A.; Pinard,E.; Jaeschke,G.; Neidhart,M.-P.(Hoffmann-La Roche,Inc.)
参考来源:US 6432985; WO 0181309

新产品编号:780435

Chemical Name: (2R,6S,13aR,14aR,16aS)-2-[2-(2-Acetamidothiazol-4-yl)-7-methoxyquinolin-4-yloxy]-6-(tert-butoxycarboxamido)-5,16-dioxohexadecahydrocyclopropa[e]pyrrolo[1,2-a][1,4]diazacyclopentadecine-...
参考文献标题:Macrocyclic peptides active against the hepatitis C virus
文献作者:Halmos,T.; Llinas-Brunet,M.; Faucher,A.-M.; Ghiro,E.; Goudreau,N.; Tsantrizos,Y.S.; Cameron,D.R.(Boehringer Ingelheim (Canada) Ltd.)
参考来源:EP 1169339; JP 2002542160; WO 0059929

L-869298

Chemical Name: 2-[5-[1(S)-[3-(Cyclopropyloxy)-4-(difluoromethoxy)phenyl]-2-(1-oxidopyridin-3-yl)ethyl]thiazol-2-yl]-1,1,1,3,3,3-hexafluoropropan-2-ol
CAS No. 362718-74-9 ((-)-enantiomer), 362718-73...
参考文献标题:Tri-aryl-substd.-ethane PDE4 inhibitors
文献作者:Girard,M.; Frenette,R.; Hamel,P.; Guay,D.; Ducharme,Y.; Blouin,M.; Friesen,R.; Cote,B.; Martins,E.; Laliberte,S.(Merck Frosst Canada Inc.)
参考来源:EP 1272488; US 6399636; WO 0170738

BMS-248360

Chemical Name: 4'-(2-Butyl-4-oxo-1,3-diazaspiro[4.4]-1-nonen-3-ylmethyl)-N-(3,4-dimethylisoxazol-5-yl)-2'-(3,3-dimethyl-2-oxopyrrolidin-1-ylmethyl)biphenyl-2-sulfonamide
CAS No. 254737-87-6
项目整合...
参考文献标题:Biphenyl sulfonamides as dual angiotensin endothelin receptor antagonists
文献作者:Macor,J.E.; Murugesan,N.; Gu,Z.; Tellew,J.E.(Bristol-Myers Squibb Co.)
参考来源:EP 1094816; JP 2002519380; US 2002143024; WO 0001389

新产品编号:851625

Chemical Name: N-Phenylcarbamic acid 2-[3-(1H-benzimidazol-2-ylsulfanylmethyl)-2-methylphenylsulfanyl]ethyl ester
CAS No. 339353-49-0
项目整合开发状态: Preclinical
项目研究机构: AstraZeneca (Originator) 参考文献标题:Compounds
文献作者:Shue,Y.-K.; K黨ler,T.; Abedi,J.; Carcanague,D.; Wuonola,M.(Pharmacia AB)
参考来源:WO 0134573

新产品编号:932307

Chemical Name: 2-(4-Hydroxy-3-methoxy-5-methylphenyl)-2-(pyridin-3-ylamino)ethylphosphonic acid diethyl ester
CAS No. 420111-16-6
项目整合开发状态: Preclinical
项目研究机构: GlaxoSmithKline (Originator), I...
参考文献标题:beta-Substd.beta-aminoethyl phosphonates
文献作者:Ife,R.J.; Nguyen,L.M.; Bentzen,C.L.; Diep,V.V.; Azoulay,R.; Phan,H.T.; Niesor,E.J.(Ilex Oncology Research-Europe SA)
参考来源:US 2002111488; WO 0234756

新产品编号:894339

Chemical Name: 5-(4-Aminobutylamino)-4-chloro-N-[5-[N-[5-[N-[5-[N-[3-(dimethylamino)propyl]carbamoyl]-1-methyl-1H-pyrrol-3-yl]carbamoyl]-1-methyl-1H-pyrrol-3-yl]carbamoyl]-1-methyl-1H-pyrrol-3-yl]isot...
参考文献标题:Charged cpds.comprising a nucleic acid binding moiety and uses therefor
文献作者:Ge,Y.; Taylor,M.J.; Baird,E.E.; Moser,H.E.; Burli,R.W.(GeneSoft,Inc.)
参考来源:JP 2003529609; WO 0174898

MCB-116

Chemical Name: 7-[4-[4-[5(S)-(Acetamidomethyl)-2-oxooxazolidin-3-yl]-2-fluorophenyl]piperazin-1-yl]-1-cyclopropyl-6-fluoro-4-oxo-1,4-dihydroquinoline-3-carboxylic acid
CAS No. 444335-12-0
项目整合开发...
参考文献标题:Antimicrobial quinolone derivs.and use of the same to treat bacterial infections
文献作者:Barbachyn,M.R.; Patel,D.V.; Gage,J.R.; Gordeev,M.F.(Pharmacia Corp.)
参考来源:WO 0259116