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

E-5842

Chemical Name: 4-(4-Fluorophenyl)-1-[4-(1,2,4-triazol-1-yl)butyl]-1,2,3,6-tetrahydropyridine citrate
CAS No. 177945-46-9 (free base), 177945-45-8 (HCl)
项目整合开发状态: Phase II
项目研究机构: Esteve (Orig...
参考文献标题:Tetrahydropyridine-(or -4-hydroxypiperidine)alkyla
文献作者:Merce-Vidal,R.; Frigola-Constansa,J.(Laboratorios del Dr.Esteve,SA)
参考来源:EP 0721455; FR 2723091; JP 1997503230; US 5731331; WO 9604287

Ro-11-1464

Chemical Name: 9-Methyl-4-phenyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepine
CAS No. 54123-09-0
项目整合开发状态: Preclinical
项目研究机构: Roche (Originator)
合成路线:Treatment of diazepinone (I) ...
参考文献标题:Diazepine derivs.
文献作者:Hellerbach,J.; Zeller,P.; Binder,D.; Hromatka,O.(F.Hoffmann-La Roche AG)
参考来源:DE 2405682; GB 1456161; US 4155913

Phomoidride B, CP-263114

Chemical Name: (-)-2-[14-[4(E)-Hexenoyl]-18-[6(E)-octenyl]-3,7,9-trioxo-2,8,15-trioxapentacyclo[10.3.3.0(1,11).0(4,16).0(6,10)]octadeca-6(10),16-dien-4-yl]acetic acid; (-)-(5R*,7aR*,9R*,11S*,11aS*,12S...
参考文献标题:Total synthesis of the CP molecules CP-263,114 and CP-225,917 - Part 1: Synthesis of key intermediates and intelligence gathering
文献作者:Nicolaou,K.C.; et al.
参考来源:Angew Chem.Int Ed Engl 1999,38(11),1669

新产品编号:85937

Chemical Name: Glutaric acid 5,11-dimethyl-6H-pyrido[4,3-b]carbazol-9-yl monoester hydrochloride
CAS No. 160650-54-4, 160650-35-1 (monomethanesulfonate salt)
项目整合开发状态: Preclinical
项目研究机构: Tan...
参考文献标题:Ellipticine derivs.with antitumor activity
文献作者:Tsujihara,K.; Harada,N.; Ozaki,K.; Ohashi,M.; Oda,K.(Tanabe Seiyaku Co.,Ltd.)
参考来源:EP 0608876; JP 1994279441; US 5605904

CVT-313

Chemical Name: N2,N2-Bis(2-hydroxyethyl)-9-isopropyl-N6-(4-methoxybenzyl)purine-2,6-diamine; 2-[N,N-Bis(2-hydroxyethyl)amino]-9-isopropyl-6-(4-methoxybenzylamino)purine
CAS No. 199986-75-9
项目整合开...
参考文献标题:Purine inhibitors of cyclin dependent kinase 2 and IkappaB-alpha
文献作者:Lum,R.T.; Blum,C.L.; Mackman,R.; Wick,M.M.; Schow,S.R.(CV Therapeutics,Inc.)
参考来源:EP 1021186; US 5866702; WO 9805335

NNC-21-0136

Chemical Name: 2-Chloro-N6-[2-(2-benzothiazolylsulfanyl)-1(R)-methylethyl]adenosine
CAS No. 162684-35-7
项目整合开发状态: Preclinical
项目研究机构: Novo Nordisk (Originator)
合成路线:Protection of D-alanino...
参考文献标题:N-substituted adenosines as novel neuroprotective A1 agonists with diminished hypotensive effects
文献作者:Knutsen,L.J.; Lau,J.; Petersen,H.; Thomsen,C.; Weis,J.U.; Shalmi,M.; Judge,M.E.; Hansen,A.J.; Sheardown,M.J.
参考来源:J Med Chem 1999,42(18),3463

N-5228

Chemical Name: trans-(all E)-N,N'-Bis(3,4-dimethoxybenzyl)-N-(3,7,11,15,19,23,27,31,35-nonamethyl-2,6,10,14,18,22,26,30,34-hexatriacontanonaenyl)cyclohexane-1,2-diamine
CAS No. 194720-56-4, 194721-...
参考文献标题:Isoprene derivs.
文献作者:Inomata,K.; Takahashi,T.; Inoue,H.; Taniuchi,M.; Yamazaki,H.; Suzuki,M.; Takazawa,T.; Kawamura,K.; Oshida,N.; Ikemoto,H.; Kishie,T.(Nisshin Seifun Group Inc.)
参考来源:EP 0787716; JP 1997268162

新产品编号:231481

Chemical Name: 3-(Benzofuran-5-yl)-2'-hydroxy-6'-[4-O-(methoxycarbonyl)-beta-D-glucopyranosyloxy]propiophenone
CAS No. 190777-98-1
项目整合开发状态: Preclinical
项目研究机构: Tanabe Seiyaku (Originator) 参考文献标题:Na+-glucose cotransporter inhibitors as antidiabetics.I.Synthesis and pharmacological properties of 4'-dehydroxyphlorizin derivatives based on a new concept
文献作者:Tsujihara,K.; Hongu,M.; Saito,K.; Inamasu,M.; Arakawa,K.; Oku,A.; Matsumoto,M.
参考来源:Chem Pharm Bull 1996,44(6),1174

E-4010

Chemical Name: 4-(3-Chloro-4-methoxybenzylamino)-1-(4-hydroxypiperidin-1-yl)phthalazine-6-carbonitrile hydrochloride
CAS No. 178308-66-2, 178308-65-1 (free base)
项目整合开发状态: Preclinical
项目研究机构:...
参考文献标题:Fused pyridazine cpd.
文献作者:Watanabe,N.; Kabasawa,Y.; Takase,Y.; Ozaki,F.; Ishibashi,K.; Miyazaki,K.; Matsukura,M.; Souda,S.; Miyake,K.; Ishihara,H.; Kodama,K.; Adachi,H.(Eisai Co.,Ltd.)
参考来源:EP 0722936; JP 1996225541; US 6218392; WO 9605176

Terprenin

Chemical Name: 3',6'-Dimethoxy-4-(3-methyl-2-butenyloxy)-p-terphenyl-2',3,4''-triol
CAS No. 197899-11-9
项目整合开发状态: Preclinical
项目研究机构: Shionogi (Originator)
合成路线:1.The Suzuki coupling of ar...
参考文献标题:Total synthesis of terprenin,a novel immunosuppressive p-terphenyl derivative
文献作者:Yonezawa,S.; Komurasaki,T.; Kawada,K.; Tsuri,T.; Fuji,M.; Kugimiya,A.; Haga,N.; Mitsumori,S.; Inagaki,M.; Nakatani,T.; Tamura,Y.; Takechi,S.; Taishi,T.; Ohtani,M.
参考来源:J Org Chem 1998,63(17),5831