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

Tariquidar, XR-9576

2-醛基-4-甲氧基苯硼酸Chemical Name: N-[2-[N-[4-[2-(6,7-Dimethoxy-1,2,3,4-tetrahydroisoquinolin-2-yl)ethyl]phenyl]carbamoyl]-4,5-dimethoxyphenyl]quinoline-3-carboxamide
CAS No. 206873-63-4
项目整合开发状态: Phas...
参考文献标题:Anthranilic acid derivs.as multi drug resistance modulators
文献作者:Ryder,H.; Ashworth,P.A.; Roe,M.J.; Brumwell,J.E.; Hunjan,S.; Folkes,A.J.; Sanderson,J.T.; Williams,S.; Maximen,L.M.(Xenova Group plc)
参考来源:EP 0934276; GB 2334521; JP 2001502683; US 6218393; WO 9817648

Osemozotan hydrochloride, MN-305, MCI-242, MKC-242

3-(1,3-苯并二氧乙醇-5-酰氧基)-n-[(2s)-2,3-二氢-1,4-苯并二恶英-2-甲基]-1-丙氨酰胺盐酸盐(1:1)Chemical Name: 2(S)-[3-(1,3-Benzodioxol-5-yloxy)propylaminomethyl]-1,4-benzodioxane hydrochloride
CAS No. 137275-80-0, 137275-81-1 ...
参考文献标题:Optically active alkylene-dioxybenzene derivs.and their use in therapy
文献作者:Iwata,H.; Baba,A.; Matsuda,T.; Egawa,M.; Tobe,A.; Saito,K.(Mitsubishi Chemical Corp.)
参考来源:EP 0446921; JP 1991264528; US 5168099; US 5234948

GW-4064, GW-4064X

3-(2,6-二氯苯基)-4-(3'-羧基-2-氯二苯乙烯-4-基)氧甲基-5-异丙基异恶唑Chemical Name: 3-[2-[2-Chloro-4-[3-(2,6-dichlorophenyl)-5-isopropylisoxazol-4-ylmethoxy]phenyl]vinyl]benzoic acid
CAS No. 278779-30-9
项目整合开发状态: Prec...
参考文献标题:Assays for ligands for nuclear receptors
文献作者:Lehmann,J.; Stimmel,J.B.; Blanchard,S.G.; Kliewer,S.A.; Willson,T.M.; Parks,D.J.(Glaxo Group Ltd.)
参考来源:WO 0037077

GYKI-12743

3(2H)-吡啶嗪,2-[3-[[(2,3-二氢-1,4-苯并二恶英-2-基)甲基]丙基]-,盐酸盐(1:1)Chemical Name: (?-2-[3-[N-(2-Benzo[1,4]dioxanyl)methylamino]propyl]-3(2H)-pyridazinone hydrochloride
CAS No. 110714-10-8
项目整合开发状态: Phase I<...
参考文献标题:3(2H)-Pyridazinone derivs.,a process and intermediates for preparing them and medicaments containing them and/or other 3(2H)-pyridazinone derivatives
文献作者:Kasztreiner,E.; Rabloczky,G.; Makk,N.; Jaszlits,L.; Matyus,P.; Cseh,G.; Pribusz,geb.Rapp,I.; Czak? K.; Diesler,E.; Elekes,I.; Kaufer,L.; Kuh醨,geb.K黵thy,M.; Kincsessy,J.; Kos醨y,J.; Nagy,Gy鰊gyi geb.C.(Richter Gedeon Vegyeszeti)
参考来源:AU 8664496; EP 0220735; JP 87161768

ST-1959, DL-111-IT

3-(2-乙基苯基)-5-(3-甲氧基苯基)-1H-1,2,4-三唑Chemical Name: 3-(2-Ethylphenyl)-5-(3-methoxyphenyl)-1H-1,2,4-triazole; 5-(2-Ethylphenyl)-3-(3-methoxyphenyl)-1H-1,2,4-triazole
CAS No. 69095-83-6
项目整合开发状态: Pha...
参考文献标题:3,5-Disubstd.-1H-1,2,4-triazoles
文献作者:Omodei Sale,A.; Consonni,P.; Galliani,G.; Lerner,L.(Lepetit SpA)
参考来源:DE 2819372

Pyraoncozine, NSC-D-364834, C-8412843, NSC-364834-D

3-(2-氯乙基)-3,4-二氢-4-氧代吡唑并[5,1-d]-1,2,3,5-四嗪-8-甲酰胺Chemical Name: 3-(2-Chloroethyl)-3,4-dihydro-4-oxopyrazolo[5,1-d]-1,2,3,5-tetrazine-8-carboxamide
CAS No. 90521-23-6
项目整合开发状态: Preclinical
项目研究...
参考文献标题:3-(Haloethyl)-4-oxopyrazolo[5,1-d]-1,2,3,5-tetrazine-8-carboxamide compounds
文献作者:Cheng,C.C.(Pfizer Inc.)
参考来源:JP 60011489; US 4504475

GW-5074

3-(3,5-二溴-4-羟基苯亚甲基)-5-碘-1,3-二氢吲哚-2-酮Chemical Name: 3-(3,5-Dibromo-4-hydroxybenzylidene)-5-iodo-2,3-dihydro-1H-indol-2-one
CAS No. 220904-83-6
项目整合开发状态: Biological Testing
项目研究机构: GlaxoSmithKl...
参考文献标题:Benzylidene-1,3-dihydro-indol-2-one derivs.as receptor tyrosine kinase inhibitors,particularly of Raf kinases
文献作者:McNutt,R.W.Jr.; Hunter,R.N.III; Jung,D.K.; Lackey,K.E.; Dickerson,S.; Harris,P.A.; Veal,J.M.; Peel,M.R.(Glaxo Group Ltd.)
参考来源:EP 1003721; WO 9910325

48740-RP, RP-48740

3-(3-吡啶基)-1H,3H-吡咯并[1,2-c]噻唑-7-甲酰胺Chemical Name: 3-(3-Pyridyl)-1H,3H-pyrrolo[1,2-c]thiazole-7-carboxamide
CAS No. 93363-11-2
项目整合开发状态: Phase II
项目研究机构: Aventis Pharma (Originator)
合成路线:The...
参考文献标题:Novel 1H,3H-pyrrolo[1,2-c]thiazole derivs.,their preparation and medicaments containing them
文献作者:Fabre,J.-L.; Farge,D.; James,C.; Lav? D.(Aventis SA)
参考来源:EP 0115979; US 4529728

SR-31747A, SR-31747, CM-31747

3-(3-氯-4-环己基苯基)-N-环己基-N-乙基-2(Z)-丙烯基胺Chemical Name: 3-(3-Chloro-4-cyclohexylphenyl)-N-cyclohexyl-N-ethyl-2(Z)-propenylamine hydrochloride
CAS No. 132173-07-0
项目整合开发状态: Phase II
项目研究机构: Sanofi-...
参考文献标题:Benzene derivates,their preparation and pharmaceutical compsns.containing them
文献作者:Breli鑢e,J.-C.; Casellas,P.; Lavastre,S.; Paul,R.(Sanofi-Synthabo)
参考来源:EP 0376850; FR 2641276; JP 1991002116; US 5354781

Estrone 3-oleate, Oleoyl-estrone

3-(4-苄氧基苯基)-DL-β-丙氨酸醇Chemical Name: 3-Oleoylestra-1,3,5(10)trien-17-one; 3-[1-Oxo-9(Z)-octadecenyloxy]estra-1,3,5(10)-trien-17-one
CAS No. 180003-17-2
项目整合开发状态: Preclinical
项目研究机构: Oleoyl-Est...
参考文献标题:Fatty-acid monoesters of estrogens for the treatment of obesity and/or overweight
文献作者:Alemany,M.(Laboratorios Salvat SA)
参考来源:EP 0771817; US 5798348