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

Tiopinac

硫平酸Chemical Name: 2-(11-Oxo-6,11-dihydrodibenzo[b,e]thiepin-3-yl)acetic acid
CAS No. 61220-69-7
项目整合开发状态: Not Determined
项目研究机构:
合成路线:The esterification of 2-nitroterephthalic acid (I) w...
参考文献标题:6,11-Dihydrodibenzothiepin-11-ones,compositions and uses thereof
文献作者:Ackrell,J.(Syntex (USA),Inc.)
参考来源:US 4000308

Bleomycin A2 sulfate

硫酸博莱霉素N1-[3-(二甲基锍)丙基]-博来霉素酰胺氯化物Chemical Name: N2-[4(R)-[2(S)-[6-Amino-2-[1(S)-[2(S)-amino-2-carbamoylethyl]-2-carbamoylethyl]-5-methylpyrimidin-4-ylcarboxamido]-3(R)-[2-O-(3-O-carbamoyl-alpha-D-manno...
参考文献标题:Five-component synthesis of marimastat analogues
文献作者:Patel,S.; et al.
参考来源:Tetrahedron Lett 1998,39(45),8333

Cefoselis sulfate, FK-037, Wincef

硫酸头孢噻利头孢噻利 Chemical Name: 5-Amino-2-[(6R,7R)-7-[2-(2-amino-4-thiazolyl)-2(Z)-(methoxyimino)acetamido]-2-carboxy-8-oxo-5-thia-1-azabicyclo[4.2.0]-oct-2-en-3-ylmethyl]-1-(2-hydroxyethyl)-1H-pyrazoliu...
参考文献标题:New cephem cpd.and process for preparation thereof
文献作者:Sakane,K.; Kawabata,K.; Miyai,K.; Inamoto,Y.(Fujisawa Pharmaceutical Co.,Ltd.)
参考来源:AU 8822271; EP 0307804; JP 1989151589; US 4952578

Bortezomib, MLN-341, DPBA, LDP-341, NSC-681239, PS-341, Velcade

硼替佐米Chemical Name: 3-Methyl-1(R)-[N-(pyrazin-2-ylcarbonyl)-L-phenylalanylamino]butylboronic acid; N-(Pyrazin-2-ylcarbonyl)-L-phenylalanyl-L-boroleucine; N-[1(S)-[N-[1(R)-(Dihydroxyboryl)-3-methylbuty...
参考文献标题:Boronic ester and acid cpds.,synthesis and uses
文献作者:Adams,J.; Ma,Y.-T.; Stein,R.; Baevsky,M.; Grenier,L.; Plamondon,L.(ProScript,Inc.)
参考来源:JP 1998510245; US 5780454; US 6083903; WO 9613266

Iodixanol, DU-6807, 2-5410-3A, OptiPrep, Visipaque, Acupaque

碘克沙醇Chemical Name: 5,5'-[(2-Hydroxytrimethylene)bis(acetylimino)]bis[N,N/1-bis(2,3-dihydroxypropyl)-2,4,6-triiodoisophthalamide
CAS No. 92339-11-2
项目整合开发状态: Launched-1993
项目研究机构: Amersham He...
参考文献标题:X-ray contrast agents
文献作者:Wille,K.; Hansen,P.-E.; Holtermann,H.(Amersham plc)
参考来源:EP 0108638; US 5349085

Iofratol, B-19470

碘拉醇Chemical Name: N,N''-(2-Hydroxypropane-1,3-diyl)bis[N'-[2-hydroxy-1-(hydroxymethyl)ethyl]-5-[2(S)-hydroxypropionamido]-2,4,6-triiodo-1,3-benzenedicarboxamide]; N,N''-(2-Hydroxytrimethylene)bis[N'-...
参考文献标题:1,3-Bis[3-(mono- or poly-hydroxy)acylamino-5-(mono- or poly-hydroxyalkyl)aminocarbonyl-2,4,6-triiodo-benzoyl-amino]-hydroxy-or hydroxyalkyl-propanes,their methods of preparation and X-ray contrast media containing them
文献作者:Uggeri,F.; Brocchetta,M.(Bracco SpA)
参考来源:EP 0557345; JP 1994504268; WO 9208691

Fozivudine tidoxil, BM-21.1290

福齐夫定替酯Chemical Name: 3'-Azido-3'-deoxy-5'-O-[2-decyloxy-3-(dodecylthio)propoxy-hydroxyphosphoryl]thymidine
CAS No. 141790-23-0
项目整合开发状态: Phase II
项目研究机构: Roche (Originator)
合成路线:Treatment...
参考文献标题:New phospholipid derivs.of nucleosides,their preparation and their use as antiviral drugs
文献作者:Zilch,H.; Leinert,H.; Mertens,A.; Herrmann,D.(Roche Diagnostics GmbH)
参考来源:DE 4026265; EP 0545966; JP 1994500546; WO 9203462

Meldonium hydrate, Quaterin, Mildronate, MET-88, Q-4224-IOS, THP(anhydrous)

米屈肼(二水合物) 米屈肼 Chemical Name: 3-(2,2,2-Trimethylhydrazinium)propionate dihydrate; 2-(2-Carboxyethyl)-1,1,1-trimethylhydrazinium hydroxyde inner salt dihydrate
CAS No. 86426-17-7, 76144-81-5 (anhydr...
参考文献标题:3-(2,2,2-Trimethylhydrazinium)propionate,method of obtaining it and use
文献作者:Guiller,S.A.; Eremeev,A.V.; Kalvinsh,I.Y.; Semenikhina,V.G.; Liepinsh,E.A.; Latvietis,Y.Y.; Anderson,P.P.; Astapenok,E.B.; Spruzh,Y.Y.; Trapetsiers,P.T.; Podoprigora,G.I.(Latvian Institute of Organic Synthesis)
参考来源:WO 8001068

Mivacurium chloride, BW-B1090U, Mivacron

米库氯铵Chemical Name: (E)-(1R,1'R)-2,2'-[4-Octenedioylbis(oxytrimethylene)]bis[6,7-dimethoxy-2-methyl-1-(3,4,5-trimethoxybenzyl)-1,2,3,4-tetrahydroisoquinolinium] dichloride; [R-[R*,R*-(E)]]-2,2'-[(1,8-...
参考文献标题:Bis-dimethoxymethyl(trimethoxybenzyl)isoquinolinium salts,their preparation and pharmaceutical compsns.containing them
文献作者:Swaringen,R.A.Jr.; El-Sayad,H.A.; Yeowell,D.A.; Savarese,J.J.(General Hospital Corporation; GlaxoSmithKline plc)
参考来源:EP 0181055; ES 8609260; JP 1986087666; JP 1986087666; US 4761419

Milacemide, CP-1552-S, Glyzan, Glyzac

米拉醋胺 N2-戊基甘氨酸酰胺盐酸盐 (1:1) Chemical Name: 2-(Pentylamino)acetamide
CAS No. 76990-56-2, 76990-85-7 (monoHCl), 79922-20-6 (phosphate(1:1)), 79912-65-5 (sulfate(1:1))
项目整合开发状态: Phase III
项目研究机构: ...
参考文献标题:Milacemide
文献作者:Serradell,M.N.; Castar,J.
参考来源:Drugs Fut 1984,9(8),587