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

SDZ-62-834zi, NSC-614383, CRC-8605, SRI-62-834

(四氢-2-(十八烷氧基)甲基呋喃-2-基)甲氧基磷酰胆碱Chemical Name: (?-2-[Hydroxy[2-(octadecyloxymethyl)tetrahydrofuran-2-ylmethoxy]phosphinyloxy]-N,N,N-trimethylethylamminium hydroxyde,inner salt P-oxide
CAS No. 113201-3...
参考文献标题:Substd.hydroxy-heterocyclyl-alkoxy-phosphinyloxy-trialkylaminium-hydroxide inner salt oxides,processes for their preparation and their use as pharmaceuticals
文献作者:Houlihan,W.J.; Lee,M.L.(Novartis AG; Novartis Deutschland GmbH)
参考来源:AU 8662038; EP 0213082; JP 1987051692

Baogongteng A

[(1R,4S,5R,7S)-4-羟基-8-氮杂双环[3.2.1]辛烷-7-基]乙酸酯Chemical Name: (-)-6beta-Acetoxy-2beta-hydroxynortropane benzoate; (1R,2S,5R,6S)-6-(Acetyloxy)-2-hydroxy-8-azoniabicyclo[3.2.1]octane benzoate
CAS No. 742...
参考文献标题:Total synthesis of Bao Gong Teng-A,a natural antiglaucoma compound
文献作者:Zeng,L.M.; Jung,M.E.; Peng,T.S.; Zeng,H.Y.; Le,Y.; Su,J.Y.
参考来源:J Org Chem 1992,57(13),3528

Talabostat, ValboroPro, PT-100

[(2R)-1-[(2S)-2-氨基-3-甲基丁酰基]吡咯烷-2-基]硼酸Talabostat 甲磺酸盐Chemical Name: L-Valyl-L-boroproline; [1-[2(S)-Amino-3-methylbutyryl]pyrrolidin-2(R)-yl]boronic acid
CAS No. 149682-77-9, 153737-95-2 (monohydroc...
参考文献标题:Cyclic boroproline cpds.
文献作者:Wallner,B.P.(Point Therapeutics,Inc.)
参考来源:JP 2002517401; WO 9962914

TEI-6170(free acid), TT-62

[(2R,3S,5S)-5-(5-氟-2,4-二氧基嘧啶-1-基)-3-羟基氧基-2-基]甲基四甲基四甲基氢磷酸盐Chemical Name: 5-Fluoro-2'-deoxyuridine 5'-myristylphosphate sodium salt; 5-Fluoro-2'-deoxyuridine 5'-tetradecylphosphate sodium salt; 2'-Deoxy...
参考文献标题:5-Fluoro-2'-deoxyuridine derivs.and a process for the preparation thereof
文献作者:Watanabe,K.; Saito,M.; Kato,Y.; Oba,T.; Fukushima,H.; Hara,T.(Teijin Ltd.)
参考来源:EP 0081386

OSW-1

[(2S,3R,4S,5R)-2-[(2S,3R,4S,5S)-3-乙酰氧基-2-[[(3R,8S,9R,10R,13S,14R,16R,17S)-3,17-二羟基-10,13-二甲基-17-[(2S)-6-甲基-3-氧代庚烷-2-基]-1,2,3,4,7,8,9,11,12,14,15,16-十二氢环戊烯并[a]菲-16-基]氧基]-5-羟基四氢吡喃-4-基]氧基-4,5-二羟基四氢吡喃-3-基...
参考文献标题:A new strategy for the stereoselective introduction of steroid side chain via alpha-alkoxy vinyl cuprates: Total synthesis of a highly potent antitumor natural product OSW-1
文献作者:Yu,W.; Jin,Z.
参考来源:J Am Chem Soc 2001,123(14),3369

Ladirubicin, PNU-159548, FCE-28729

[(2S,3S,4S,6R)-6-[[(1S,3S)-3-乙酰基-3,5,12-三羟基-6,11-二氧代-2,4-二氢-1H-并四苯-1-基]氧基]-4-(氮丙啶-1-基)-2-甲基四氢吡喃-3-基]甲烷磺酸酯Chemical Name: 3'-(1-Aziridinyl)-3'-deamino-4-demethoxy-4'-O-(methanesulfonyl)daunomycin
CAS...
参考文献标题:3'-Aziridino-anthracycline derivs.
文献作者:Bargiotti,A.; Caruso,M.; Grandi,M.; Ripamonti,M.; Suarato,A.(Pharmacia AB)
参考来源:EP 0683788; JP 1996506835; US 5532218; WO 9516695

Rapacuronium bromide, Org-9487, Raplon

[(2S,3S,5S,10S,13S,16S,17R)-3-乙酰氧基-10,13-二甲基-2-哌啶-1-基-16-(1-丙-2-烯基哌啶-1-鎓-1-基)-2,3,4,5,6,7,8,9,11,12,14,15,16,17-十四氢-1H-环戊二烯并[a]菲-17-基]丙酸酯溴化物Chemical Name: 1-[3alpha-Acetoxy-2beta-(1-piperidinyl)-17bet...
参考文献标题:Monoquaternary 2,16-bispiperidinylandrostane derivs
文献作者:Sleigh,T.; Carlyle,I.C.; Muir,A.W.(Akzo Nobel N.V.)
参考来源:EP 0571012; JP 1995267984; US 5418226

CRA-2059, APC-2059

[(3R,6R)-6-[4-[[4-(二氨基苯甲基苯基)苯基]甲基氨甲酰]哌拉嗪-1-羰基]氧-2,3,3a,5,6,6a-六氢呋喃[3,2-b]呋喃-3-基] 4-[[4-(二氨基基苯氨基)苯基]甲基氨甲酰]哌拉嗪-1-羧酸盐Chemical Name: (3R,3aS,6R,6aS)-3,6-Bis[4-[N-(4-guanidinobenzyl)carbamoyl]piperazin-1-y...
参考文献标题:Compsns.and methods for treating mast-cell inflammatory condition
文献作者:Gangloff,A.R.; Kuo,E.Y.-L.; Dener,J.M.; Rice,K.D.(Axys Pharmaceuticals,Inc.)
参考来源:US 6022969; WO 9609297

Bengamide B

[(3S,6S)-1-甲基-7-氧代-6-[[(E,2R,3R,4S,5R)-3,4,5-三羟基-2-甲氧基-8-甲基壬-6-烯酰基]氨基]氮杂环庚-3-基]十四烷酸酯Chemical Name: Tetradecanoic acid 1-methyl-7-oxo-6(S)-[3(R),4(S),5(R)-trihydroxy-2(R)-methoxy-8-methyl-6(E)-nonenami...
参考文献标题:Total synthesis of bengamides B and E
文献作者:Kinder,F.R.Jr.; Wattanasin,S.; Versace,R.W.; Bair,K.W.; Bontempo,J.; Green,M.A.; Lu,Y.J.; Marepalli,H.R.; Phillips,P.E.; Roche,D.; Tran,L.D.; Wang,R.; Waykole,L.; Xu,D.D.; Zabludoff,S.
参考来源:J Org Chem 2001,66(6),2118

Testosterone buciclate, CDB-1781, 20 Aet-1

[(8R,9S,10R,13S,14S,17S)-10,13-二甲基-3-氧代-1,2,6,7,8,9,11,12,14,15,16,17-十二氢环戊烯并[a]菲-17-基]4-丁基环己烷-1-羧酸酯Chemical Name: Testosterone trans-4-n-butylcyclohexylcarboxylate; [17beta(trans)]-(4-Butylcyclohexyl...
参考文献标题:Long-acting androgenic cpds.and pharmaceutical compsns.thereof
文献作者:Kim,H.K.; Blye,R.P.; Bialy,G.; Archer,S.; Fried,J.; Crabbe,P.; Djerassi,C.; Diczfalusy,E.R.
参考来源:US 4948790