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

ES-6864

L-环戊酰-戊酰,5-环己基-2,4,5-三氧基-N-[2-(4-吗啡烯基)乙基]-4-[[(2S)-2-[[(2R)-4-(4-甲基苯丙基)-2-(1-萘基甲基)-1,4-二氧基丁基]氨基]-1-羟基-3-(4-噻唑基)丙基]氨基]-(9CI)Chemical Name: N-[N-[3-(Morpholinocarbonyl)-2(R)-(1-naphthylmethyl)propionyl]...
参考文献标题:New renin-inhibitory oligopeptides,their preparation and their use
文献作者:Kataoko,M.; Yabe,Y.; Iijima,Y.; Takahagi,H.; Koike,H.; Kokubu,T.; Hiwada,K.; Morisawa,Y.(Sankyo Co.,Ltd.)
参考来源:EP 0274259; JP 1989063559; US 5378690

NSC-650426, SPK-241, KRN-5500

L-甘油-b-L-甘露-七基吡酯基胺,4-脱氧-4-[[2-[[(2E,4E)-1-氧基-2,4-四氟化铀-1-酰基]氨基]-N-1H-嘌呤-6-基-Chemical Name: N6-[4-Deoxy-4-[N2-[2(E),4(E)-tetradecadienoyl]glycylamino]-L-glycero-beta-L-manno-heptopyranosyl]adenine; N6-[...
参考文献标题:Spicamycin derivs.and the use thereof
文献作者:Otake,N.; Kawai,H.; Kawasaki,T.; Odagawa,A.; Kamishohara,M.; Sakai,T.(Kirin Brewery Co.,Ltd.)
参考来源:EP 0525479; JP 1993186494; US 5461036; US 5631238

Arginine pyroglutamate

L-精氨酸-L-焦谷氨酸盐Chemical Name: L-Arginine 5-oxo-L-proline
CAS No. 56265-06-6
项目整合开发状态: Biological Testing
项目研究机构:
合成路线:By vacuum evaporation of a refluxed solution of pyroglutamic acid (II) ...
参考文献标题:Chemistry and pharmacology of argine-pyroglutamate
文献作者:Provenzano,P.M.; et al.
参考来源:Arzneim-Forsch Drug Res 1977,27(8),1553

LY-335518

L-谷氨酸,N-(2-(2,4-二氨基-1,5,6,7-四氢吡啶-6-基)乙基苯甲酰)-Chemical Name: N-[4-[2-(2,4-Diamino-5,6,7,8-tetrahydropyrido[2,3-d]pyrimidin-6-yl)ethyl]benzoyl]-L-glutamic acid
CAS No. 95674-54-7
项目整合开发状态: Preclini...
参考文献标题:The synthesis and biological activity of a series of 2,4-diaminopyrido[2,3-d]pyrimidine based antifolates as antineoplastic and antiarthritic agents
文献作者:Gossett,L.S.; Habeck,L.L.; Shackelford,K.A.; Mendelsohn,L.G.; Gates,S.B.; Worzalla,J.F.; Self,T.D.; Theobald,K.S.; Andis,S.L.; Schultz,R.M.; Shih,C.
参考来源:Bioorg Med Chem Lett 1999,9(1),75

Nifalatide hydrochloride, BW-942C

L-酪氨酰-D-蛋氨酰甘氨酰-4-硝基苯基丙氨酰-L-脯氨酸酰胺S-氧化盐酸尼法那塔 Chemical Name: L-Tyrosyl-D-methionylglycyl-4-nitrophenylalanyl-L-prolinamide S-oxide hydrochloride; L-Tyrosyl-gamma-(methylsulfinyl)-D-alpha-aminobutyrylgly...
参考文献标题:Treatment of diarrhoea and dysentery
文献作者:Wilkinson,S.(Glaxo Wellcome Inc.)
参考来源:JP 7992938

PRL-2915

L-阿拉尼胺,4-氯-L-苯丙酰-D-半氨基-3-(3-吡啶基)-L-异丙酰-D-色氨酸-L-赖氨酸-3-甲基-甲基-L-戊醇-L-半氨酸-3-(2-萘基)-,环状(2-7)-二硫化物Chemical Name: 4-Chloro-L-phenylalanyl-D-cysteinyl-3-(3-pyridyl)-L-alanyl-D-tryptophyl-L-lysyl-3-(methyl)-L-...
参考文献标题:Somatostatin antagonists
文献作者:Murphy,W.; Coy,D.H.; Morgan,B.(Biomeasure Inc.; Tulane Educational Fund)
参考来源:WO 9824807

Pelitrexol, AG-2037, AG-2038((6R)-isomer), AG-2032(racemate)

N-((5-(2-((6S)-2-氨基-1,4,5,6,7,8-六氢-4-氧代吡啶并[2,3-D]嘧啶-6-基)乙基)-4-甲基-2-噻吩)甲酰基)-L-谷氨酸Chemical Name: N-[5-[2-[2-Amino-4-oxo-3,4,5,6,7,8-hexahydropyrido[2,3-d]pyrimidin-6(S)-yl]ethyl]-4-methylthien-2-ylcarbo...
参考文献标题:Cpds.useful as antiproliferative agents and GARFT inhibitors
文献作者:Varney,M.D.; Romines,W.H.(Agouron Pharmaceuticals,Inc.)
参考来源:WO 9603406

Mesulergine hydrochloride, CU-32085, CQ-32085

N'-((8alpha)-1,6-二甲基麦角灵-8-基)-N,N-二甲基氨基磺酰胺单盐酸盐美舒麦角 Chemical Name: N'-(1,6-Dimethylergolin-8alpha-yl)-N,N-dimethylsulfamide monohydrochloride; 1,6-Dimethyl-8alpha-(N,N-dimethylsulfamoylamino)ergoline m...
参考文献标题:Sulfonamido and sulfamoylamino-ergoline-I derivatives
文献作者:Stuetz,P.; Fehr,T.; Stadler,P.(Novartis AG)
参考来源:BE 0849745; CA 1092100; CH 620441; DE 2656344; ES 454442; FR 2336135; GB 1567484; JP 7778900; NL 7614018

DMP-904, SP-904

N-(1-乙基丙基)-3-(4-甲氧基-2-甲基苯基)-2,5-二甲基吡唑并[1,5-A]嘧啶-7-胺Chemical Name: 7-(1-Ethylpropylamino)-3-(4-methoxy-2-methylphenyl)-2,5-dimethylpyrazolo[1,5-a]pyrimidine
CAS No. 202579-74-6
项目整合开发状态: Preclini...
参考文献标题:Azolo triazines and pyrimidines
文献作者:Arvanitis,A.G.; Chorvat,R.J.(DuPont Pharmaceuticals Co.)
参考来源:US 6124289; WO 9803510

T-1317, T-0901317

N-(2,2,2-三氟乙基)-N-[4-[2,2,2-三氟-1-羟基-1-(三氟甲基)乙基]苯基]-苯磺酰胺Chemical Name: N-(2,2,2-Trifluoroethyl)-N-[4-[2,2,2-trifluoro-1-hydroxy-1-(trifluoromethyl)ethyl]phenyl]benzenesulfonamide
CAS No. 293754-55-9<...
参考文献标题:Compsns.and methods for raising HDL cholesterol levels
文献作者:Shan,B.(Tularik Inc.)
参考来源:WO 0103705