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

ZK-811752, BX-471

ZK-811752(BX471)抑制剂 (2R)-1-[[[4-氯-2-(脲基)苯氧基]甲基]羰基]-2-甲基-4-(4-氟苄基)哌嗪 Chemical Name: N-[5-Chloro-2-[2-[4-(4-fluorobenzyl)-2(R)-methylpiperazin-1-yl]-2-oxoethoxy]phenyl]urea hydrochloride
CAS No. 2882...
参考文献标题:Piperazine derivs.and their use as anti-inflammatory agents
文献作者:Monahan,S.D.; Xu,W.; Morissey,M.M.; Bauman,J.G.; Ng,H.P.; Hesselgesser,J.E.; Liang,M.; Zheng,W.; Islam,I.; May,K.B.; Ghannam,A.F.; Buckman,B.O.; Horuk,R.; Wei,G.P.(Schering AG)
参考来源:US 6207665; WO 9856771

ZK-90055

ZK-90055盐酸盐Chemical Name: Methyl 4-(2-tert-butylamino-1-hydroxyethyl)-7-hy- droxyindole-2-carboxylate hydrochloride
CAS No. 84638-81-3
项目整合开发状态: Preclinical
项目研究机构: Schering AG (Originator) 参考文献标题:Indole derivatives pharmaceutical preparations based thereon and beta -receptor stimulation therewith
文献作者:Heindl,J.; Loge,O.(Schering AG)
参考来源:DE 3115993; EP 0062919; GB 2098205; JP 58004765; US 4835175

新产品编号:970275

α-亚甲基-γ-丁内酯Chemical Name: 3-Methylenedihydrofuran-2(3H)-one
CAS No. 547-65-9
项目整合开发状态: Preclinical
项目研究机构: Morishita Jintan (Originator)
合成路线:By condensation of ethyl oxalylbutyrolactone (...
参考文献标题:alpha-Methylene-gamma-lactone
文献作者:Aboul-Enein,H.Y.
参考来源:Drugs Fut 1980,5(7),352

alpha-Galactosylceramide, AGL-582, KRN-7000

α-半乳糖神经酰胺Chemical Name: (2S,3S,4R)-1-O-(alpha-D-Galactopyranosyl)-2-(N-hexacosanoylamino)-1,3,4-octadecatrienol; N-[1(S)-(alpha-D-Galactopyranosyloxymethyl)-2(S),3(R)-dihydroxyheptadecyl]hexacosanamid...
参考文献标题:Novel sphingoglycolipid and use thereof
文献作者:Higa,T.; Akimoto,K.; Koezuka,Y.; Sakai,T.; Morita,M.; Natori,T.(Kirin Brewery Co.,Ltd.)
参考来源:EP 0609437; JP 1993508706; US 5936076; WO 9305055

Dihydroqinghaosu, Artenimol, Dihydroartemisinin, DHA, Cotecxin

α-双氢青蒿素双氢青蒿素 Chemical Name: (3R,5aS,6R,8aS,9R,10RS,12R,12aR)-Decahydro-10-hydroxy-3,6,9-trimethyl-3, 12-epoxy-12H-pyrano[4,3-j]-1,2-benzodioxepine
CAS No. 81496-81-3 (alpha-isomer), 71939-50-9 (be...
参考文献标题:173.The chemistry of drugs.Part IV.Configurations of antimalarials derived from qinghaosu: Dihydroqinghaosu,artemether,and artesunic acid
文献作者:Lu,X.-D.; et al.
参考来源:Helv Chim Acta 1984,67(6),1515

Anecortave acetate, AL-3789, Retaane

δ-9(11)-氢化可的松醋酸酯Chemical Name: 21-Acetoxy-17alpha-hydroxypregna-4,9(11)-diene-3,20-dione
CAS No. 7753-60-8
项目整合开发状态: Phase III
项目研究机构: Alcon (Originator)
合成路线:Androstenedione (II) was conv...
参考文献标题:9-alpha-Hydroxy steroids and process for their preparation
文献作者:Batist,J.N.M.; Marx,A.F.; Van Zoest,W.J.; Kapur,J.C.(Gist-Brocades NV)
参考来源:EP 0263569; JP 1989500907; WO 8802753

Flavodilol maleate, PR-87730L

丁-2-烯二酸:7-(2-羟基-3-丙基氨基丙氧基)-2-苯基苯并吡喃-4-酮黄酮地洛 Chemical Name: (?-7-[2-Hydroxy-3-(propylamino)propoxy]-2-phenyl-4H-1-benzopyran-4-one (Z)-2-butenedioate (1:1) (salt); (?-7-(2-Hydroxy-3-(propylamino)prop...
参考文献标题:Antihypertensive agents
文献作者:Wu,E.S.-C.(Pennwalt Corp.)
参考来源:EP 0064165; US 4501755

KB-R7785

丁二酰胺,N1-羟基-2-甲基-N4-[(1S)-2-(甲基氨基)-2-氧基-1-苯乙基]-3-(2-甲基丙基)-,(2S,3R)-Chemical Name: N-[4-(Hydroxyamino)-2(R)-isobutyl-3(S)-methylsuccinyl]-L-2-phenylglycine methylamide
CAS No. 168158-16-5, 168393-60-...
参考文献标题:Acylphenylglycine deriv.and preventive and remedy for diseases caused by increased collagenase activity containing said cpd.as active ingredient
文献作者:Hirayama,R.; Tsukida,T.; Yamamoto,M.; Ikeda,S.; Sakamoto,F.; Obata,Y.; Matsuo,K.(Kanebo Pharmaceuticals,Ltd.)
参考来源:EP 0712838; JP 1995101925; US 5795891; WO 9504715

Bufuralol, Ro-34787

丁呋洛尔Chemical Name: alpha-[(tert-Butylamino)methyl]-7-ethyl-2-benzofuranmethanol
CAS No. 54340-62-4
项目整合开发状态: Phase III
项目研究机构: Roche (Originator), Helsinn (Licensee)
合成路线:The condensation ...
参考文献标题:Verfahren zur Herstellung von Benzofuranderivaten
文献作者:Osbon,J.M.; et al.(Bristol-Myers Squibb Co.)
参考来源:CH 498109; DE 1543653; FR 1479002; FR 6011M; GB 1106057; NL 6606441

Bufezolac, LM-22070

丁苯唑酸Chemical Name: 2-(1-Isobutyl-3,4-diphenyl-1H-pyrazol-5-yl)acetic acid
CAS No. 50270-32-1
项目整合开发状态: Not Determined
项目研究机构:
合成路线:It can be prepared in two different ways:1) The reaction...
参考文献标题:
文献作者:Gueremy,C.; Renault,C.
参考来源:BE 796465; GB 1387306; US 3984731