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

QC-12

N-[2-羟基-5-(3,5,7-三羟基-4-氧代-4H-1-苯并吡喃-2-基)苯氧基羰基]甘氨酸Chemical Name: N-[2-Hydroxy-5-(3,5,7-trihydroxy-4-oxo-4H-1-benzopyran-2-yl)phenoxycarbonyl]glycine
CAS No. 201280-73-1
项目整合开发状态: Phase I/II
项目...
参考文献标题:Analogues or derivs.of quercetin (prodrugs)
文献作者:Golding,B.T.; Griffin,R.J.; Quarterman,C.P.; Slack,J.A.; Williams,J.G.(University of Birmingham)
参考来源:EP 0912541; JP 2000512988; WO 9749693

1400W, 1400W94

N-[3-(氨甲基)苄基]乙脒Chemical Name: N-[3-(Aminomethyl)benzyl]acetamidine
CAS No. 180001-34-7
项目整合开发状态: Preclinical
项目研究机构: GlaxoSmithKline (Originator)
合成路线:The reaction of m-xylenediamine (I) w...
参考文献标题:Acetamidine derivs.and their use as inhibitors for the nitric oxide synthase
文献作者:Oplinger,J.A.; Garvey,E.P.; Furfine,E.S.; Shearer,B.G.; Collins,J.L.(Glaxo Wellcome plc)
参考来源:EP 0799191; JP 1999500711; US 5866612; WO 9619440

FR-168888

N''-[3-(羟甲基)-5-(1H-吡咯-1-基)苯甲酰]鸟苷甲磺酸盐Chemical Name: N''-[3-(Hydroxymethyl)-5-(1H-pyrrol-1-yl)benzoyl]guanidine methanesulfonate
CAS No. 168620-46-0, 168620-45-9 (free base), 168620-05-1 (HCl)
项目整...
参考文献标题:Guanidine derivs.as inhibitors of Na+/H+ exchange in cells
文献作者:Kuno,A.; Inoue,Y.; Takasugi,H.; Mizuno,H.; Yamasaki,K.(Fujisawa Pharmaceutical Co.,Ltd.)
参考来源:EP 0699185; JP 1996511243; US 5824691; WO 9426709

JTE-607

N-[3,5-二氯-2-羟基-4-[2-(4-甲基-1-哌嗪基)乙氧基]苯甲酰]-L-苯丙氨酸乙基酯二盐酸Chemical Name: N-[3,5-Dichloro-2-hydroxy-4-[2-(4-methyl-1-piperazinyl)ethoxy]benzoyl]-L-phenylalanine ethyl ester dihydrochloride
CAS No. 188791...
参考文献标题:Amide compounds and use of the same
文献作者:Haruta,J.; Sakuma,K.; Watanabe,Y.(Japan Tobacco Inc.)
参考来源:EP 0849256

SB-237376

N-[3-[2-(3,4-二甲氧基苯基)乙基氨基]丙基]-4-硝基苯甲酰盐酸盐Chemical Name: N-[3-[2-(3,4-Dimethoxyphenyl)ethylamino]propyl]-4-nitrobenzamide hydrochloride
CAS No. 179258-62-9, 179258-59-4 (free base)
项目整合开发状态: Discon...
参考文献标题:Nitro-benzamides useful as anti-arrhythmic agents
文献作者:Nadler,G.M.M.G.; Martin,M.J.R.(SmithKline Beecham plc)
参考来源:EP 0788474; FR 2726267; JP 1998508013; US 5977179; WO 9613479

BIM-46068

N-[3-[2(S)-[2(R)-氨基-3-磺基丙基甲基]-3(S)-甲基戊基]-5,5-二甲基-4(R)-噻唑烷基羰基]-L-甲硫氨酸甲基酯Chemical Name: N-[3-[2(S)-[2(R)-Amino-3-sulfanylpropylamino]-3(S)-methylpentyl]-5,5-dimethyl-4(R)-thiazolidinylcarbonyl]-L-methio...
参考文献标题:Inhibitors of prenyl transferases
文献作者:Dong,Z.X.; Kim,S.H.(Biomeasure Inc.)
参考来源:WO 9800409

OPC-21268

N-[3-[4-[[4-(3,4-二氢-2-氧代-1(2H)-喹啉基)-1-哌啶基]羰基]苯氧基]丙基]乙酰胺Chemical Name: 1-[1-[4-[3-(Acetylamino)propoxy]benzoyl]piperidin-4-yl]-1,2,3,4-tetrahydro-2-quinolinone; N-[3-[4-[4-(2-Oxo-1,2,3,4-tetrahydro-1-q...
参考文献标题:Carbostyril derivs
文献作者:Ogawa,H.; Miyamoto,H.; Kondo,K.; Yamashita,H.; Nakaya,K.; Tominaga,M.; Yabuuchi,Y.(Otsuka Pharmaceutical Co.,Ltd.)
参考来源:EP 0382185; JP 1991173870; US 5225402; US 5436256; US 5652247

CP-199330

N-[3-[6-(7-氯-2-喹啉甲氧基)-4(R)-羟基-3,4-二氢-2H-1-苯并吡喃-3(S)-甲基]-4-甲氧基苯基]三氟甲烷磺酰胺Chemical Name: N-[3-[6-(7-Chloro-2-quinolinylmethoxy)-4(R)-hydroxy-3,4-dihydro-2H-1-benzopyran-3(S)-ylmethyl]-4-methoxyphenyl]tri...
参考文献标题:Sulfonamide derivs.of benzenefused hydroxy substd.cycloalkyl and heterocyclic ring cpds.
文献作者:Marfat,A.(Pfizer Inc.)
参考来源:EP 0665842; JP 1995508534; US 5641789; WO 9408996

SB-228357

N-[3-氟-5-(3-吡啶)苯基]-2,3-二氢-5-甲氧基-6-(三氟甲基)-1H-吲哚-1-羧酰胺Chemical Name: N-[3-Fluoro-5-(3-pyridyl)phenyl]-5-methoxy-6-(trifluoromethyl)indoline-1-carboxamide
CAS No. 181629-93-6
项目整合开发状态: Preclinical<...
参考文献标题:Indole derivs.as 5-HT receptor antagonist
文献作者:Gaster,L.M.; Wyman,P.A.; Mulholland,K.R.; Davies,D.T.; Duckworth,D.M.; Forbes,I.T.; Jones,G.E.(SmithKline Beecham plc)
参考来源:EP 0808312; JP 1998513442; US 5990133; WO 9623783

MMI-166

N-[4-(2-苯基-2H-四唑-5-基)苯基磺酰]-D-色氨酸Chemical Name: N-[4-(2-Phenyl-2H-tetrazol-5-yl)phenylsulfonyl]-D-tryptophan
CAS No. 193809-84-6, 352462-08-9
项目整合开发状态: Preclinical
项目研究机构: Shionogi (Originator...
参考文献标题:Sulfonated amino acid derivs.and metalloproteinase inhibitors containing the same
文献作者:Watanabe,F.; Tsuzuki,H.; Ohtani,M.(Shionogi & Co.Ltd.)
参考来源:EP 0950656; JP 2001316254; US 6207698; US 6235768; US 6441021; WO 9727174